Preparation and Optical Properties of Infrared Transparent 3Y-TZP Ceramics

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Chuanfeng Wang

2017-04-01

Full Text Available In the present study, a tough tetragonal zirconia polycrystalline (Y-TZP material was developed for use in high-speed infrared windows and domes. The influence of the preparation procedure and the microstructure on the material’s optical properties was evaluated by SEM and FT-IR spectroscopy. It was revealed that a high transmittance up to 77% in the three- to five-micrometer IR region could be obtained when the sample was pre-sintered at 1225 °C and subjected to hot isostatic pressing (HIP at 1275 °C for two hours. The infrared transmittance and emittance at elevated temperature were also examined. The in-line transmittance remained stable as the temperature increased to 427 °C, with degradation being observed only near the infrared cutoff edge. Additionally, the emittance property of 3Y-TZP ceramic at high temperature was found to be superior to those of sapphire and spinel. Overall, the results indicate that Y-TZP ceramic is a potential candidate for high-speed infrared windows and domes.

Deposition of SiOx thin films on Y-TZP by reactive magnetron sputtering: influence of plasma parameters on the adhesion properties between Y-TZP and resin cement for application in dental prosthesis

Directory of Open Access Journals (Sweden)

José Renato Calvacanti de Queiroz

2011-01-01

Full Text Available In this paper SiOx thin films were deposited on Y-TZP ceramics by reactive magnetron sputtering technique in order to improve the adhesion properties between Y-TZP and resin cement for applications in dental prosthesis. For fixed cathode voltage, target current, working pressure and target-to-substrate distance, SiOx thin films were deposited at different oxygen concentrations in the Ar+O2 plasma forming gas. After deposition processes, SiOx thin films were characterized by profilometry, energy dispersive spectroscopy (EDS, optical microscopy and scanning electron microscopy (SEM. Adhesion properties between Y-TZP and resin cement were evaluated by shear testing. Results indicate that films deposited at 20%O2 increased the bond strength to (32.8 ± 5.4 MPa. This value has not been achieved by traditional methods.

The effect of some factors on Ms and SME in Ce-TZP ceramics

International Nuclear Information System (INIS)

Jiang, B.; Tu, J.; Hsu, T.Y.; Qi, X.; Zheng, X.; Zhong, J.

1992-01-01

As known to all, shape memory behaviour has been observed in a variety of metallic alloys. This phenomenon, however, is not only observed in that field but also in other materials recently, such as in polymers, intermetallic compounds and ceramics, especially in zirconia ceramics. Swain observed the shape recovery of a bent magnesia-partially-stabilized zirconia (Mg-PSZ) bar upon heating above a certain temperature. The maximum deflection which was nearly completely recovered on heating is about 300 μm. Chen et al., investigated the pseudoelasticity and shape memory effect (SME) in ceria-stabilized tetragonal zirconia polycrystals (Ce-TZP) containing 12 mol% CeO 2 . Wang et al., also observed the SME in Ce-TZP containing 10 mol% CeO 2 . In this paper, the authors would like to introduce some of results conducted recently in our group on SME in Ce-TZP ceramics

The phase stability and toughening effect of 3Y-TZP dispersed in the lanthanum zirconate ceramics

International Nuclear Information System (INIS)

Wang, Yanfei; Xiao, Ping

2014-01-01

The low fracture toughness of lanthanum zirconate (La 2 Zr 2 O 7 , LZ) greatly impedes its wide application as thermal barrier coatings (TBC). The 3 mol% Y 2 O 3 -stabilized tetragonal zirconia polycrystals (3Y-TZP) have been introduced to toughen the brittle LZ ceramics. The dispersive 3Y-TZP undergoes a simultaneous t–m transformation upon cooling below a critical volume fraction x of 3Y-TZP, above which its tetragonal phases can however be preserved. The different stabilities of 3Y-TZP second phases arise from a variation of residual tensile stress within them. The fracture toughness has been greatly improved by dispersing the tetragonal particulates (t-3YSZ) in the LZ matrix and the primary toughening mechanisms are phase transformations of the dispersive second phases and the residual compressive stress within the matrix. An anticipated increase of fracture toughness from the ferroelastic toughening and the residual compressive stress toughening highlights the great potentials to improve coating durability by depositing t′-3YSZ/LZ composite TBCs by the industrial non-equilibrium route

Local administration of a hedgehog agonist accelerates fracture healing in a mouse model

International Nuclear Information System (INIS)

Kashiwagi, Miki; Hojo, Hironori; Kitaura, Yoshiaki; Maeda, Yujiro; Aini, Hailati; Takato, Tsuyoshi; Chung, Ung-il; Ohba, Shinsuke

2016-01-01

Bone fracture healing is processed through multiple biological stages including the transition from cartilaginous callus to bony callus formation. Because of its specific, temporal and indispensable functions demonstrated by mouse genetic studies, Hedgehog (Hh) signaling is one of the most potent signaling pathways involved in these processes, but the effect of Hh-signaling activation by small compounds on the repair process had not yet been addressed. Here we examined therapeutic effects of local and one shot-administration of the Hh agonist known as smoothened agonist (SAG) on bone fracture healing in a mouse model. A quantitative analysis with three-dimensional micro-computed tomography showed that SAG administration increased the size of both the cartilaginous callus and bony callus at 14 days after the surgery. A histological analysis showed that SAG administration increased the number of cells expressing a proliferation marker and a chondrocyte marker in cartilaginous callus as well as the cells expressing an osteoblast marker in bony callus. These results indicate that the SAG administration resulted in an enhancement of callus formation during bone fracture healing, which is at least in part mediated by an increase in chondrocyte proliferation in cartilaginous callus and the promotion of bone formation in bony callus. Therapeutic strategies with a SAG-mediated protocol may thus be useful for the treatment of bone fractures. - Highlights: • Local administration of a Hh agonist accelerates callus formation. • The Hh agonist administration promotes chondrocyte proliferation in the soft callus. • The Hh agonist administration increases osteoblast formation in the hard callus.

Elimination of ion losses in the EhGP-10-1 charge-exchange accelerator

International Nuclear Information System (INIS)

Fridrikh, M.

1986-01-01

To improve the ion transit factor in the EhGP-10-1 charge-exchange accelerator the injector ion-optical properties are studied. The injector operates at constant high voltage U a -23 kV. Using an immersion lens the negative ion energy before entering the accelerating tube is increased up to energy proportional to the conductor voltage. A single electrostatic lens provides a cross-over in the vicinity of immersion lens. By reducing the electric field gradient at the accelerating tube inlet, optimizing input electrode voltage and shifting the single lens by 0.26 m towards the accelerating tube inlet almost full beam transit is attained at all conductor voltages

Crystal orientation mapping applied to the Y-TZP/WC composite

CERN Document Server

Faryna, M; Sztwiertnia, K

2002-01-01

Crystal orientation measurements made by electron backscattered diffraction (EBSD) in the scanning electron microscope (SEM) and microscopic observations provided the basis for a quantitative investigation of microstructure in an yttria stabilized, tetragonal zirconia-based (Y-TZP) composite. Automatic crystal orientation mapping (ACOM) in a SEM can be preferable to transmission electron microscopy (TEM) for microstructural characterization, since no sample thinning is required, extensive crystal data is already available, and the analysis area is greatly increased. A composite with a 20 vol.% tungsten carbide (WC) content was chosen since it revealed crystal relationships between the matrix and carbide phase already established by TEM analysis. However, this composite was difficult to investigate in the EBSD/ SEM since it is non-conductive, the Y-TZP grain size is of the order of the system resolution, and the sample surface, though carefully prepared, reveals a distinctive microtopography. In this paper, so...

The effect of continuous application of MDP-containing primer and luting resin cement on bond strength to tribochemical silica-coated Y-TZP.

Science.gov (United States)

Lim, Myung-Jin; Yu, Mi-Kyung; Lee, Kwang-Won

2018-05-01

This study investigated the effect of continuous application of 10-methacryloyloxydecyldihydrogen phosphate (MDP)-containing primer and luting resin cement on bond strength to tribochemical silica-coated yttria-stabilized tetragonal zirconia polycrystal (Y-TZP). Forty bovine teeth and Y-TZP specimens were prepared. The dentin specimens were embedded in molds, with one side of the dentin exposed for cementation with the zirconia specimen. The Y-TZP specimen was prepared in the form of a cylinder with a diameter of 3 mm and a height of 10 mm. The bonding surface of the Y-TZP specimen was sandblasted with silica-coated aluminium oxide particles. The forty tribochemical silica-coated Y-TZP specimens were cemented to the bovine dentin (4 groups; n = 10) with either an MDP-free primer or an MDP-containing primer and either an MDP-free resin cement or an MDP-containing resin cement. After a shear bond strength (SBS) test, the data were analyzed using 1-way analysis of variance and the Tukey test (α = 0.05). The group with MDP-free primer and resin cement showed significantly lower SBS values than the MDP-containing groups ( p Y-TZP was the best choice among the alternatives tested in this study.

Influence of firing time and framework thickness on veneered Y-TZP discs curvature.

Science.gov (United States)

Jakubowicz-Kohen, Boris D; Sadoun, Michaël J; Douillard, Thierry; Mainjot, Amélie K

2014-02-01

The objective of the present work was to study the curvature of very thinly, veneered Y-TZP discs of different framework thicknesses submitted to different firing times. Fifteen 20-mm-wide Y-TZP discs were produced in three different thicknesses: 0.75, 1, 1.5mm. One disc from each group was left unveneered while the others were layered with a 0.1mm veneering ceramic layer. All discs underwent five firing cycles for a total cumulative firing time of 30 min, 1, 2, 5 and 10h at 900°C. The curvature profile was measured using a profilometer after the veneering process and after each firing cycle respectively. A fitted curve was then used to estimate the, curvature radius. The coefficient of thermal expansion (CTE) measurements were taken on veneering, ceramic and Y-TZP beam samples that underwent the same firing schedule. Those data were used to calculate the curvature generated by CTE variations over firing time. All bilayered samples exhibited a curvature that increased over firing time inversely to framework thickness. However non-veneered samples did not exhibit any curvature modification. The results of the present study reveal that even a very thin veneer layer (0.1mm) can induce a significant curvature of Y-TZP discs. The dilatometric results showed that Tg and CTE, variations are not sufficient to explain this curvature. A chemical-induced zirconia volume, augmentation located at the framework sub-surface near the interface could explain the sample, curvature and its increase with firing time. Copyright © 2013 Academy of Dental Materials. Published by Elsevier Ltd. All rights reserved.

Mechanical characterization of the 3Y-TZP co-doped with yttria and niobia Equimolar addition

International Nuclear Information System (INIS)

Assis, Joao Marcos Kruszynski de; Nono, Maria do Carmo de Andrade; Dorat, Daniele Ramos; Fonseca, Flavia Baccaro; Reis, Danieli Aparecida

2010-01-01

The main goal of this work is to study the effect of the yttria and niobia equimolar addition in the 3Y-TZP on the mechanical properties (hardness, fracture toughness and four point bending strength) aiming to get a stable tetragonal phase (t´) under applied stress, to use as TBC´s. Four compositions with equimolar addition of yttria and niobia in the 3Y-TZP were produced, 13%, 14.5%, 16% and 17.5%. The mixtures were prepared in high energy ball milling for 10 minutes and the samples prepared on uniaxial and isostatic pressing. The selected temperature sintering was 1.550 deg C for 1 hour. Analyses of X-Ray Diffraction, hardness, fracture toughness and four point bending strength were performed. An increase on the mechanical properties analyzed was expected with yttria and niobia addition in comparison to 3Y-TZP, but instead a decrease was observed after these additions. (author)

Preparación y densificación de monolitos cerámicos nanoestructurados de Y-TZP por Sol-gel

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Tartaj, J.

1999-12-01

Full Text Available Y-TZP seeded gel monoliths have been prepared by a sol-gel method based on the coprecipitation of Zr4+ and Y3+ precursors as hydroxides and the stabilisation of the suspension in pure ethanol with a disc turbine. The addition of solid Y-TZP nanometer- size seed particles into the Y-TZP precursor solution play a crucial role during cristallisation and densification of monoliths. Basically, induced a preferential nucleation, which enhance the crystallisation kinetics and the activation energy is reasonably lowered. As a result of the increased nucleation frequency for the crystallisation process a well-developed homogeneous porous microstructure is obtained facilitating the sintering and so the densification at lower temperatures. In this way, Y-TZP highly densificated ceramics monoliths have been obtained at 1050ºC, with a grain size within the nanometer range.

Monolitos de geles de Y-TZP semillados han sido preparados por un método de sol-gel basado en la coprecipitación de precursores de Zr4+ y Y3+ en forma de hidróxidos y la estabilización de la suspensión en etanol puro con una turbina de disco. La adición de partículas nanométricas de Y-TZP cristalizadas a la solución precursora juega un papel fundamental durante la cristalización y densificación de los monolitos. Básicamente, se induce una nucleación preferente, que mejora la cinética de cristalización y reduce razonablemente la energía de activación. Como resultado del incremento de la frecuencia de nucleación para el proceso de cristalización, se obtiene una microestructura porosa, homogénea y bien desarrollada que facilita la sinterización y por tanto la densificación del material a temperaturas más bajas. De esta forma, monolitos cerámicos de Y-TZP altamente densificados han sido obtenidos a 1050ºC, con un tamaño de grano dentro de un rango nanométrico.

Y-TZP zirconia regeneration firing: Microstructural and crystallographic changes after grinding.

Science.gov (United States)

Ryan, Daniel Patrick Obelenis; Fais, Laiza Maria Grassi; Antonio, Selma Gutierrez; Hatanaka, Gabriel Rodrigues; Candido, Lucas Miguel; Pinelli, Ligia Antunes Pereira

2017-07-26

This study evaluated microstructural and crystallographic phase changes after grinding (G) and regeneration firing/anneling (R) of Y-TZP ceramics. Thirty five bars (Lava TM and Ice Zirkon) were divided: Y-TZP pre-sintered, control (C), regeneration firing (R), dry grinding (DG), dry grinding+regeneration firing (DGR), wet grinding (WG) and wet grinding+regeneration firing (WGR). Grinding was conducted using a diamond bur and annealing at 1,000°C. The microstructure was analyzed by SEM and the crystalline phases by X-ray diffraction (XRD). XRD showed that pre-sintered specimens contained tetragonal and monoclinic phases, while groups C and R showed tetragonal, cubic and monoclinic phases. After grinding, the cubic phase was eliminated in all groups. Annealing (DGR and WGR) resulted in only tetragonal phase. SEM showed semi-circular cracks after grinding and homogenization of particles after annealing. After grinding, surfaces show tetragonal and monoclinic phases and R can be assumed to be necessary prior to porcelain layering when grinding is performed.

Graphite and PMMA as pore formers for thermoplastic extrusion of porous 3Y-TZP oxygen transport membrane supports

DEFF Research Database (Denmark)

Bjørnetun Haugen, Astri; Gurauskis, Jonas; Kaiser, Andreas

2016-01-01

A gas permeable porous support is a crucial part of an asymmetric oxygen transport membrane (OTM). Here, we develop feedstocks for thermoplastic extrusion of tubular, porous 3Y-TZP (partially stabilized zirconia polycrystals, (Y2O3)0.03(ZrO2)0.97)) ceramics, using graphite and/or polymethyl....... This demonstrates the suitability of thermoplastic extrusion for fabrication of porous 3Y-TZP OTM supports, or for other technologies requiring porous ceramics....

Injection molding of Y-TZP powders prepared by colloidal processing

International Nuclear Information System (INIS)

Kimura, Y.; Mineshita, O.; Kaga, T.; Tokinaga, T.; Obitsu, M.

1991-01-01

TZP powders containing 3mol% Y 2 O 3 were prepared from ZrOCl 2 solution via an aqueous colloidal suspension of ZrO 2 . Processing variables were optimized to obtain powders suitable for injection molding. Wettability of powders with binders, fluidity of melting compound, removal of binder from green body, and properties of sintered body were investigated

Performance of 3Y-TZP bioceramics under cyclic fatigue loading

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Renato Chaves Souza

2008-03-01

Full Text Available In this work, the static mechanical properties and cyclic fatigue life of 3 mol. (% Y2O3-stabilized tetragonal zirconia polycrystalline (3Y-TZP ceramics were investigated. Pre-sintered samples were sintered in air at 1600 °C for 120 minutes, and characterized by X ray diffraction and scanning electronic microscopy. Hardness and fracture toughness were determined by Vicker's indentation method, and Modulus of Rupture was determined by four-point bending testing. Fully dense sintered samples, near to 100% of theoretical density, presented hardness, fracture toughness and bending strength of 13.5 GPa, 8.2 MPa.m½ and 880 MPa, respectively. The cyclic fatigue tests were also realized using four-point bending testing, within a frequency of 25 Hz and stress ratio R of 0.1. The increasing of load stress lead to decreasing of the number of cycles and the run-out specimens number. The tetragonal-monoclinic (t-m ZrO2-transformation observed by X ray diffraction contributes to the increasing of the fatigue life. The 3Y-TZP samples clearly presents a range of loading conditions where cyclic fatigue can be detected.

Surface roughness and hardness of yttria stabilized zirconia (Y-TZP after 10 years of simulated brushing

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Lucas Miguel Candido

Full Text Available Introduction: The Y-TZP zirconia used for prosthetic infrastructure, in some clinical situations, can be exposed to the oral environment. In these situations, a polished surface without changes is extremely important. Objective: The aim of this study was to evaluate the mean roughness (Ra and Vickers hardness of Y-TZP zirconia (Lava™ after simulating ten years of brushing. Material and method: Thirty-six Y-TZP bar-shaped specimens (20mm X 4mm X 1.2mm were divided into three groups: storage in distilled water (DW, n=12, control; brushing with distilled water (BDW, n=12 and brushing with distilled water and fluoride toothpaste (BFT, n=12. Brushing was performed using a brushing machine with a soft-bristled toothbrush, simulating 10 years of brushing (878.400 cycles, 100gf. The mean roughness (Ra in μm and Vickers hardness (VHN of all specimens were measured twice: before and after the experimental treatment, in profilometer and microhardness tester (500gf, 30 seconds, respectively. Data were analyzed using the two-way ANOVA test (α = 0.05. Result: The interaction between groups was not significant for roughness (p = 0.701 nor for hardness (p = 0.928. The final averages for Ra (μm were equal to: DW - 0.63; BDW - 0.64; and, BFT - 0.68. The final averages for Vickers hardness (VHN were: DW - 1301.16; BDW - 1316.60; and, BFT - 1299.58. Conclusion: It was concluded that the brushing with distilled or fluoridated toothpaste was not able to change the roughness and hardness of Y-TZP zirconia used in this study.

Effect of low-temperature aging on the mechanical behavior of ground Y-TZP

NARCIS (Netherlands)

Pereira, G.K.R.; Amaral, M.; Cesar, P.F.; Bottino, M.C.; Kleverlaan, C.J.; Valandro, L.F.

2015-01-01

This study evaluated the effects of low-temperature aging on the surface topography, phase transformation, biaxial flexural strength, and structural reliability of a ground Y-TZP ceramic. Disc-shaped specimens were manufactured and divided according to two factors: "grinding" - without grinding

Ageing kinetics and strength of airborne-particle abraded 3Y-TZP ceramics.

Science.gov (United States)

Cotič, Jasna; Jevnikar, Peter; Kocjan, Andraž

2017-07-01

The combined effects of alumina airborne-particle abrasion and prolonged in vitro ageing on the flexural strength of 3Y-TZP ceramic have been studied. The aim was to identify the different effects on the surface and subsurface regions that govern the performance of this popular bioceramic known for its susceptibility to low-temperature degradation (LTD). As-sintered or airborne-particle abraded 3Y-TZP discs were subjected to ageing at 134°C for up to 480h. Biaxial flexural strength was measured and the relative amount of monoclinic phase determined using X-ray diffraction. The transformed zone depth (TZD) was observed on cross-sections with scanning electron microscopy coupled with a focused ion beam. Segmented linear regression was used to analyze the flexural strength and TZD as functions of the ageing time. A two-step linear ageing kinetics was detected in airborne-particle abraded specimens, reflecting the different microstructures through which the LTD proceeds into the bulk. A 10μm thick altered zone under the abraded surface was involved in both the surface strengthening and the increased ageing resistance. When the zone was annihilated by the LTD, the strength of the ceramic specimens and the speed of LTD returned to the values measured before abrasion. Even at prolonged ageing times, the strength of abraded groups was not lower than that of as-sintered groups. Both the ageing kinetics and the flexural strength were prominently affected by airborne-particle abrasion, which altered the subsurface microstructure and phase composition. Airborne-particle abrasion was not harmful to the 3Y-TZP ceramics' stability. Copyright © 2017 The Academy of Dental Materials. Published by Elsevier Ltd. All rights reserved.

Synthesis and crystallization behavior of 3 mol% yttria stabilized tetragonal zirconia polycrystals (3Y-TZP) nanosized powders prepared using a simple co-precipitation process

Energy Technology Data Exchange (ETDEWEB)

Hsu, Yu-Wei [Graduate Institute of Applied Science, National Kaohsiung University of Applied Sciences, 415 Chien-Kung Road, Kaohsiung 80782, Taiwan (China); Yang, Ko-Ho, E-mail: yangkoho@cc.kuas.edu.tw [Graduate Institute of Applied Science, National Kaohsiung University of Applied Sciences, 415 Chien-Kung Road, Kaohsiung 80782, Taiwan (China); Department of Mold and Die Engineering, National Kaohsiung University of Applied Sciences, 415 Chien-Kung Road, Kaohsiung 80782, Taiwan (China); Chang, Kuo-Ming [Department of Mechanical Engineering, National Kaohsiung University of Applied Sciences, 415 Chien-Kung Road, Kaohsiung 80782, Taiwan (China); Dental Materials Research Center, National Kaohsiung University of Applied Sciences, 415 Chien-Kung Road, Kaohsiung 80782, Taiwan (China); Yeh, Sung-Wei [Metal Industries Research and Development Centre, 1001 Kaohsiung Highway, Kaohsiung 811, Taiwan (China); Wang, Moo-Chin, E-mail: mcwang@kmu.edu.tw [Department of Fragrance and Cosmetics Science, Kaohsiung Medical University, 100, Shihchuan 1st Road, Kaohsiung 80728, Taiwan (China)

2011-06-16

Highlights: > The thermal behavior of 3Y-TZP precursor powders had been investigated. > The crystallization behavior of 3Y-TZP nanopowders had been investigated. > The activation energy for crystallization of tetragonal ZrO{sub 2} was obtained. > The growth morphology parameter n is approximated as 2.0. > The crystallites show a plate-like morphology. - Abstract: The synthesis and crystallization behavior of 3 mol% yttria stabilized tetragonal zirconia polycrystals (3Y-TZP) nanopowders prepared using a simple co-precipitation process at 348 K and pH = 7 were investigated using differential scanning calorimetry/thermogravimetry (DSC/TG), an X-ray diffractometer (XRD), the Raman spectra, transmission electron microscopy (TEM), selected area electron diffraction (SAED), and an energy dispersive spectrometer (EDS). The activation energy of tetragonal ZrO{sub 2} crystallization from 3Y-TZP freeze-dried precursor powders using a non-isothermal method, namely, 169.2 {+-} 21.9 kJ mol{sup -1}, was obtained. The growth morphology parameter n was approximated as 2.0, which indicated that it had a plate-like morphology. The XRD, Raman spectra, and SAED patterns showed that the phase of the tetragonal ZrO{sub 2} was maintained at 1273 K. The crystallite size of 3Y-TZP freeze-dried precursor powders calcined at 1273 K for 5 min was 21.3 nm.

Synthesis and crystallization behavior of 3 mol% yttria stabilized tetragonal zirconia polycrystals (3Y-TZP) nanosized powders prepared using a simple co-precipitation process

International Nuclear Information System (INIS)

Hsu, Yu-Wei; Yang, Ko-Ho; Chang, Kuo-Ming; Yeh, Sung-Wei; Wang, Moo-Chin

2011-01-01

Highlights: → The thermal behavior of 3Y-TZP precursor powders had been investigated. → The crystallization behavior of 3Y-TZP nanopowders had been investigated. → The activation energy for crystallization of tetragonal ZrO 2 was obtained. → The growth morphology parameter n is approximated as 2.0. → The crystallites show a plate-like morphology. - Abstract: The synthesis and crystallization behavior of 3 mol% yttria stabilized tetragonal zirconia polycrystals (3Y-TZP) nanopowders prepared using a simple co-precipitation process at 348 K and pH = 7 were investigated using differential scanning calorimetry/thermogravimetry (DSC/TG), an X-ray diffractometer (XRD), the Raman spectra, transmission electron microscopy (TEM), selected area electron diffraction (SAED), and an energy dispersive spectrometer (EDS). The activation energy of tetragonal ZrO 2 crystallization from 3Y-TZP freeze-dried precursor powders using a non-isothermal method, namely, 169.2 ± 21.9 kJ mol -1 , was obtained. The growth morphology parameter n was approximated as 2.0, which indicated that it had a plate-like morphology. The XRD, Raman spectra, and SAED patterns showed that the phase of the tetragonal ZrO 2 was maintained at 1273 K. The crystallite size of 3Y-TZP freeze-dried precursor powders calcined at 1273 K for 5 min was 21.3 nm.

3Y-TZP/Si2N2O composite obtained by pressureless sintering

International Nuclear Information System (INIS)

Santos, Carlos Augusto Xavier

2006-01-01

Zirconia 3YTZP presents excellent properties at room temperature. These properties decrease as the temperature increases because high temperature acts negatively over the stress induced transformation toughening in the matrix. The addition of Si 3 N 4 and SiC in a Y-TZP matrix is very interesting because leads to formation of silicon oxynitride and it increases the mechanical properties like toughness and hardness. Certainly the mechanical properties increment is limited by several difficulties which have appeared during processing and heating of these materials. This paper studies the Y-TZP/Si 2 N 2 0 pressureless sintered composite, under different temperatures, showing the behavior of 20 vol %Si 3 N 4 -SiC when added in YTZP matrix and heated under no pressure system. Al 2 O 3 and Y 2 O 3 were used as sintering aids. The mixture was milled and molded by cold isostatic pressure. Samples were heated at 1500 deg, 1600 deg and 17000 deg C x 2h without pressure under atmospheric conditions using Si 3 N 4 bed-powder. Samples were characterized by XRD and density, hardness, toughness, bending strength were measured. The structure of the material was observed in SEMITEM/EPMA to verify the distribution and composition of the materials in the composite and the contact between filler surface and the matrix. The formation of SiON 2 was observed in the sintered material due to reaction between both nitride and carbide with Y - TZP matrix. Furthermore the material showed an increment of both hardness and toughness as temperature increases. The samples presented considerable resistance to oxidation below 1000 deg C. (author)

Microbial adhesion on novel yttria-stabilized tetragonal zirconia (Y-TZP) implant surfaces with nitrogen-doped hydrogenated amorphous carbon (a-C:H:N) coatings.

Science.gov (United States)

Schienle, Stefanie; Al-Ahmad, Ali; Kohal, Ralf Joachim; Bernsmann, Falk; Adolfsson, Erik; Montanaro, Laura; Palmero, Paola; Fürderer, Tobias; Chevalier, Jérôme; Hellwig, Elmar; Karygianni, Lamprini

2016-09-01

Biomaterial surfaces are at high risk for initial microbial colonization, persistence, and concomitant infection. The rationale of this study was to assess the initial adhesion on novel implant surfaces of Enterococcus faecalis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans upon incubation. The tested samples were 3 mol% yttria-stabilized tetragonal zirconia polycrystal (3Y-TZP) samples with nitrogen-doped hydrogenated amorphous carbon (a-C:H:N) coating (A) and 3Y-TZP samples coated with ceria-stabilized zirconia-based (Ce-TZP) composite and a-C:H:N (B). Uncoated 3Y-TZP samples (C) and bovine enamel slabs (BES) served as controls. Once the surface was characterized, the adherent microorganisms were quantified by estimating the colony-forming units (CFUs). Microbial vitality was assessed by live/dead staining, and microbial-biomaterial surface topography was visualized by scanning electron microscopy (SEM). Overall, A and B presented the lowest CFU values for all microorganisms, while C sheltered significantly less E. faecalis, P. aeruginosa, and C. albicans than BES. Compared to the controls, B demonstrated the lowest vitality values for E. coli (54.12 %) and C. albicans (67.99 %). Interestingly, A (29.24 %) exhibited higher eradication rates for S. aureus than B (13.95 %). Within the limitations of this study, a-C:H:N-coated 3Y-TZP surfaces tended to harbor less initially adherent microorganisms and selectively interfered with their vitality. This could enable further investigation of the new multi-functional zirconia surfaces to confirm their favorable antimicrobial properties in vivo.

Ceramic Composites of 3Y-TZP Doped with CuO: Processing, Microstructure and Tribology

NARCIS (Netherlands)

Ran, S.

2006-01-01

The work described in this thesis is about processing, microstructure and tribology of CuO doped 3Y-TZP (3 mol% yttria stabilised tetragonal zirconia polycrystals) composite ceramics. This group of materials has shown attractive properties such as superplastic behaviour at elevated temperature and a

Neutron diffraction investigation for possible anisotropy within monolithic Al2O3/Y-TZP composites fabricated by stacking together cast tapes

International Nuclear Information System (INIS)

Ruiz-Hervias, J.; Bruno, G.; Gurauskis, J.; Sanchez-Herencia, A.J.; Baudin, C.

2006-01-01

The development of residual stresses in two Al 2 O 3 + 5 vol.% yttria-tetragonal zirconia polycrystal (Y-TZP) ceramic composites fabricated by conventional slip casting and by joining green cast tapes was investigated. Neutron diffraction profiles revealed compressive microstresses (-200 MPa) in the Al 2 O 3 matrix and tensile ones (2200 MPa) in the Y-TZP particles, irrespective of the processing route and the direction of measurement, which demonstrates the lack of residual macrostresses due to the joining procedure

Effect of bioglass additions on the sintering of Y-TZP bioceramics

Energy Technology Data Exchange (ETDEWEB)

Habibe, A.F.; Maeda, L.D.; Souza, R.C.; Barboza, M.J.R.; Daguano, J.K.M.F. [USP-EEL, Universidade de Sao Paulo, Escola de Engenharia de Lorena, Polo Urbo-Industrial, Gleba AI6, s/n, P.O. Box 116, CEP 12600-970, Lorena-SP (Brazil); Rogero, S.O. [IPEN/CNEN-SP, Instituto de Pesquisas Energeticas e Nucleares, Av. Prof. Lineu Prestes, 2242, Sao Paulo-SP, CEP 05508-900 (Brazil); Santos, C., E-mail: claudinei@demar.eel.usp.br [USP-EEL, Universidade de Sao Paulo, Escola de Engenharia de Lorena, Polo Urbo-Industrial, Gleba AI6, s/n, P.O. Box 116, CEP 12600-970, Lorena-SP (Brazil)

2009-08-01

The objective of this work was to evaluate the influence of bioglass additions on the sintering and mechanical properties of yttria-stabilized zirconia ceramics, Y-TZP. Samples containing different bioglass additions, varying between 0 and 30 wt.%, were cold uniaxial pressed at 80 MPa and sintered in air at 1200 deg. C or 1300 deg. C for 120 min. Sintered samples were characterized by X-ray Diffractometry and Scanning Electron Microscopy. Hardness and fracture toughness were determined using Vickers indentation method. As a preliminary biological evaluation, in vitro cytotoxicity tests by Neutral Red Uptake method (using mouse connective tissue cells, NCTC clone L929 from ATCC bank) were realized to determine the cytotoxicity level of ZrO{sub 2}-bioglass ceramics. The increasing of bioglass amount leads to the decreasing of relative density due to martensitic (tetragonal-monoclinic) transformation during cooling of the sintered samples. Y-TZP samples sintered at 1300 deg. C containing 5 wt.% of bioglass presented the best results, with high relative density, hardness and fracture toughness of 11.3 GPa and 6.1 MPa m{sup 1/2}, respectively. Furthermore, the un-cytotoxic behavior was observed in all sintering conditions and bioglass amounts used in this study.

Y-TZP ceramic processing from coprecipitated powders : A comparative study with three commercial dental ceramics

NARCIS (Netherlands)

Lazar, Dolores R. R.; Bottino, Marco C.; Ozcan, Mutlu; Valandro, Luiz Felipe; Amaral, Regina; Ussui, Valter; Bressiani, Ana H. A.

2008-01-01

Objectives. (1) To synthesize 3 mol% yttria-stabilized zirconia (3Y-TZP) powders via coprecipitation route, (2) to obtain zirconia ceramic specimens, analyze surface characteristics, and mechanical properties, and (3) to compare the processed material with three reinforced dental ceramics. Methods.

Correlación entre la microestructura y el comportamiento plástico a alta temperatura de compuestos TZP-Ni (40% vol.

Directory of Open Access Journals (Sweden)

Morales-Rodríguez, A.

2005-10-01

Full Text Available Microstructure and high-temperature mechanical behaviour of TZP-Ni composites with 40 vol.% of nickel above the percolation threshold (placed in 34 vol.% in these wet‑processed ceramic-metal composites has been studied. The microstructure has been characterized using scanning electron microscopy. The composite plasticity has been studied by means of uniaxial compressive creep tests under constant load in argon atmosphere carried out in the temperature range between 900 and 1250 ºC and stresses between 9 and 144 MPa. TZP skeleton has been deformed in similar conditions to study nickel effect in global cermet behavior. The metallic phase has been removed from the cermets using chemical etching with HNO3. The plastic behavior of these materials is controlled by the ceramic matrix. The deformation rates are higher than monolithic TZP ones. This fact has been explained taking into account the metallic phase distribution into the matrix in these composites. Metal percolation provides materials with high ductility allowing the cermets to deform at temperatures as low as 900 ºC.

Se ha estudiado la microestructura y el comportamiento mecánico a alta temperatura de compuestos de circona tetragonal (3Y-TZP con un 40% en volumen de níquel (referidos en adelante como TZP-Ni. El contenido en níquel está por encima del punto de percolación, que en estos compuestos cerámico-metal procesados en vía húmeda se sitúa en el 34% vol. de contenido metálico. La caracterización microestructural se ha realizado mediante observaciones de microscopía electrónica de barrido. La plasticidad de los compuestos se ha estudiado mediante ensayos de fluencia en compresión uniaxial a carga constante en atmósfera de argón realizados en el rango de temperaturas entre 900 y 1250 ºC y tensiones entre 9 y 144 MPa. Para estudiar el efecto del níquel en el comportamiento del cermet se ensayaron en condiciones similares esqueletos de TZP, obtenidos mediante la

Effect of airborne particle abrasion protocols on surface topography of Y-TZP ceramic Efeito do protocolo de jateamento com partículas na topografia da superfície de uma cerâmica Y-TZP

Directory of Open Access Journals (Sweden)

J. R. C. Queiroz

2012-06-01

Full Text Available This study aimed to evaluate Y-TZP surface after different airborne particle abrasion protocols. Seventy-six Y-TZP ceramic blocks (5×4×4 mm³ were sintered and polished. Specimens were randomly divided into 19 groups (n=4 according to control group and 3 factors: a protocol duration (2 and 4 s; b particle size (30 µm, alumina coated silica particle; 45 µm, alumina particle; and 145 µm, alumina particle and; c pressure (1.5, 2.5 and 4.5 bar. Airborne particle abrasion was performed following a strict protocol. For qualitative and quantitative results, topography surfaces were analyzed in a digital optical profilometer (Interference Microscopic, using different roughness parameters (Ra, Rq, Rz, X-crossing, Mr1, Mr2 and Sdr and 3D images. Surface roughness also was analyzed following the primer and silane applications on Y-TZP surfaces. One-way ANOVA revealed that treatments (application period, particle size and pressure of particle blasting provided significant difference for all roughness parameters. The Tukey test determined that the significant differences between groups were different among roughness parameters. In qualitative analysis, the bonding agent application reduced roughness, filing the valleys in the surface. The protocols performed in this study verified that application period, particle size and pressure influenced the topographic pattern and amplitude of roughness.O objetivo deste estudo foi avaliar a superfície de uma cerâmica à base de zircônia tetragonal estabilizada por ítria (Y-TZP após diferentes protocolos de jateamento com partículas. Setenta e seis blocos cerâmicos de Y-TZP (5 x 4 x 4 mm³ foram sinterizados e polidos. As amostras foram randomicamente divididas em 19 grupos (n=4 sendo um controle e 18 grupos utilizando 3 fatores: a tempo (2 e 4 s; b tamanho de partícula (30 µm - partículas de alumina revestida por sílica; 45 µm - partículas de alumina; 145 µm - partículas de alumina e; c pressão (1

The effect of grinding on the mechanical behavior of Y-TZP ceramics: A systematic review and meta-analyses.

Science.gov (United States)

Pereira, G K R; Fraga, S; Montagner, A F; Soares, F Z M; Kleverlaan, C J; Valandro, L F

2016-10-01

The aim of this study was to systematically review the literature to assess the effect of grinding on the mechanical properties, structural stability and superficial characteristics of Y-TZP ceramics. The MEDLINE via PubMed and Web of Science (ISI - Web of Knowledge) electronic databases were searched with included peer-reviewed publications in English language and with no publication year limit. From 342 potentially eligible studies, 73 were selected for full-text analysis, 30 were included in the systematic review with 20 considered in the meta-analysis. Two reviewers independently selected the studies, extracted the data, and assessed the risk of bias. Statistical analyses were performed using RevMan 5.1, with random effects model, at a significance level of 0.05. A descriptive analysis considering phase transformation, Y-TZP grain size, Vickers hardness, residual stress and aging of all included studies were executed. Four outcomes were considered in the meta-analyses (factor: grinding x as-sintered) in global and subgroups analyses (grinding tool, grit-size and cooling) for flexural strength and roughness (Ra) data. A significant difference (pgrinding; subgroup analyses revealed that different parameters also lead to different effects on roughness. High heterogeneity was found in some comparisons. Generally grinding promotes decrease in strength and increase in roughness of Y-TZP ceramics. However, the use of a grinding tool that allows greater accuracy of the movement (i.e. contra angle hand-pieces coupled to slowspeed turbines), small grit size (<50μm) and the use of plenty coolant seem to be the main factors to decrease the defect introduction and allow the occurrence of the toughening transformation mechanism, decreasing the risk of deleterious impact on Y-TZP mechanical properties. Copyright © 2016 Elsevier Ltd. All rights reserved.

High temperature microplasticity of fine-grained Y-TZP zirconia studied by mechanical spectroscopy

International Nuclear Information System (INIS)

Donzel, L.; Schaller, R.

1997-01-01

Mechanical spectroscopy has been used to study the early stage of the plastic deformation, i.e. the microplasticity of Y-TZP ceramics. Measurements on samples with different grain sizes have shown that the mechanical loss is proportional to the inverse of the square root of the grain size. The existence of a threshold stress has been observed. (orig.)

Mechanical behavior of a Y-TZP ceramic for monolithic restorations: effect of grinding and low-temperature aging.

Science.gov (United States)

Pereira, G K R; Silvestri, T; Camargo, R; Rippe, M P; Amaral, M; Kleverlaan, C J; Valandro, L F

2016-06-01

This study aimed to investigate the effects of grinding with diamond burs and low-temperature aging on the mechanical behavior (biaxial flexural strength and structural reliability), surface topography, and phase transformation of a Y-TZP ceramic for monolithic dental restorations. Disc-shaped specimens (Zirlux FC, Ivoclar Vivadent) were manufactured according to ISO 6872 (2008) and divided in accordance with two factors: "grinding - 3 levels" and "LTD - 2 levels". Grinding was performed using a contra-angle handpiece under constant water-cooling with different grit-sizes (extra-fine and coarse diamond burs). LTD was simulated in an autoclave at 134°C, under a pressure of 2 bar, over a period of 20h. Surface topography analysis showed an increase in roughness based on surface treatment grit-size (Coarse>Xfine>Ctrl), LTD did not influence roughness values. Both grinding and LTD promoted an increase in the amount of m-phase, although different susceptibilities to degradation were observed. According to existing literature the increase of m-phase content is a direct indicative of Y-TZP degradation. Weibull analysis showed an increase in characteristic strength after grinding (Coarse=Xfine>Ctrl), while for LTD, distinct effects were observed (Ctrlgrinding showed not to be detrimental to the mechanical properties of Zirlux FC Y-TZP ceramic. Copyright © 2016 Elsevier B.V. All rights reserved.

Synergistic acceleration of thyroid hormone degradation by phenobarbital and the PPARα agonist WY14643 in rat hepatocytes

International Nuclear Information System (INIS)

Wieneke, N.; Neuschaefer-Rube, F.; Bode, L.M.; Kuna, M.; Andres, J.; Carnevali, L.C.; Hirsch-Ernst, K.I.; Pueschel, G.P.

2009-01-01

Energy balance is maintained by controlling both energy intake and energy expenditure. Thyroid hormones play a crucial role in regulating energy expenditure. Their levels are adjusted by a tight feedback-controlled regulation of thyroid hormone production/incretion and by their hepatic metabolism. Thyroid hormone degradation has previously been shown to be enhanced by treatment with phenobarbital or other antiepileptic drugs due to a CAR-dependent induction of phase II enzymes of xenobiotic metabolism. We have recently shown, that PPARα agonists synergize with phenobarbital to induce another prototypical CAR target gene, CYP2B1. Therefore, it was tested whether a PPARα agonist could enhance the phenobarbital-dependent acceleration of thyroid hormone elimination. In primary cultures of rat hepatocytes the apparent half-life of T3 was reduced after induction with a combination of phenobarbital and the PPARα agonist WY14643 to a larger extent than after induction with either compound alone. The synergistic reduction of the half-life could be attributed to a synergistic induction of CAR and the CAR target genes that code for enzymes and transporters involved in the hepatic elimination of T3, such as OATP1A1, OATP1A3, UGT1A3 and UGT1A10. The PPARα-dependent CAR induction and the subsequent induction of T3-eliminating enzymes might be of physiological significance for the fasting-induced reduction in energy expenditure by fatty acids as natural PPARα ligands. The synergism of the PPARα agonist WY14643 and phenobarbital in inducing thyroid hormone breakdown might serve as a paradigm for the synergistic disruption of endocrine control by other combinations of xenobiotics.

FEA and microstructure characterization of a one-piece Y-TZP abutment.

Science.gov (United States)

da Silva, Lucas Hian; Ribeiro, Sebastião; Borges, Alexandre Luís Souto; Cesar, Paulo Francisco; Tango, Rubens Nisie

2014-11-01

The most important drawback of dental implant/abutment assemblies is the need for a fixing screw. This study aimed to develop an esthetic one-piece Y-TZP abutment to suppress the use of the screw. Material characterization was performed using a bar-shaped specimen obtained by slip-casting to validate the method prior to prototype abutment fabrication by the same process. The mechanical behavior of the prototype abutment was verified and compared with a conventional abutment by finite element analysis (FEA). The abutment was evaluated by micro-CT analysis and its density was measured. FEA showed stress concentration at the first thread pitch during installation and in the cervical region during oblique loading for both abutments. However, stress concentration was observed at the base of the screw head and stem in the conventional abutment. The relative density for the fabricated abutment was 95.68%. Micro-CT analysis revealed the presence of elongated cracks with sharp edges over the surface and porosity in the central region. In the light of these findings, the behavior of a one-piece abutment is expected to be better than that of the conventional model. New studies should be conducted to clarify the performance and longevity of this one-piece Y-TZP abutment. Copyright © 2014 Academy of Dental Materials. Published by Elsevier Ltd. All rights reserved.

Characterization of Conventional and High-Translucency Y-TZP Dental Ceramics Submitted to Air Abrasion.

Science.gov (United States)

Tostes, Bhenya Ottoni; Guimarães, Renato Bastos; Noronha-Filho, Jaime Dutra; Botelho, Glauco Dos Santos; Guimarães, José Guilherme Antunes; Silva, Eduardo Moreira da

2017-01-01

This study evaluated the effect of air-abrasion on t®m phase transformation, roughness, topography and the elemental composition of three Y-TZP (Yttria-stabilized tetragonal zirconia polycrystal) dental ceramics: two conventional (Lava Frame and IPS ZirCad) and one with high-translucency (Lava Plus). Plates obtained from sintered blocks of each ceramic were divided into four groups: AS (as-sintered); 30 (air-abrasion with 30 mm Si-coated Al2O3 particles); 50 (air-abrasion with 50 mm Al2O3 particles) and 150 (air-abrasion with 150 mm Al2O3 particles). After the treatments, the plates were submitted to X-ray diffractometry; 3-D profilometry and SEM/EDS. The AS surfaces were composed of Zr and t phases. All treatments produced t®m phase transformation in the ceramics. The diameter of air-abrasion particles influenced the roughness (150>50>30>AS) and the topography. SEM analysis showed that the three treatments produced groove-shaped microretentions on the ceramic surfaces, which increased with the diameter of air-abrasion particles. EDS showed a decrease in Zr content along with the emergence of O and Al elements after air-abrasion. Presence of Si was also detected on the plates air-abraded with 30 mm Si-coated Al2O3 particles. It was concluded that irrespective of the type and diameter of the particles, air-abrasion produced t®m phase transformation, increased the roughness and changed the elemental composition of the three Y-TZP dental ceramics. Lava Plus also behaved similarly to the conventional Y-TZP ceramics, indicating that this high translucency ceramic could be more suitable to build monolithic ceramic restorations in the aesthetic restorative dentistry field.

Comparative study of flexural strength test methods on CAD/CAM Y-TZP dental ceramics

Science.gov (United States)

Xu, Yongxiang; Han, Jianmin; Lin, Hong; An, Linan

2015-01-01

Clinically, fractures are the main cause of computer-aided design and computer-aided manufacturing (CAD/CAM) 3 mol%-yttria-stabilized tetragonal zirconia polycrystal (Y-TZP) all-ceramic dental restorations failure because of repetitive occlusal loading. The goal of this work is to study the effect of test methods and specimen’s size on the flexural strength of five ceramic products. Both bi-axial flexure test (BI) and uni-axial flexure tests (UNI), including three-point flexure test (3PF) and four-point flexure test (4PF), are used in this study. For all five products, the flexural strength is as follows: BI > 3PF > 4PF. Furthermore, specimens with smaller size (3PF-s) have higher values than the bigger ones (3PF). The difference between BI and UNI resulted from the edge flaws in ceramic specimens. The relationship between different UNI (including 3PF-s, 3PF and 4PF) can be explained according to Weibull statistical fracture theory. BI is recommended to evaluate the flexural strength of CAD/CAM Y-TZP dental ceramics. PMID:26816646

Comparative study of flexural strength test methods on CAD/CAM Y-TZP dental ceramics.

Science.gov (United States)

Xu, Yongxiang; Han, Jianmin; Lin, Hong; An, Linan

2015-12-01

Clinically, fractures are the main cause of computer-aided design and computer-aided manufacturing (CAD/CAM) 3 mol%-yttria-stabilized tetragonal zirconia polycrystal (Y-TZP) all-ceramic dental restorations failure because of repetitive occlusal loading. The goal of this work is to study the effect of test methods and specimen's size on the flexural strength of five ceramic products. Both bi-axial flexure test (BI) and uni-axial flexure tests (UNI), including three-point flexure test (3PF) and four-point flexure test (4PF), are used in this study. For all five products, the flexural strength is as follows: BI > 3PF > 4PF. Furthermore, specimens with smaller size (3PF-s) have higher values than the bigger ones (3PF). The difference between BI and UNI resulted from the edge flaws in ceramic specimens. The relationship between different UNI (including 3PF-s, 3PF and 4PF) can be explained according to Weibull statistical fracture theory. BI is recommended to evaluate the flexural strength of CAD/CAM Y-TZP dental ceramics.

Effect of Grinding and Multi-Stimuli Aging on the Fatigue Strength of a Y-TZP Ceramic.

Science.gov (United States)

Silvestri, Tais; Pereira, Gabriel Kalil Rocha; Guilardi, Luis Felipe; Rippe, Marilia Pivetta; Valandro, Luiz Felipe

2018-01-01

This study aimed to investigate the effect of grinding and multi-stimuli aging on the fatigue strength, surface topography and the phase transformation of Y-TZP ceramic. Discs were manufactured according to ISO-6872:2008 for biaxial flexure testing (diameter: 15 mm; thickness: 1.2 mm) and randomly assigned considering two factors "grinding" and "aging": C- control (as-sintered); CA- control + aging; G- ground; GA- ground + aging. Grinding was carried out with coarse diamond burs under water-cooling. Aging protocols consisted of: autoclave (134°C, 2 bars pressure, 20 hours), followed by storage for 365 days (samples were kept untouched at room temperature), and by mechanical cycling (106 cycles by 20 Hz under a load of 50% from the biaxial flexure monotonic tests). Flexural fatigue strengths (20,000 cycles; 6 Hz) were determined under sinusoidal cyclic loading using staircase approach. Additionally, surface topography analysis by FE-SEM and phase transformation analysis by X-ray Diffractometry were performed. Dixon and Mood methodology was used to analyze the fatigue strength data. Grinding promotes alterations of topographical pattern, while aging apparently did not alter it. Grinding triggered t-m phase transformation without impacting the fatigue strength of the Y-TZP ceramic; and aging promoted an intense t-m transformation that resulted in a toughening mechanism leading to higher fatigue strength for as-sintered condition, and a tendency of increase for ground condition (C grinding and aging procedures did not affect deleteriously the fatigue strength of the evaluated Y-TZP ceramic, although, it promotes surface topography alterations, except to aging, and t-m phase transformation.

Negative cooperativity in binding of muscarinic receptor agonists and GDP as a measure of agonist efficacy.

Science.gov (United States)

Jakubík, J; Janíčková, H; El-Fakahany, E E; Doležal, V

2011-03-01

Conventional determination of agonist efficacy at G-protein coupled receptors is measured by stimulation of guanosine-5'-γ-thiotriphosphate (GTPγS) binding. We analysed the role of guanosine diphosphate (GDP) in the process of activation of the M₂ muscarinic acetylcholine receptor and provide evidence that negative cooperativity between agonist and GDP binding is an alternative measure of agonist efficacy. Filtration and scintillation proximity assays measured equilibrium binding as well as binding kinetics of [³⁵S]GTPγS and [³H]GDP to a mixture of G-proteins as well as individual classes of G-proteins upon binding of structurally different agonists to the M₂ muscarinic acetylcholine receptor. Agonists displayed biphasic competition curves with the antagonist [³H]-N-methylscopolamine. GTPγS (1 µM) changed the competition curves to monophasic with low affinity and 50 µM GDP produced a similar effect. Depletion of membrane-bound GDP increased the proportion of agonist high-affinity sites. Carbachol accelerated the dissociation of [³H]GDP from membranes. The inverse agonist N-methylscopolamine slowed GDP dissociation and GTPγS binding without changing affinity for GDP. Carbachol affected both GDP association with and dissociation from G(i/o) G-proteins but only its dissociation from G(s/olf) G-proteins. These findings suggest the existence of a low-affinity agonist-receptor conformation complexed with GDP-liganded G-protein. Also the negative cooperativity between GDP and agonist binding at the receptor/G-protein complex determines agonist efficacy. GDP binding reveals differences in action of agonists versus inverse agonists as well as differences in activation of G(i/o) versus G(s/olf) G-proteins that are not identified by conventional GTPγS binding. © 2011 The Authors. British Journal of Pharmacology © 2011 The British Pharmacological Society.

Characterization of a Diamond Ground Y-TZP and Reversion of the Tetragonal to Monoclinic Transformation.

Science.gov (United States)

Candido, L M; Fais, Lmg; Ferreira, E B; Antonio, S G; Pinelli, Lap

To characterize the surface of an yttria-stabilized zirconia (Y-TZP) ceramic after diamond grinding in terms of its crystalline phase, morphology, mean roughness (Ra), and wettability as well as to determine a thermal treatment to reverse the resulting tetragonal to monoclinic (t-m) transformation. Y-TZP specimens were distributed into different groups according to the actions (or no action) of grinding and irrigation. Grinding was accomplished using a diamond stone at a low speed. The samples were characterized by x-ray diffraction (XRD), scanning electron microscopy, goniometry, and profilometry. In situ high-temperature XRD was used to determine an annealing temperature to reverse the t-m transformation. Ra was submitted to the Kruskal-Wallis test, followed by the Dunn test (α=0.05). The volume fraction of the monoclinic phase and contact angle were submitted to one-way analysis of variance, followed by the Tukey test (α=0.05). Monoclinic zirconia was observed on the surface of samples after dry and wet grinding with a diamond stone. The volume fraction of the monoclinic phase was smaller on the dry ground samples (3.6%±0.3%) than on the wet ground samples (5.6%±0.3%). High-temperature XRD showed reversion of the t-m phase transformation, which started at 700°C and completed at 800°C in a conventional oven. Grinding with a diamond stone partially transformed the crystalline phase on the surface of a Y-TZP ceramic from tetragonal to monoclinic zirconia while simultaneously increasing the surface roughness and wettability. The t-m transformation could be reversed by heat treatment at 800°C or 900°C for 60 minutes or 1000°C for 30 minutes.

Mechanical behavior of a Y-TZP ceramic for monolithic restorations: effect of grinding and low-temperature aging

NARCIS (Netherlands)

Pereira, G.K.R.; Silvestri, T.; Camargo, R.; Rippe, M.P.; Amaral, M.; Kleverlaan, C.J.; Valandro, L.F.

2016-01-01

This study aimed to investigate the effects of grinding with diamond burs and low-temperature aging on the mechanical behavior (biaxial flexural strength and structural reliability), surface topography, and phase transformation of a Y-TZP ceramic for monolithic dental restorations. Disc-shaped

Effect of intra-oral aging on t→m phase transformation, microstructure, and mechanical properties of Y-TZP dental ceramics.

Science.gov (United States)

Miragaya, Luciana Meireles; Guimarães, Renato Bastos; Souza, Rodrigo Othávio de Assunção E; Santos Botelho, Glauco Dos; Antunes Guimarães, José Guilherme; da Silva, Eduardo Moreira

2017-08-01

The aim of the present study was to evaluate the influence of intra-oral aging on the tetragonal-to-monoclinic (t→m) phase transformation of two Y-TZP dental ceramics - Lava Frame (Frame) and Lava Plus (Plus) - and determine the impact of this response on their microstructures and mechanical properties: flexural strength, Young's modulus, microhardness and fracture toughness. Standardized ceramic specimens were analyzed by X-ray diffraction (XRD), scanning electron microscopy (SEM) and atomic force microscopy (AFM). After the baseline analysis, the specimens were attached to personalized intra-oral resin appliances and exposed to the oral cavity of 20 subjects for 60 days and then analyzed again. Specimens produced for mechanical properties evaluation were also analyzed before and after the 60-day intra-oral aging. The data were analyzed using two-way ANOVA and Tukey HSD's post hoc test (α=0.05). Weibull analysis was used to evaluate the strength reliability. Both Y-TZP ceramics suffered t→m phase transformation after 60-day intra-oral aging (Plus=4.7%/Frame=7.7%). SEM and AFM analyses showed dislodgement of ZrO 2 grains and a significant increase in roughness after intra-oral aging for both ceramics. Both Y-TZP ceramics suffered a decrease on flexural strength, Young's modulus and fracture toughness after intra-oral aging (pdental ceramics. Copyright © 2017 Elsevier Ltd. All rights reserved.

Microstructural changes in ground 3Y-TZP and their effect on mechanical properties

Energy Technology Data Exchange (ETDEWEB)

Munoz-Tabares, J.A., E-mail: j.a.munoz.tabares@gmail.com [Departament de Ciencia dels Materials i Enginyeria Metallurgica, Universitat Politecnica de Catalunya, Avda. Diagonal 647 (ETSEIB), 08028 Barcelona (Spain); Jimenez-Pique, E. [Departament de Ciencia dels Materials i Enginyeria Metallurgica, Universitat Politecnica de Catalunya, Avda. Diagonal 647 (ETSEIB), 08028 Barcelona (Spain); Centre de Recerca en Nanoenginyeria (CRnE), C. Pascual i Vila 15, 08028 Barcelona (Spain); Reyes-Gasga, J. [Instituto de Fisica, Universidad Nacional Autonoma de Mexico, Circuito de la Investigacion Cientifica s/n, Cd Universitaria, 04510 Mexico DF (Mexico); Anglada, M. [Departament de Ciencia dels Materials i Enginyeria Metallurgica, Universitat Politecnica de Catalunya, Avda. Diagonal 647 (ETSEIB), 08028 Barcelona (Spain); Centre de Recerca en Nanoenginyeria (CRnE), C. Pascual i Vila 15, 08028 Barcelona (Spain)

2011-10-15

In the present work we studied the changes in the microstructure and mechanical properties that are produced by grinding of tetragonal polycrystalline zirconia doped with 3 mol.% yttria (3Y-TZP). It is shown that the X-ray diffraction spectrum of ground 3Y-TZP presents asymmetric broadening of the (1 1 1) tetragonal peak, reversal of the intensity of the (0 0 2) and (2 0 0) tetragonal peaks, and tetragonal to monoclinic (t-m) phase transformation. The in-depth monoclinic phase distribution obtained by micro-Raman spectroscopy has been related with the compression residual stresses profile generated during grinding. These compressive residual stresses are also responsible for the observed increase in mechanical properties (strength and apparent fracture toughness). The subsurface microstructure of ground specimens has been analyzed by transmission electron microscopy and three different regions were found from the interior to the surface: (1) a t-m phase transformation zone in the deeper region, (2) a plastically deformed zone, with dynamically recovered dislocation cells, and (3) a surface recrystallized zone with grains of {approx}20 nm in diameter, resulting from in situ recrystallization. In addition, microcracking is concentrated on the sides of the grinding grooves, corresponding to the zone of maximum tensile stress during contact with an abrasive particle.

Tetragonal zirconia ceramics in Zr O2-Ce O2 system (Ce-TZP): preparation, characterization and mechanical properties

International Nuclear Information System (INIS)

Andrade Nono, M.C. de.

1992-01-01

This paper describes and discusses the results achieved in a study about Ce-TZP ceramics prepared from conventional powder mixtures of Zr O 2 and Ce O 2 (with composition in the range of 8 to 16 mol% Ce O 2 ). Physical and chemical characteristics were related with the powder compaction behavior and with the sintering state. The sintered ceramics showed a level of high porosity (≅ 4%), mainly due to the fairly adequate powder characteristics and compaction. The crystalline phases were analysed from X-rays diffraction data and showed that these ceramics can present tetragonal-to-monoclinic stress induced transformation. The bending strength, fracture toughness and Vickers hardness results were influenced by Ce O 2 content microstructure and sintering temperature. These Ce-TZP ceramics showed mechanical strength results comparable to those published in the international literature. (author)

Grinding With Diamond Burs and Hydrothermal Aging of a Y-TZP Material: Effect on the Material Surface Characteristics and Bacterial Adhesion.

Science.gov (United States)

Dutra, Dam; Pereira, Gkr; Kantorski, K Z; Exterkate, Ram; Kleverlaan, C J; Valandro, L F; Zanatta, F B

The aim of this study was to evaluate the effect of grinding with diamond burs and low-temperature aging on the material surface characteristics and bacteria adhesion on a yttrium-stabilized tetragonal zirconia polycrystalline (Y-TZP) surface. Y-TZP specimens were made from presintered blocks, sintered as recommended by the manufacturer, and assigned into six groups according to two factors-grinding (three levels: as sintered, grinding with extra-fine diamond bur [25-μm grit], and grinding with coarse diamond bur [181-μm grit]) and hydrothermal aging-to promote low-temperature degradation (two levels: presence/absence). Phase transformation (X-ray diffractometer), surface roughness, micromorphological patterns (atomic force microscopy), and contact angle (goniometer) were analyzed. Bacterial adhesion (colony-forming units [CFU]/biofilm) was quantified using an in vitro polymicrobial biofilm model. Both the surface treatment and hydrothermal aging promoted an increase in m-phase content. Roughness values increased as a function of increasing bur grit sizes. Grinding with a coarse diamond bur resulted in significantly lower values of contact angle (p0.05). Grinding with diamond burs and hydrothermal aging modified the Y-TZP surface properties; however, these properties had no effect on the amount of bacteria adhesion on the material surface.

Synthesis and characterisation of dual-phase Y-TZP and RuO2 nanopowders: dense electrode precursors.

NARCIS (Netherlands)

van Zyl, W.E.; Winnubst, Aloysius J.A.; Raming, T.P.; Schmuhl, R.; Verweij, H.

2002-01-01

The synthesis and characterisation of nanopowders in the dual-phase system tetragonal-Y2O3-doped ZrO2 (Y-TZP) and RuO2 are described. Five powders were prepared from a co-precipitation (CP) method with stoichiometric variation in the RuO2 content (5–46 mol%) and two powders were prepared from

The effect of grinding on the mechanical behavior of Y-TZP ceramics: A systematic review and meta-analyses

NARCIS (Netherlands)

Pereira, G.K.R.; Fraga, S.; Montagner, A.F.; Soares, F.Z.M.; Kleverlaan, C.J.; Valandro, L.F.

2016-01-01

The aim of this study was to systematically review the literature to assess the effect of grinding on the mechanical properties, structural stability and superficial characteristics of Y-TZP ceramics. The MEDLINE via PubMed and Web of Science (ISI – Web of Knowledge) electronic databases were

CeO2-stabilized tetragonal ZrO2 polycrystals (Ce-TZP ceramics)

International Nuclear Information System (INIS)

Andrade Nono, M.C. de.

1990-12-01

This work presents the development and the characterization of CeO 2 -stabilized tetragonal ZrO 2 polycrystals (Ce-TZP ceramics), since it is considered candidate material for applications as structural high performance ceramics. Sintered ceramics were fabricated from mixtures of powders containing different CeO 2 content prepared by conventional and nonconventional techniques. These powders and their resultant sintered ceramics were specified by chemical and physical characterization, compactation state and mechanical properties. The chemical characteristics were determined by chemical analysis and the physical characteristics were evaluated by phase content, particle and agglomerate size and aspect, and powder porosity. (author)

Drug and cell type-specific regulation of genes with different classes of estrogen receptor beta-selective agonists.

Directory of Open Access Journals (Sweden)

Sreenivasan Paruthiyil

2009-07-01

Full Text Available Estrogens produce biological effects by interacting with two estrogen receptors, ERalpha and ERbeta. Drugs that selectively target ERalpha or ERbeta might be safer for conditions that have been traditionally treated with non-selective estrogens. Several synthetic and natural ERbeta-selective compounds have been identified. One class of ERbeta-selective agonists is represented by ERB-041 (WAY-202041 which binds to ERbeta much greater than ERalpha. A second class of ERbeta-selective agonists derived from plants include MF101, nyasol and liquiritigenin that bind similarly to both ERs, but only activate transcription with ERbeta. Diarylpropionitrile represents a third class of ERbeta-selective compounds because its selectivity is due to a combination of greater binding to ERbeta and transcriptional activity. However, it is unclear if these three classes of ERbeta-selective compounds produce similar biological activities. The goals of these studies were to determine the relative ERbeta selectivity and pattern of gene expression of these three classes of ERbeta-selective compounds compared to estradiol (E(2, which is a non-selective ER agonist. U2OS cells stably transfected with ERalpha or ERbeta were treated with E(2 or the ERbeta-selective compounds for 6 h. Microarray data demonstrated that ERB-041, MF101 and liquiritigenin were the most ERbeta-selective agonists compared to estradiol, followed by nyasol and then diarylpropionitrile. FRET analysis showed that all compounds induced a similar conformation of ERbeta, which is consistent with the finding that most genes regulated by the ERbeta-selective compounds were similar to each other and E(2. However, there were some classes of genes differentially regulated by the ERbeta agonists and E(2. Two ERbeta-selective compounds, MF101 and liquiritigenin had cell type-specific effects as they regulated different genes in HeLa, Caco-2 and Ishikawa cell lines expressing ERbeta. Our gene profiling studies

Results of a Phase 1 Dose Escalation Study of Intravesical TMX-101 in Patients with Nonmuscle Invasive Bladder Cancer

NARCIS (Netherlands)

Falke, Johannes; Lammers, Rianne J. M.; Arentsen, Harm C.; Ravic, Miroslav; Pozzi, Raffaella; Cornel, Erik B.; Vergunst, Henk; de Reijke, Theo M.; Witjes, J. Alfred

2013-01-01

Purpose: Imiquimod, a toll like receptor 7 (TLR-7) agonist, is effective as a topical treatment for skin malignancies. TMX-101 is a liquid formulation of imiquimod. In this study we establish a safety profile of TMX-101 in patients with nonmuscle invasive bladder cancer. Materials and Methods: We

Results of a phase 1 dose escalation study of intravesical TMX-101 in patients with nonmuscle invasive bladder cancer

NARCIS (Netherlands)

Falke, J.; Lammers, R.; Arentsen, H.C.; Ravic, M.; Pozzi, R.; Cornel, E.B.; Vergunst, H.; Reijke, T.M. de; Witjes, J.A.

2013-01-01

PURPOSE: Imiquimod, a toll like receptor 7 (TLR-7) agonist, is effective as a topical treatment for skin malignancies. TMX-101 is a liquid formulation of imiquimod. In this study we establish a safety profile of TMX-101 in patients with nonmuscle invasive bladder cancer. MATERIALS AND METHODS: We

Random walk analysis of grain motion during superplastic deformation of TZP

International Nuclear Information System (INIS)

Okamoto, T; Yasuda, K; Shiota, T

2009-01-01

This study focuses on grain motion in TZP (Tetragonal Zirconia Polycrystal) ceramics during superplastic deformation. The specimen was 16 times elongated repeatedly at 1400 0 C in air. The increment of true plastic strain was set to be 2%, and the specimen was deformed up to 30.3% true plastic strain finally. After each deformation, displacement vectors of specified 748 grains were measured from their position vectors determined by FE-SEM micrographs. As a result, the grains move to the tensile loading direction in zigzag way. And also, the zigzag motion changes with plastic strain: The grains move randomly (random walk motion) by the first 15% true plastic strain, and then grain motion becomes spatially uniform gradually. It is related to changes of constraint of surrounding matrix.

Microestructura de Al2O3/TZP codopado con Fe2O3 y TiO2 fabricado por reacción (RBAO

Directory of Open Access Journals (Sweden)

Jiménez, M.

2003-02-01

Full Text Available Reaction-bonded 80 vol% Al2O3/TZP (2 mol% Y2O3-stabilized tetragonal zirconia polycrystals composites co-doped with 1 vol% Fe2O3 and 1 vol% TiO2 have been produced, and then presureless sintered (1450 ºC, 60 min or sinter-forged (20 MPa, 1200 ºC, 60 min. The resulting microstructures have been characterized using scanning electron microscopy. Both types of materials are dense, with a fine and homogeneous dual microstructure consisting of Al2O3 and TZP grains without intermediate grain boundary phases. Sinter-forged composites exhibit a very narrow pore size distribution, essentially smaller than the grain size of the alumina and zirconia phases. Co-doping promotes the sintering of alumina at lower temperatures, while still retains a fine grain size due to the presence of the dispersed zirconia phase. First results on presureless sintered RBAO materials show a fracture strength higher than in conventionally sintered and sinter-forged composites.Se han fabricado compuestos de 80% vol. Al2O3/TZP (ZrO2 estabilizada con 2% mol Y2O3 codopados con 1% vol. Fe2O3 y 1% vol. TiO2 mediante la tecnología RBAO (“Reaction Bonding of Aluminum Oxide”, que se han sinterizado libremente (1450 ºC, 60 min y bajo carga uniaxial (20 MPa, 1200 ºC, 60 min. Se ha caracterizado la microestructura mediante microscopía electrónica de barrido. Ambos materiales son densos con una microestructura homogénea formada por granos de alúmina y de circona, sin fases en juntas de grano. En el caso de la sinterización bajo carga, la distribución del tamaño de los poros es muy estrecha, y esencialmente menor que las correspondientes a los granos de Al2O3 y TZP. El codopado promueve la sinterización de la alúmina, mientras que los granos dispersos de circona inhiben su crecimiento de grano. Los ensayos preliminares de flexión en cuatro puntos realizados sobre los materiales sinterizados sin carga indican una resistencia a la fractura superior a la que presentan los

Effect of TiN Addition on 3Y-TZP Ceramics with Emphasis on Making EDM-Able Bodies

Science.gov (United States)

Khosravifar, Mahnoosh; Mirkazemi, Seyyed Mohammad; Taheri, Mahdiar; Golestanifard, Farhad

2018-04-01

In this study, to produce electrically conductive ceramics, rapid hot press (RHP) sintering of 3 mol.% yttria-stabilized tetragonal zirconia polycrystal (3Y-TZP) and 3Y-TZP/TiN composites with TiN amounts of 25, 35, and 45 vol.% was performed at 1300, 1350, and 1400 °C. Interestingly, the toughness and hardness were improved in the presence of TiN up to 35 vol.% and maximum fracture toughness and hardness of 5.40 ± 0.05 MPa m1/2 and 14.50 ± 0.06 GPa, respectively, were obtained. However, the bending strength was decreased which could be attributed to the rather weak interfaces of nitride and oxide phases. Regarding the zirconia matrix, the effect of grain size on fracture toughness of the samples has been studied using x-ray diffraction and field emission scanning electron microscope (FESEM) analysis. It was also found that electrical resistivity decreased to the value of 6.88 × 10-6 Ω m at 45 vol.% of TiN. It seems the TiN grains form a network to impose conductivity on the ZrO2 body; however, below 35 vol.% TiN, due to lack of percolation effect, this conductivity could not be maintained according to FESEM studies. Finally, electrically conductive samples were successfully machined by electrical discharge machining (EDM).

Effect of Initial ZrOCl₂ Concentration on the Homogeneous Precipitation of Nanoscale 3Y-TZP Powder.

Science.gov (United States)

Jeong, Hyeongdo; Lee, Jong Kook

2018-09-01

Nanoscale yttria-stabilized zirconia (Y-TZP) powder was synthesized by homogeneous precipitation via urea hydrolysis, and the influence of a dispersing agent and the initial ZrOCl2 concentration on the powder characteristics was investigated. A precipitated gel was obtained from the reaction of the precursor solution with zirconium oxychloride, yttrium chloride, and urea with heating at 110 °C for 5 h. The initial ZrOCl2 concentration was controlled from 0.25 to 1 M. To observe the effect of adding a dispersing agent on the agglomeration of primary particles, we used two starting compositions, one with and the other without a dispersing agent, ammonium polymethacrylate. Two crystalline powders were obtained after drying, calcination, and milling the gel, and we investigated the powder characteristics, such as particle agglomeration, the specific surface area, the microstructure, and phase composition. Two scales of agglomerates were observed in the particle size distribution, namely, 190 to 362 nm at the primary scale and 1.6-4.0 μm at the secondary scale. The amount of secondary agglomerate increased from 6 to 20 vol% with the increasing initial ZrOCl2 concentration. The size of both types of agglomerate and the amount of secondary agglomerates decreased due to the addition of the dispersing agent, especially the primary agglomerate size. The sintered density and microstructure of Y-TZP were affected by the agglomeration behavior, especially the amount of secondary agglomerates.

PARTIAL AGONISTS, FULL AGONISTS, ANTAGONISTS - DILEMMAS OF DEFINITION

NARCIS (Netherlands)

HOYER, D; BODDEKE, HWGM

The absence of selective antagonists makes receptor characterization difficult, and largely dependent on the use of agonists. However, there has been considerable debate as to whether certain drugs acting at G protein-coupled receptors are better described as agonists, partial agonists or

ACCELERATORS: School report

Energy Technology Data Exchange (ETDEWEB)

Anon.

1987-12-15

The expanded 1987 US Particle Accelerator School, held at Fermilab from 20 July to 14 August, included two two-week sessions. In the first, 101 students covered three university-style courses, listed as upper-division University of Chicago physics, covering the fundamentals of particle beams, magnetic optics and acceleration; relativistic electronics; and high energy storage rings. The 180 participants in the second session profited from 24 short courses presented by experts and covering a wide variety of topics in the physics and technology of particle accelerators.

Pharmacological profile of DA-6886, a novel 5-HT4 receptor agonist to accelerate colonic motor activity in mice.

Science.gov (United States)

Lee, Min Jung; Cho, Kang Hun; Park, Hyun Min; Sung, Hyun Jung; Choi, Sunghak; Im, Weonbin

2014-07-15

DA-6886, the gastrointestinal prokinetic benzamide derivative is a novel 5-HT4 receptor agonist being developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C). The purpose of this study was to characterize in vitro and in vivo pharmacological profile of DA-6886. We used various receptor binding assay, cAMP accumulation assay, organ bath experiment and colonic transit assay in normal and chemically constipated mice. DA-6886 exhibited high affinity and selectivity to human 5-HT4 receptor splice variants, with mean pKi of 7.1, 7.5, 7.9 for the human 5-HT4a, 5-HT4b and 5-HT4d, respectively. By contrast, DA-6886 did not show significant affinity for several receptors including dopamine D2 receptor, other 5-HT receptors except for 5-HT2B receptor (pKi value of 6.2). The affinity for 5-HT4 receptor was translated into functional agonist activity in Cos-7 cells expressing 5-HT4 receptor splice variants. Furthermore, DA-6886 induced relaxation of the rat oesophagus preparation (pEC50 value of 7.4) in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels revealed that it inhibited hERG channel current with an pIC50 value of 4.3, indicating that the compound was 1000-fold more selective for the 5-HT4 receptor over hERG channels. In the normal ICR mice, oral administration of DA-6886 (0.4 and 2mg/kg) resulted in marked stimulation of colonic transit. Furthermore, in the loperamide-induced constipation mouse model, 2mg/kg of DA-6886 significantly improved the delay of colonic transit, similar to 10mg/kg of tegaserod. Taken together, DA-6886 is a highly potent and selective 5-HT4 receptor agonist to accelerate colonic transit in mice, which might be therapeutic agent having a favorable safety profile in the treatment of gastrointestinal motor disorders such as IBS-C and chronic constipation. Copyright © 2014 Elsevier B.V. All rights reserved.

Repair bond strength of composite resin to sandblasted and laser irradiated Y-TZP ceramic surfaces.

Science.gov (United States)

Kirmali, Omer; Barutcigil, Çağatay; Ozarslan, Mehmet Mustafa; Barutcigil, Kubilay; Harorlı, Osman Tolga

2015-01-01

This study investigated the effects of different surface treatments on the repair bond strength of yttrium-stabilized tetragonal zirconia polycrystalline ceramic (Y-TZP) zirconia to a composite resin. Sixty Y-TZP zirconia specimens were prepared and randomly divided into six groups (n = 10) as follows: Group 1, surface grinding with Cimara grinding bur (control); Group 2, sandblasted with 30 µm silica-coated alumina particles; Group 3, Nd:YAG laser irradiation; Group 4, Er,Cr:YSGG laser irradiation; Group 5, sandblasted + Nd:YAG laser irradiation; and Group 6, sandblasted + Er,Cr:YSGG laser irradiation. After surface treatments, the Cimara(®) System was selected for the repair method and applied to all specimens. A composite resin was built-up on each zirconia surface using a cylindrical mold (5 × 3 mm) and incrementally filled. The repair bond strength was measured with a universal test machine. Data were analyzed using a one-way ANOVA and a Tukey HSD test (p = 0.05). Surface topography after treatments were evaluated by a scanning electron microscope (SEM). Shear bond strength mean values ranged from 15.896 to 18.875 MPa. There was a statistically significant difference between group 3 and the control group (p < 0.05). Also, a significant increase in bond strength values was noted in group 6 (p < 0.05). All surface treatment methods enhanced the repair bond strength of the composite to zirconia; however, there were no significant differences between treatment methods. The results revealed that Nd:YAG laser irradiation along with the combination of sandblasting and Er,Cr:YSGG laser irradiation provided a significant increase in bond strength between the zirconia and composite resin. © Wiley Periodicals, Inc.

Y-TZP ceramic processing from coprecipitated powders: a comparative study with three commercial dental ceramics.

Science.gov (United States)

Lazar, Dolores R R; Bottino, Marco C; Ozcan, Mutlu; Valandro, Luiz Felipe; Amaral, Regina; Ussui, Valter; Bressiani, Ana H A

2008-12-01

(1) To synthesize 3mol% yttria-stabilized zirconia (3Y-TZP) powders via coprecipitation route, (2) to obtain zirconia ceramic specimens, analyze surface characteristics, and mechanical properties, and (3) to compare the processed material with three reinforced dental ceramics. A coprecipitation route was used to synthesize a 3mol% yttria-stabilized zirconia ceramic processed by uniaxial compaction and pressureless sintering. Commercially available alumina or alumina/zirconia ceramics, namely Procera AllCeram (PA), In-Ceram Zirconia Block (CAZ) and In-Ceram Zirconia (IZ) were chosen for comparison. All specimens (6mmx5mmx5mm) were polished and ultrasonically cleaned. Qualitative phase analysis was performed by XRD and apparent densities were measured on the basis of Archimedes principle. Ceramics were also characterized using SEM, TEM and EDS. The hardness measurements were made employing Vickers hardness test. Fracture toughness (K(IC)) was calculated. Data were analyzed using one-way analysis of variance (ANOVA) and Tukey's test (alpha=0.05). ANOVA revealed that the Vickers hardness (pceramic materials composition. It was confirmed that the PA ceramic was constituted of a rhombohedral alumina matrix, so-called alpha-alumina. Both CAZ and IZ ceramics presented tetragonal zirconia and alpha-alumina mixture of phases. The SEM/EDS analysis confirmed the presence of aluminum in PA ceramic. In the IZ and CAZ ceramics aluminum, zirconium and cerium in grains involved by a second phase containing aluminum, silicon and lanthanum were identified. PA showed significantly higher mean Vickers hardness values (H(V)) (18.4+/-0.5GPa) compared to vitreous CAZ (10.3+/-0.2GPa) and IZ (10.6+/-0.4GPa) ceramics. Experimental Y-TZP showed significantly lower results than that of the other monophased ceramic (PA) (pceramics (pceramic processing conditions led to ceramics with mechanical properties comparable to commercially available reinforced ceramic materials.

Effects of currently used pesticides in the AhR-CALUX assay: comparison between the human TV101L and the rat H4IIE cell line

DEFF Research Database (Denmark)

Long, M.; Laier, Peter; Vinggaard, Anne

2003-01-01

TV101L hepatoma cell lines. In comparison the results indicated that the rat H4IIE cell line is more sensitive than the human TV101L for detection of TCDD inducing AhR-CALUX activity. The pesticides iprodione, chlorpyrifos and prochloraz showed dose-dependent AhR agonistic effects in both cell lines...

A Unified Model of the GABA(A) Receptor Comprising Agonist and Benzodiazepine Binding Sites

DEFF Research Database (Denmark)

Kongsbak, Kristine Grønning; Bergmann, Rikke; Sørensen, Pernille Louise

2013-01-01

We present a full-length a1b2c2 GABA receptor model optimized for agonists and benzodiazepine (BZD) allosteric modulators. We propose binding hypotheses for the agonists GABA, muscimol and THIP and for the allosteric modulator diazepam (DZP). The receptor model is primarily based on the glutamate......-gated chloride channel (GluCl) from C. elegans and includes additional structural information from the prokaryotic ligand-gated ion channel ELIC in a few regions. Available mutational data of the binding sites are well explained by the model and the proposed ligand binding poses. We suggest a GABA binding mode...... of the agonists in the orthosteric site. The carbonyl group of DZP is predicted to interact with two threonines a1T206 and c2T142, similar to the acidic moiety of GABA. The chlorine atom of DZP is placed near the important a1H101 and the N-methyl group near a1Y159, a1T206, and a1Y209. We present a binding mode...

Glutamate receptor agonists

DEFF Research Database (Denmark)

Vogensen, Stine Byskov; Greenwood, Jeremy R; Bunch, Lennart

2011-01-01

The neurotransmitter (S)-glutamate [(S)-Glu] is responsible for most of the excitatory neurotransmission in the central nervous system. The effect of (S)-Glu is mediated by both ionotropic and metabotropic receptors. Glutamate receptor agonists are generally a-amino acids with one or more...... stereogenic centers due to strict requirements in the agonist binding pocket of the activated state of the receptor. By contrast, there are many examples of achiral competitive antagonists. The present review addresses how stereochemistry affects the activity of glutamate receptor ligands. The review focuses...... mainly on agonists and discusses stereochemical and conformational considerations as well as biostructural knowledge of the agonist binding pockets, which is useful in the design of glutamate receptor agonists. Examples are chosen to demonstrate how stereochemistry not only determines how the agonist...

Superplastic characteristics and microstructure of neutron irradiated 3Y-TZP

International Nuclear Information System (INIS)

Shibata, Taiju; Motohashi, Yoshinobu; Ishihara, Masahiro; Baba, Shinichi; Sawa, Kazuhiro

2006-01-01

Fast neutrons (energy > 1.6 x 10 -13 J) were irradiated to 3Y-TZP specimens, typical superplastic ceramics, at the fluence of 2.5 x 10 24 and 4.3 x 10 24 m -2 at JMTR of JAEA. The Vickers hardness with indentation load of 4.9 and 9.8 N at room temperature was seemed to be slightly increased by the irradiation. Through the superplastic tensile tests in a temperature range from 1623 to 1773 K with initial strain rates of 5.0 x 10 -4 and 1.0 x 10 -3 s -1 , it was found that the superplastic flow stress is decreased with increasing the neutron fluence. The microstructural features of the fractured specimens were observed by a SEM. It implies that the grain boundary microstructure of the irradiated specimens would be changed by annealing in the superplastic tests are elevated temperatures. It is quite probable that the irradiation-induced vacancy clusters might play an important role to weaken the grain boundary cohesion which may be an important factor to determine the superplastic properties, and hence they would decrease the superplastic flow stress. (author)

Can low-fusing glass application affect the marginal misfit and bond strength of Y-TZP crowns?

Science.gov (United States)

Antunes, Monize Carelli Felipe; Miranda, Jean Soares; Carvalho, Ronaldo Luís Almeida de; Carvalho, Rodrigo Furtado de; Kimpara, Estevão Tomomitsu; Assunção E Souza, Rodrigo Othávio de; Leite, Fabíola Pessôa Pereira

2018-01-01

To evaluate the effect of different surface treatments on the marginal misfit and retentive strength between Y-TZP crowns and an epoxy resin. Forty (40) epoxy resin (G10) abutments (height: 5mm, conicity: 60, finish line: large chamfer) with equal dimensions were milled and included in polyurethane to simulate the periodontal ligament. Next, 40 Y-TZP crowns (thickness: 1mm) were milled (Cerec in Lab) and randomly divided into four groups (n=10) according to the surface treatment: GS(glaze spray), GP(glaze powder/liquid), P(zirconia primer) and RS(tribochemical silica coating). The conditioned surfaces were cemented with dual self-adhesive cement, light cured and submitted to thermomechanical cycling (2x106, 100N, 4Hz, 5°/55°C). Marginal misfit was analyzed by a stereomicroscope and SEM. Retentive strength test was performed (1mm/min) until crown debonding. Glaze layer thickness was also performed to GS and GP groups. Marginal misfit data were analyzed by Kruskal Wallis and Dunn tests; one-way ANOVA and Tukey (5%) analyzed the tensile strength data. The marginal misfit of the GS (48.6±19.9μm) and GP (65.4±42.5μm) were statistically lower than the RS (96±62.9μm) and P (156±113.3μm) (p=0.001). The retentive strength of the GP (470.5±104.1N) and GS (416.8±170.2N) were similar to the P (342.1±109.7N), but statistically higher than those of the RS (208.9±110N). The GS and GP glaze layer was 11.64μm and 9.73μm respectively. Thus, glaze application promoted lower marginal discrepancy and higher retentive strength values than conventional techniques.

Effect of Grinding and Resintering on the Fatigue Limit and Surface Characterization of a Y-TZP Ceramic.

Science.gov (United States)

Polli, Gabriela Scatimburgo; Hatanaka, Gabriel Rodrigues; Abi-Rached, Filipe de Oliveira; Pinelli, Lígia Antunes Pereira; Góes, Márcio de Sousa; Cesar, Paulo Francisco; Reis, José Maurício Dos Santos Nunes

2016-01-01

This study evaluated the effect of grinding protocols and resintering on flexural fatigue limit and surface characterization of LavaTM Y-TZP. Bar-shaped specimens (20×4.0×1.2 mm, n=40; 20×4.0×1.5 mm, n=80) were obtained. Half of the thinner specimens (1.2 mm) constituted the as-sintered group (AS), while the thicker ones (1.5 mm) were ground with diamond burs under irrigation (WG) or not (G). The other half of thinner and half of ground specimens were resintered (1000 ºC, 30 min), forming the groups ASR, WGR and GR. Fatigue limit (500,000 cycles, 10 Hz) was evaluated by staircase method in a 4-point flexural fixture. Data were analyzed by 2-way ANOVA and Tukey's test (α=0.05). Surface topography (n=3) and fracture area (n=3) were evaluated by SEM. X-ray diffraction data (n=1) was analyzed by Rietveld refinement. ANOVA revealed significant differences (pgrinding protocol, resintering and their interaction. Grinding increased the fatigue limit of non-resintered groups. There was no significant difference among the resintered groups. Resintering significantly increased the fatigue limit of the AS group only. Both protocols created evident grooves on zirconia surface. The failures initiated at the tensile side of all specimens. The percentages (wt%) of monoclinic phase were AS (8.6), ASR (1.2), G (1.8), GR (0.0), WG (8.2), WGR (0.0) before, and AS (7.4), ASR (6.5), G (3.2), GR (0.2), WG (4.6), WGR (1.1) after cyclic loading. Grinding increased the fatigue limit of non-resintered Y-TZP and formed evident grooves on its surface. Resintering provided significant increase in the fatigue limit of as-sintered specimens. In general, grinding and resintering decreased or zeroed the monoclinic phase.

41 CFR 101-27.101 - General.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true General. 101-27.101 Section 101-27.101 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 27-INVENTORY MANAGEMENT 27.1-Stock...

Lost mold-rapid infiltration forming: Strength control in mesoscale 3Y-TZP ceramics

Science.gov (United States)

Antolino, Nicholas E.

The strength of nanoparticulate enabled microdevices and components is directly related to the interfacial control between particles and the flaws introduced as these particles come together to form the device or component. One new application for micro-scale or meso-scale (10's microm to 100's microm) devices is surgical instruments designed to enter the body, perform a host of surgeries within the body cavity, and be extracted with no external incisions to the patient. This new concept in surgery, called natural orifice transluminal endoscopic surgery (NOTES), requires smaller and more functional surgical tools. Conventional processing routes do not exist for making these instruments with the desired size, topology, precision, and strength. A process, called lost mold-rapid infiltration forming (LM-RIF), was developed to satisfy this need. A tetragonally stabilized zirconia polycrystalline material (3Y-TZP) is a candidate material for this process and application because of its high strength, chemical stability, high elastic modulus, and reasonably high toughness for a ceramic. Modern technical ceramics, like Y-TZP, are predicated on dense, fine grained microstructures and functional mesoscale devices must also adhere to this standard. Colloid and interfacial chemistry was used to disperse and concentrate the Y-TZP nanoparticles through a very steep, yet localized, potential energy barrier against the van der Waals attractive force. The interparticle interaction energies were modeled and compared to rheological data on the suspension. At high concentrations, the suspension was pseudoplastic, which is evidence that a structure was formed within the suspension that could be disrupted by a shearing force. The LM-RIF process exploits this rheological behavior to fill mold cavities created by photolithography. The premise of the LM-RIF process is to process the particulate material into a dense ceramic body while the unsintered mesoscale parts are supported en masse

A comparison of the tribological behaviour of Y-TZP in tea and coffee under micro-abrasion conditions

International Nuclear Information System (INIS)

Sharifi, S; Stack, M M

2013-01-01

The micro-abrasion of Y-TZP, a candidate dental restorative material, was investigated in a range of caffeine-containing solutions which included tea and coffee. Additions of sugar and milk were used to test the effects of viscosity and pH on the wear rate. The results indicated a significant increase in wear rate in the various solutions, with some correlation between wear rate and increases in viscosity and this was linked to enhance particle entrainment in the more viscous solutions. The generally lower wear rate in tea compared to coffee was associated with a longer ageing period in this solution before uniform wear was observed. Micro-abrasion maps were used to characterize the differences in performance for the material in the environments studied. (paper)

A comparison of the tribological behaviour of Y-TZP in tea and coffee under micro-abrasion conditions

Science.gov (United States)

Sharifi, S.; Stack, M. M.

2013-10-01

The micro-abrasion of Y-TZP, a candidate dental restorative material, was investigated in a range of caffeine-containing solutions which included tea and coffee. Additions of sugar and milk were used to test the effects of viscosity and pH on the wear rate. The results indicated a significant increase in wear rate in the various solutions, with some correlation between wear rate and increases in viscosity and this was linked to enhance particle entrainment in the more viscous solutions. The generally lower wear rate in tea compared to coffee was associated with a longer ageing period in this solution before uniform wear was observed. Micro-abrasion maps were used to characterize the differences in performance for the material in the environments studied.

Daño por contacto de cerámicas Y-TZP sometidas a degradación hidrotérmica

OpenAIRE

Trinel, Jérémy

2009-01-01

Este trabajo evalúa el comportamiento del daño por contacto en cerámicas de circona 3Y-TZP sometida a diferentes tiempos de degradación hidrotérmica (0, 5, 10, 30 y 60 horas), mediante la utilización de metodologías de indentación esférica (hertziana) Se analiza el comportamiento plástico del material mediante la evaluación del daño que se genera producto de la aplicación de cargas monotónicas en la superficie. Así mismo se desarrolla un mapa de daño y se evalúa el comportamie...

Origin of unusual sintering phenomena in compacts of chloride-derived 3Y-TZP nanopowders

Directory of Open Access Journals (Sweden)

Sweeney Sean M.

2014-01-01

Full Text Available After evaluating three alternative possibilities, the present study shows that seemingly minor amounts (at least as low as 0.06 wt% of chlorine impurities are responsible for the poor sintering behavior observed in chloride-derived 3 mol% yttria stabilized zirconia (3Y-TZP nanopowders. Models and quantitative estimates are used to explain the role of evolved HCl and ZrCl4 gases in such anomalous behaviors as reduced sintered densities for higher green densities, de-densification, improved sintering in nitrogen over oxygen, and formation of a dense shell microstructure. Two solutions to problematic residual chlorides are compared: 1 a thermal treatment composed of an extended hold at 1000°C to allow HCl gas removal before the onset of closed porosity, and 2 a chemical treatment performed by washing bisque-fired samples at room temperature using a concentrated ammonium hydroxide solution to remove chlorides. The thermal treatment was found to be superior.

41 CFR 101-30.101-8 - Conversion.

Science.gov (United States)

2010-07-01

... classifications, stock numbers, names, and identification data to using those of the Federal Catalog System in all... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Conversion. 101-30.101-8 Section 101-30.101-8 Public Contracts and Property Management Federal Property Management Regulations...

41 CFR 101-39.101-1 - Agency cooperation.

Science.gov (United States)

2010-07-01

...-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.1-Establishment, Modification, and Discontinuance of Interagency Fleet... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Agency cooperation. 101-39.101-1 Section 101-39.101-1 Public Contracts and Property Management Federal Property Management...

Fracture Toughness and Micro-Strain of Y-TZP Nanoceramics at Different Sintering Temperature

Directory of Open Access Journals (Sweden)

Rabiha S. Yaseen

2017-11-01

Full Text Available The objective of this research is to study the effect of sintering temperature on the mechanical properties and micro-strain of yttria tetragonal zirconia polycrystalls (Y-TZP nanostructure.   Where green disk formed by uniaxially press, sintered at (1500 – 1550 – 1600⁰C in air for 2hr then polished to mirror shape for fracture toughness and micro-hardness measurement by Vickers indenter at (60 kg to 100gm loads. Atomic force microscopy (AFM technique was use to measure the change in grain size and shape of the samples, X-ray diffraction (XRD evaluated to identify the phases and to measure the micro-strain of the samples.          The Results show that increasing sintering temperature will increase the grain size with increasing the average of micro-strain. Tetragonal  phase is the prevailing phase with small amount of cubic phase and the amount of monoclinic phase was under detection limite after sintering but there is increas in lattice dimension according to micro-strain calculation and grinding process produce micro-strain. With increasing the sintering temperature micro-hardness and fracture toughness will increas.

Effects of core-to-dentin thickness ratio on the biaxial flexural strength, reliability, and fracture mode of bilayered materials of zirconia core (Y-TZP) and veneer indirect composite resins.

Science.gov (United States)

Su, Naichuan; Liao, Yunmao; Zhang, Hai; Yue, Li; Lu, Xiaowen; Shen, Jiefei; Wang, Hang

2017-01-01

Indirect composite resins (ICR) are promising alternatives as veneering materials for zirconia frameworks. The effects of core-to-dentin thickness ratio (C/Dtr) on the mechanical property of bilayered veneer ICR/yttria-tetragonal zirconia polycrystalline (Y-TZP) core disks have not been previously studied. The purpose of this in vitro study was to assess the effects of C/Dtr on the biaxial flexural strength, reliability, and fracture mode of bilayered veneer ICR/ Y-TZP core disks. A total of 180 bilayered 0.6-mm-thick composite resin disks in core material and C/Dtr of 2:1, 1:1, and 1:2 were tested with either core material placed up or placed down for piston-on-3-ball biaxial flexural strength. The mean biaxial flexural strength, Weibull modulus, and fracture mode were measured to evaluate the variation trend of the biaxial flexural strength, reliability, and fracture mode of the bilayered disks with various C/Dtr. One-way analysis of variance (ANOVA) and chi-square tests were used to evaluate the variation tendency of fracture mode with the C/Dtr or material placed down during testing (α=.05). Light microscopy was used to identify the fracture mode. The mean biaxial flexural strength and reliability improved with the increase in C/Dtr when specimens were tested with the core material either up and down, and depended on the materials that were placed down during testing. The rates of delamination, Hertzian cone cracks, subcritical radial cracks, and number of fracture fragments partially depended on the C/Dtr and the materials that were placed down during testing. The biaxial flexural strength, reliability, and fracture mode in bilayered structures of Y-TZP core and veneer ICR depend on both the C/Dtr and the material that was placed down during testing. Copyright © 2016 Editorial Council for the Journal of Prosthetic Dentistry. Published by Elsevier Inc. All rights reserved.

41 CFR 101-30.101-1a - Item of production.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Item of production. 101-30.101-1a Section 101-30.101-1a Public Contracts and Property Management Federal Property Management....1-General § 101-30.101-1a Item of production. Item-of-production means those articles, equipment...

Unique in vitro and in vivo thrombopoietic activities of ingenol 3,20 dibenzoate, a Ca(++-independent protein kinase C isoform agonist.

Directory of Open Access Journals (Sweden)

Frederick K Racke

Full Text Available Thrombopoiesis following severe bone marrow injury frequently is delayed, thereby resulting in life-threatening thrombocytopenia for which there are limited treatment options. The reasons for these delays in recovery are not well understood. Protein kinase C (PKC agonists promote megakaryocyte differentiation in leukemia cell lines and primary cells. However, little is known about the megakaryopoietic effects of PKC agonists on primary CD34+ cells grown in culture or in vivo. Here we present evidence that the novel PKC isoform-selective agonist 3,20 ingenol dibenzoate (IDB potently stimulates early megakaryopoiesis of human CD34+ cells. In contrast, broad spectrum PKC agonists failed to do so. In vivo, a single intraperitoneal injection of IDB selectively increased platelets in mice without affecting hemoglobin or white counts. Finally, IDB strongly mitigated radiation-induced thrombocytopenia, even when administered 24 hours after irradiation. Our data demonstrate that novel PKC isoform agonists such as IDB may represent a unique therapeutic strategy for accelerating the recovery of platelet counts following severe marrow injury.

41 CFR 101-30.101-3 - National stock number.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true National stock number. 101-30.101-3 Section 101-30.101-3 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 30-FEDERAL CATALOG SYSTEM 30...

The epileptogenic spectrum of opiate agonists.

Science.gov (United States)

Snead, O C; Bearden, L J

1982-11-01

The present authors gave mu, delta, kappa, epsilon and sigma opiate receptor agonists intracerebroventricularly to rats both singly and in combination while monitoring the electroencephalogram from cortical and depth electrodes. Dose-response curves were plotted with naloxone against the changes produced by each agonist, and the effect of a number of anticonvulsant drugs on agonist-induced seizures was ascertained. Each opiate agonist produced a different seizure pattern with a different naloxone dose-response curve and anticonvulsant profile. The order of convulsive potency was epsilon greater than delta greater than mu greater than sigma much greater than kappa. Petit mal-like seizure activity was unique to the delta agonist, leucine-enkephalin, while only the mu agonist, morphine produced generalized convulsive seizures. These experiments raise the possibility that opiate systems in the brain may be involved in the pathogenesis of a wide spectrum of seizure disorders.

The Effect of Glucagon-Like Peptide 1 Receptor Agonists on Weight Loss in Type 2 Diabetes: A Systematic Review and Mixed Treatment Comparison Meta-Analysis.

Directory of Open Access Journals (Sweden)

Jessica E Potts

Full Text Available To determine the effects of glucagon-like peptide-1 receptor agonists compared with placebo and other anti-diabetic agents on weight loss in overweight or obese patients with type 2 diabetes mellitus.Electronic searches were conducted for randomised controlled trials that compared a glucagon-like peptide-1 receptor agonist therapy at a clinically relevant dose with a comparator treatment (other type 2 diabetes treatment or placebo in adults with type 2 diabetes and a mean body mass index ≥ 25 kg/m2. Pair-wise meta-analyses and mixed treatment comparisons were conducted to examine the difference in weight change at six months between the glucagon-like peptide-1 receptor agonists and each comparator.In the mixed treatment comparison (27 trials, the glucagon-like peptide-1 receptor agonists were the most successful in terms of weight loss; exenatide 2 mg/week: -1.62 kg (95% CrI: -2.95 kg, -0.30 kg, exenatide 20 μg: -1.37 kg (95% CI: -222 kg, -0.52 kg, liraglutide 1.2 mg: -1.01 kg (95%CrI: -2.41 kg, 0.38 kg and liraglutide 1.8 mg: -1.51 kg (95% CI: -2.67 kg, -0.37 kg compared with placebo. There were no differences between the GLP-1 receptor agonists in terms of weight loss.This review provides evidence that glucagon-like peptide-1 receptor agonist therapies are associated with weight loss in overweight or obese patients with type 2 diabetes with no difference in weight loss seen between the different types of GLP-1 receptor agonists assessed.

Evaluation of partial beta-adrenoceptor agonist activity.

Science.gov (United States)

Lipworth, B J; Grove, A

1997-01-01

A partial beta-adrenoceptor (beta-AR) agonist will exhibit opposite agonist and antagonist activity depending on the prevailing degree of adrenergic tone or the presence of a beta-AR agonist with higher intrinsic activity. In vivo partial beta-AR agonist activity will be evident at rest with low endogenous adrenergic tone, as for example with chronotropicity (beta 1/beta 2), inotropicity (beta 1) or peripheral vasodilatation and finger tremor (beta 2). beta-AR blocking drugs which have partial agonist activity may exhibit a better therapeutic profile when used for hypertension because of maintained cardiac output without increased systemic vascular resistance, along with an improved lipid profile. In the presence of raised endogenous adrenergic tone such as exercise or an exogenous full agonist, beta-AR subtype antagonist activity will become evident in terms of effects on exercise induced heart rate (beta 1) and potassium (beta 2) responses. Reduction of exercise heart rate will occur to a lesser degree in the case of a beta-adrenoceptor blocker with partial beta 1-AR agonist activity compared with a beta-adrenoceptor blocker devoid of partial agonist activity. This may result in reduced therapeutic efficacy in the treatment of angina on effort when using beta-AR blocking drugs with partial beta 1-AR agonist activity. Effects on exercise hyperkalaemia are determined by the balance between beta 2-AR partial agonist activity and endogenous adrenergic activity. For predominantly beta 2-AR agonist such as salmeterol and salbutamol, potentiation of exercise hyperkalaemia occurs. For predominantly beta 2-AR antagonists such as carteolol, either potentiation or attenuation of exercise hyperkalaemia occurs at low and high doses respectively. beta 2-AR partial agonist activity may also be expressed as antagonism in the presence of an exogenous full agonist, as for example attenuation of fenoterol induced responses by salmeterol. Studies are required to investigate whether

41 CFR 101-1.101 - Federal Property Management Regulations System.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Federal Property Management Regulations System. 101-1.101 Section 101-1.101 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1...

41 CFR 101-30.101-13 - Management data.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Management data. 101-30....1-General § 101-30.101-13 Management data. Management data means recorded data that relate an item... of supply, or inventory control. Management data do not affect the identification of an item. [41 FR...

Conformational changes in acetylcholine binding protein investigated by temperature accelerated molecular dynamics.

Directory of Open Access Journals (Sweden)

Zeynab Mohammad Hosseini Naveh

Full Text Available Despite the large number of studies available on nicotinic acetylcholine receptors, a complete account of the mechanistic aspects of their gating transition in response to ligand binding still remains elusive. As a first step toward dissecting the transition mechanism by accelerated sampling techniques, we study the ligand-induced conformational changes of the acetylcholine binding protein (AChBP, a widely accepted model for the full receptor extracellular domain. Using unbiased Molecular Dynamics (MD and Temperature Accelerated Molecular Dynamics (TAMD simulations we investigate the AChBP transition between the apo and the agonist-bound state. In long standard MD simulations, both conformations of the native protein are stable, while the agonist-bound structure evolves toward the apo one if the orientation of few key sidechains in the orthosteric cavity is modified. Conversely, TAMD simulations initiated from the native conformations are able to produce the spontaneous transition. With respect to the modified conformations, TAMD accelerates the transition by at least a factor 10. The analysis of some specific residue-residue interactions points out that the transition mechanism is based on the disruption/formation of few key hydrogen bonds. Finally, while early events of ligand dissociation are observed already in standard MD, TAMD accelerates the ligand detachment and, at the highest TAMD effective temperature, it is able to produce a complete dissociation path in one AChBP subunit.

Analysis of flame acceleration in open or vented obstructed pipes

Science.gov (United States)

Bychkov, Vitaly; Sadek, Jad; Akkerman, V'yacheslav

2017-01-01

While flame propagation through obstacles is often associated with turbulence and/or shocks, Bychkov et al. [V. Bychkov et al., Phys. Rev. Lett. 101, 164501 (2008), 10.1103/PhysRevLett.101.164501] have revealed a shockless, conceptually laminar mechanism of extremely fast flame acceleration in semiopen obstructed pipes (one end of a pipe is closed; a flame is ignited at the closed end and propagates towards the open one). The acceleration is devoted to a powerful jet flow produced by delayed combustion in the spaces between the obstacles, with turbulence playing only a supplementary role in this process. In the present work, this formulation is extended to pipes with both ends open in order to describe the recent experiments and modeling by Yanez et al. [J. Yanez et al., arXiv:1208.6453] as well as the simulations by Middha and Hansen [P. Middha and O. R. Hansen, Process Safety Prog. 27, 192 (2008) 10.1002/prs.10242]. It is demonstrated that flames accelerate strongly in open or vented obstructed pipes and the acceleration mechanism is similar to that in semiopen ones (shockless and laminar), although acceleration is weaker in open pipes. Starting with an inviscid approximation, we subsequently incorporate hydraulic resistance (viscous forces) into the analysis for the sake of comparing its role to that of a jet flow driving acceleration. It is shown that hydraulic resistance is actually not required to drive flame acceleration. In contrast, this is a supplementary effect, which moderates acceleration. On the other hand, viscous forces are nevertheless an important effect because they are responsible for the initial delay occurring before the flame acceleration onset, which is observed in the experiments and simulations. Accounting for this effect provides good agreement between the experiments, modeling, and the present theory.

Effects of local anesthetics on cholinergic agonist binding affinity of central nervous system. cap alpha. -bungarotoxin receptors

Energy Technology Data Exchange (ETDEWEB)

Lukas, R.L.; Bennett, E.L.

1979-12-01

In general, pharmacological effects of local anesthetics may be attributed to their ability to reversibly block the propagation of nerve and muscle action potentials. At physiologically potent concentrations, local anesthetics (LA) also act as noncompetitive antagonists of the physiological response of post-synaptic nicotinic acetylcholine receptors (nAChR) to cholinergic agonists, and increase agonist binding affinities of nAChR from electric organ. It is postulated that the primary site of LA action on nAChR function is at the receptor-coupled ionophore. Furthermore, LA-nAChR ionophore interactions are thought to accelerate physiological desensitization of nAChR, manifest biochemically as increased affinity of nAChR for agonist. Specific receptors for ..cap alpha..-bungarotoxin (..cap alpha..-Bgt), a potent competitive antagonist at nAChR sites in the periphery, have been detected in rat central nervous system membrane preparations. The affinity of these central ..cap alpha..-Bgt receptors (..cap alpha..-BgtR) for cholinergic agonists is found to increase on exposure to agonist. Nevertheless, on the basis of inconsistent pharmacological and physiological results, uncertainty remains regarding the relationship between ..cap alpha..-BgtR and authentic nAChR in the CNS, despite a wide body of biochemical and histological evidence consistent with their identity. Reasoning that if CNS ..cap alpha..-BgtR are true in nAChR, coupled to functional ion channels, LA might be expected to cause biochemically measurable increases in ..cap alpha..-BgtR affinity for cholinergic agonists, we have undertaken a study of the effects of LA on the ability of acetylcholine (ACh) to inhibit interaction of ..cap alpha..-BgtR with /sup 3/H-labeled ..cap alpha..-Bgt.

The Effects of Ammonium Polyacrylate and Diammonium Citrate as Base and Acid Dispersion Agents on Yttria-Stabilized Zirconia (3Y-TZP Dispersion Properties

Directory of Open Access Journals (Sweden)

Pestaria Sinaga

2018-01-01

Full Text Available Stable slurries in dispersions of 3Y-TZP in aqueous suspension with the addition of different concentrations of dispersants such as ammonium polyacrylate (APA and diammonium citrate (DAC were investigated. The dispersion properties were investigated by measuring the particle size, zeta potential, sedimentation, and viscosity as a function of the wt.% of the dispersant. Both dispersant agents were attached to the 3Y-TZP surface by the carboxylic group, as shown by the FTIR results. The addition of dispersants was found to produce more dispersed and stabilized aqueous suspension. As shown the viscosity result, that there is no being viscosity peak has been occurring and viscosity going decrease as the shear rates increasing which mean that the suspension has shear thinning behavior and there is no agglomeration as the shear rate is increased. It was determined that 3.5 wt.% of DAC and APA produced the best and most stable slurry; when 3.5 wt.% of DAC and APA was added, the zeta potential showed the largest value in the monodisperse condition. The low pH value of DAC has obtained the higher zeta potential value than APA, which was assumed due to low pH of DAC suspension. At low pH, the adsorption of the adsorbate will occur in a flat adsorbed, while at higher pH the polyelectrolyte will dangle into solution, thus reducing electrostatic repulsion as it is found in the case of APA addition. In this condition, the particle size was decreased to the lower value and the slurry’s stability was obtained with the lowest sedimentation height after the sedimentation test for 30 days. The sample was milled in an attrition mill at 1,000 rpm for four hours.

41 CFR 101-26.505-4-101-26.505-6 - [Reserved

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true [Reserved] 101-26.505-4-101-26.505-6 Section 101-26.505-4-101-26.505-6 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26...

Dopaminergic agonists for hepatic encephalopathy

DEFF Research Database (Denmark)

Als-Nielsen, B; Gluud, L L; Gluud, C

2004-01-01

Hepatic encephalopathy may be associated with an impairment of the dopaminergic neurotransmission. Dopaminergic agonists may therefore have a beneficial effect on patients with hepatic encephalopathy.......Hepatic encephalopathy may be associated with an impairment of the dopaminergic neurotransmission. Dopaminergic agonists may therefore have a beneficial effect on patients with hepatic encephalopathy....

Beta-agonists and animal welfare

Science.gov (United States)

The use of beta-agonists in animal feed is a high profile topic within the U.S. as consumers and activist groups continue to question its safety. The only beta-agonist currently available for use in swine is ractopamine hydrochloride (RAC). This is available as Paylean™ (Elanco Animal Health – FDA a...

Treatment of dry eye syndrome with orally administered CF101: data from a phase 2 clinical trial.

Science.gov (United States)

Avni, Isaac; Garzozi, Hanna J; Barequet, Irina S; Segev, Fanni; Varssano, David; Sartani, Gil; Chetrit, Noa; Bakshi, Erez; Zadok, David; Tomkins, Oren; Litvin, Gilad; Jacobson, Kenneth A; Fishman, Sari; Harpaz, Zivit; Farbstein, Motti; Yehuda, Sara Bar; Silverman, Michael H; Kerns, William D; Bristol, David R; Cohn, Ilan; Fishman, Pnina

2010-07-01

To explore the safety and efficacy of CF101, an A(3) adenosine receptor agonist, in patients with moderate to severe dry eye syndrome. Phase 2, multicenter, randomized, double-masked, placebo-controlled, parallel-group study. Sixty-eight patients completed the study, 35 patients in the placebo group and 33 patients in the CF101 group. Patients were treated orally with either 1 mg CF101 pills or matching vehicle-filled placebo pills, given twice daily for 12 weeks, followed by a 2-week posttreatment observation. An improvement of more than 25% over baseline at week 12 in one of the following parameters: (1) tear break-up time (BUT); (2) superficial punctate keratitis assessed by fluorescein staining results; and (3) Schirmer tear test 1 results. Clinical laboratory safety tests, ophthalmic examinations, intraocular pressure (IOP) measurements, electrocardiographic evaluations, vital sign measurements, and monitoring of adverse events. A statistically significant increase in the proportion of patients who achieved more than 25% improvement in the corneal staining and in the clearance of corneal staining was noted between the CF101-treated group and the placebo group. Treatment with CF101 resulted in a statistically significant improvement in the mean change from baseline at week 12 of the corneal staining, BUT, and tear meniscus (TM) height in the CF101-treated group. CF101 was well tolerated and exhibited an excellent safety profile with no serious adverse events. A statistically significant decrease from baseline was observed in the IOP of the CF101-treated group in comparison with the placebo group. CF101, given orally, induced a statistically significant improvement in the corneal staining and an improvement in the BUT and TM in patients with moderate to severe dry eye syndrome. The drug was very well tolerated. These data and the anti-inflammatory characteristic of CF101 support further study of the drug as a potential treatment for the signs and symptoms of dry

The potential for buoyant displacement gas release events in Tank 241-SY-102 after waste transfer from Tank 241-SY-101

International Nuclear Information System (INIS)

Wells, BE; Meyer, P.E.; Chen, G.

2000-01-01

Tank 241-SY-101 (SY-101) is a double-shell, radioactive waste storage tank with waste that, before the recent transfer and water back-dilution operations, was capable of retaining gas and producing buoyant displacement (BD) gas release events (GREs). Some BD GREs caused gas concentrations in the tank headspace to exceed the lower flammability limit (LFL). A BD GRE occurs when a portion of the nonconvective layer retains enough gas to become buoyant, rises to the waste surface, breaks up, and releases some of its stored gas. The installation of a mixer pump in 1993 successfully mitigated gas retention in the settled solids layer in SY-101 and has since prevented BD GREs. However, operation of the mixer pump over the years caused gas retention in the floating crust layer and a corresponding accelerated waste level growth. The accelerating crust growth trend observed in 1997--98 led to initiation of sequences of waste removal and water back-dilutions in December 1999. Waste is removed from the mixed slurry layer in Tank SY-101 and transferred into Tank 241-Sy-102 (SY-102). Water is then added back to dissolve soluble solids that retain gas. The initial transfer of 89,500 gallons of SY-101 waste, diluted in-line at 0.94:1 by volume with water, to SY-102 was conducted in December 1999. The second transfer of 230,000 gallons of original SY-101 waste, diluted approximately 0.9:1, was completed in January 2000, and the third transfer of 205,500 gallons of original SY-101 waste diluted at 0.9:1 was completed in March 2000

Cytotoxicity and biocompatibility of Zirconia (Y-TZP posts with various dental cements

Directory of Open Access Journals (Sweden)

Hyeongsoon Shin

2016-08-01

Full Text Available Objectives Endodontically treated teeth with insufficient tooth structure are often restored with esthetic restorations. This study evaluated the cytotoxicity and biological effects of yttria partially stabilized zirconia (Y-TZP blocks in combination with several dental cements. Materials and Methods Pairs of zirconia cylinders with medium alone or cemented with three types of dental cement including RelyX U200 (3M ESPE, FujiCEM 2 (GC, and Panavia F 2.0 (Kuraray were incubated in medium for 14 days. The cytotoxicity of each supernatant was determined using 3-(4,5-dimethylthiazole-2-yl-2,5-diphenyltetrazolium bromide (MTT assays on L929 fibroblasts and MC3T3-E1 osteoblasts. The levels of interleukin-6 (IL-6 mRNA were evaluated by reverse transcription polymerase chain reaction (RT-PCR, and IL-6 protein was evaluated by enzyme-linked immunosorbent assays (ELISA. The data were analyzed using one-way ANOVA and Tukey post-hoc tests. A p < 0.05 was considered statistically significant. Results The MTT assays showed that MC3T3-E1 osteoblasts were more susceptible to dental cements than L929 fibroblasts. The resin based dental cements increased IL-6 expression in L929 cells, but reduced IL-6 expression in MC3T3-E1 cells. Conclusions Zirconia alone or blocks cemented with dental cement showed acceptable biocompatibilities. The results showed resin-modified glass-ionomer based cement less produced inflammatory cytokines than other self-adhesive resin-based cements. Furthermore, osteoblasts were more susceptible than fibroblasts to the biological effects of dental cement.

Alpha-2 adrenergic agonists for the prevention of cardiac complications among adults undergoing surgery.

Science.gov (United States)

Duncan, Dallas; Sankar, Ashwin; Beattie, W Scott; Wijeysundera, Duminda N

2018-03-06

was clonidine in 21 trials, dexmedetomidine in 24 trials and mivazerol in two trials.In non-cardiac surgery, there was high quality evidence that α-2 adrenergic agonists led to a similar risk of all-cause mortality compared with control groups (1.3% with α-2 adrenergic agonists versus 1.7% with control; RR 0.80, 95% CI 0.61 to 1.04; participants = 14,081; studies = 16). Additionally, the risk of cardiac mortality was similar between treatment groups (0.8% with α-2 adrenergic agonists versus 1.0% with control; RR 0.86, 95% CI 0.60 to 1.23; participants = 12,525; studies = 5, high quality evidence). The risk of myocardial infarction was probably similar between treatment groups (RR 0.94, 95% CI 0.69 to 1.27; participants = 13,907; studies = 12, moderate quality evidence). There was no associated effect on the risk of stroke (RR 0.93, 95% CI 0.55 to 1.56; participants = 11,542; studies = 7; high quality evidence). Conversely, α-2 adrenergic agonists probably increase the risks of clinically significant bradycardia (RR 1.59, 95% CI 1.18 to 2.13; participants = 14,035; studies = 16) and hypotension (RR 1.24, 95% CI 1.03 to 1.48; participants = 13,738; studies = 15), based on moderate quality evidence.There was insufficient evidence to determine the effect of α-2 adrenergic agonists on all-cause mortality in cardiac surgery (RR 0.52, 95% CI 0.26 to 1.04; participants = 1947; studies = 16) and myocardial infarction (RR 1.01, 95% CI 0.43 to 2.40; participants = 782; studies = 8), based on moderate quality evidence. There was one cardiac death in the clonidine arm of a study of 22 participants. Based on very limited data, α-2 adrenergic agonists may have reduced the risk of stroke (RR 0.37, 95% CI 0.15 to 0.93; participants = 1175; studies = 7; outcome events = 18; low quality evidence). Conversely, α-2 adrenergic agonists increased the risk of bradycardia from 6.4% to 12.0% (RR 1.88, 95% CI 1.35 to 2.62; participants = 1477; studies = 10; moderate quality evidence

Modification of kindled amygdaloid seizures by opiate agonists and antagonists.

Science.gov (United States)

Albertson, T E; Joy, R M; Stark, L G

1984-03-01

The effects of 19 opiate agonists and antagonists on kindled amygdaloid seizures in the rat were studied. The mu agonists tended to reduce the length of elicited afterdischarges and behavioral ranks, while markedly increasing postictal electroencephalogram spikes and behavioral arrest time. These effects were reversed by naloxone. The kappa agonists reduced behavioral rank and variably reduced afterdischarge length with a concomitant lengthening of postictal behavioral arrest time and number of electroencephalogram spikes. The putative sigma agonist, SKF 10,047, reduced afterdischarge durations only at the higher doses tested. The decreases found after the sigma agonists in postictal electroencephalogram spiking and time of behavioral arrest were not reversed by naloxone. Only the lower doses of normeperidine were found to decrease seizure thresholds. The mixed agonist/antagonists (MAA) cyclazocine and cyclorphan markedly increased seizure threshold and reduced afterdischarge duration and behavioral rank. Only the MAA pentazocine tended to increase threshold but not suprathreshold afterdischarge durations. The order of ability to modify the ictal events was MAA (selected) greater than kappa agonists greater than mu agonists greater than sigma agonists. The increase in postictal events (behavior arrest and spikes) was caused most effectively by pretreatment with mu agonist greater than kappa agonist greater than selected MAA greater than sigma agonists.(ABSTRACT TRUNCATED AT 250 WORDS)

A Discussion of SY-101 Crust Gas Retention and Release Mechanisms

International Nuclear Information System (INIS)

Mendoza, D.P.; Mahoney, L.A.; Gauglitz, P.A.; Rassat, S.D.; Caley, S.M.

1999-01-01

The flammable gas hazard in Hanford waste tanks was made an issue by the behavior of double-shell Tank (DST) 241-SY-101 (SY-101). Shortly after SY-101 was filled in 1980, the waste level began rising periodically, due to the generation and retention of gases within the slurry, and then suddenly dropping as the gases were released. An intensive study of the tank's behavior revealed that these episodic releases posed a safety hazard because the released gas was flammable, and, in some cases, the volume of gas released was sufficient to exceed the lower flammability limit (LFL) in the tank headspace (Alleinann et al. 1993). A mixer pump was installed in SY-101 in late 1993 to prevent gases from building up in the settled solids layer, and the large episodic gas releases have since ceased (Allemann et al. 1994; Stewart et al. 1994; Brewster et al. 1995). However, the surface level of SY-101 has been increasing since at least 1995, and in recent months the level growth has shown significant and unexpected acceleration. Based on a number of observations and measurements, including data from the void fraction instrument (VFI), we have concluded that the level growth is caused largely by increased gas retention in the floating crust. In September 1998, the crust contained between about 21 and 43% void based on VFI measurements (Stewart et al. 1998). Accordingly, it is important to understand the dominant mechanisms of gas retention, why the gas retention is increasing, and whether the accelerating level increase will continue, diminish or even reverse. It is expected that the retained gas in the crust is flammable, with hydrogen as a major constituent. This gas inventory would pose a flammable gas hazard if it were to release suddenly. In May 1997, the mechanisms of bubble retention and release from crust material were the subject of a workshop. The evaluation of the crust and potential hazards assumed a more typical void of roughly 15% gas. It could be similar to

A Discussion of SY-101 Crust Gas Retention and Release Mechanisms

Energy Technology Data Exchange (ETDEWEB)

SD Rassat; PA Gauglitz; SM Caley; LA Mahoney; DP Mendoza

1999-02-23

The flammable gas hazard in Hanford waste tanks was made an issue by the behavior of double-shell Tank (DST) 241-SY-101 (SY-101). Shortly after SY-101 was filled in 1980, the waste level began rising periodically, due to the generation and retention of gases within the slurry, and then suddenly dropping as the gases were released. An intensive study of the tank's behavior revealed that these episodic releases posed a safety hazard because the released gas was flammable, and, in some cases, the volume of gas released was sufficient to exceed the lower flammability limit (LFL) in the tank headspace (Allemann et al. 1993). A mixer pump was installed in SY-101 in late 1993 to prevent gases from building up in the settled solids layer, and the large episodic gas releases have since ceased (Allemann et al. 1994; Stewart et al. 1994; Brewster et al. 1995). However, the surface level of SY-101 has been increasing since at least 1995, and in recent months the level growth has shown significant and unexpected acceleration. Based on a number of observations and measurements, including data from the void fraction instrument (VFI), we have concluded that the level growth is caused largely by increased gas retention in the floating crust. In September 1998, the crust contained between about 21 and 43% void based on VFI measurements (Stewart et al. 1998). Accordingly, it is important to understand the dominant mechanisms of gas retention, why the gas retention is increasing, and whether the accelerating level increase will continue, diminish or even reverse. It is expected that the retained gas in the crust is flammable, with hydrogen as a major constituent. This gas inventory would pose a flammable gas hazard if it were to release suddenly. In May 1997, the mechanisms of bubble retention and release from crust material were the subject of a workshop. The evaluation of the crust and potential hazards assumed a more typical void of roughly 15% gas. It could be similar to

User Manual for the AZ-101 Data Acquisition System (AS-101 DAS)

Energy Technology Data Exchange (ETDEWEB)

BRAYTON, D.D.

2000-02-17

User manual for the TK AZ-101 Waste Retrieval System Data Acquisition System. The purpose of this document is to describe use of the AZ-101 Data Acquisition System (AZ-101 DAS). The AZ-101 DAS is provided to fulfill the requirements for data collection and monitoring as defined in Letters of Instruction (LOI) from Numatec Hanford Corporation (NHC) to Fluor Federal Services (FFS). For a complete description of the system, including design, please refer to the AZ-101 DAS System Description document, RPP-5572.

User Manual for the AZ-101 Data Acquisition System (AS-101 DAS)

International Nuclear Information System (INIS)

BRAYTON, D.D.

2000-01-01

User manual for the TK AZ-101 Waste Retrieval System Data Acquisition System. The purpose of this document is to describe use of the AZ-101 Data Acquisition System (AZ-101 DAS). The AZ-101 DAS is provided to fulfill the requirements for data collection and monitoring as defined in Letters of Instruction (LOI) from Numatec Hanford Corporation (NHC) to Fluor Federal Services (FFS). For a complete description of the system, including design, please refer to the AZ-101 DAS System Description document, RPP-5572

Dopamine agonist withdrawal syndrome: implications for patient care.

Science.gov (United States)

Nirenberg, Melissa J

2013-08-01

Dopamine agonists are effective treatments for a variety of indications, including Parkinson's disease and restless legs syndrome, but may have serious side effects, such as orthostatic hypotension, hallucinations, and impulse control disorders (including pathological gambling, compulsive eating, compulsive shopping/buying, and hypersexuality). The most effective way to alleviate these side effects is to taper or discontinue dopamine agonist therapy. A subset of patients who taper a dopamine agonist, however, develop dopamine agonist withdrawal syndrome (DAWS), which has been defined as a severe, stereotyped cluster of physical and psychological symptoms that correlate with dopamine agonist withdrawal in a dose-dependent manner, cause clinically significant distress or social/occupational dysfunction, are refractory to levodopa and other dopaminergic medications, and cannot be accounted for by other clinical factors. The symptoms of DAWS include anxiety, panic attacks, dysphoria, depression, agitation, irritability, suicidal ideation, fatigue, orthostatic hypotension, nausea, vomiting, diaphoresis, generalized pain, and drug cravings. The severity and prognosis of DAWS is highly variable. While some patients have transient symptoms and make a full recovery, others have a protracted withdrawal syndrome lasting for months to years, and therefore may be unwilling or unable to discontinue DA therapy. Impulse control disorders appear to be a major risk factor for DAWS, and are present in virtually all affected patients. Thus, patients who are unable to discontinue dopamine agonist therapy may experience chronic impulse control disorders. At the current time, there are no known effective treatments for DAWS. For this reason, providers are urged to use dopamine agonists judiciously, warn patients about the risks of DAWS prior to the initiation of dopamine agonist therapy, and follow patients closely for withdrawal symptoms during dopamine agonist taper.

Treatment of Plaque-Type Psoriasis With Oral CF101: Data from a Phase II/III Multicenter, Randomized, Controlled Trial.

Science.gov (United States)

David, Michael; Gospodinov, Dimitar Konstantinov; Gheorghe, Nicola; Mateev, Grisha Stefanov; Rusinova, Mariyana Venelinova; Hristakieva, Evgeniya; Solovastru, Laura Gheuca; Patel, Rita V; Giurcaneanu, Calin; Hitova, Mariela Chepileva; Purcaru, Anca Ioana; Horia, Beti; Tsingov, Iliya Iliev; Yankova, Rumyana Kaloferova; Kadurina, Miroslava Ilieva; Ramon, Michal; Rotaru, Maria; Simionescu, Olga; Benea, Vasile; Demerdjieva, Zdravka Velichkova; Cosgarea, Maria Rodica; Morariu, Horia Silviu; Michael, Ziv; Cristodor, Patricia; Nica, Carmen; Silverman, Michael H; Bristol, David R; Harpaz, Zivit; Farbstein, Motti; Cohen, Shira; Fishman, Pnina

2016-08-01

CF101, an adenosine A3 receptor agonist, is an orally bioavailable small molecule drug presenting an anti-psoriatic effect demonstrated in a Phase 2 clinical trial in psoriasis patients. To evaluate the safety and efficacy of CF101 treatment in a Phase 2/3 study in patients with moderate to severe plaque-type psoriasis. This multicenter, double-blind, 2-segment, placebo-controlled study randomized subjects with moderate to severe plaque psoriasis to CF101 1 or 2 mg, or placebo twice daily. At either week 12 (Segment 1) or 16 (Segment 2), the placebo group crossed over to CF101 BID through week 32 in an open-label fashion. At week 12, following an interim analysis, the CF101 1mg group was discontinued due to futility. The primary endpoint was proportion of patients achieving ≥75% improvement in Psoriasis Area Severity Index (PASI 75). Efficacy testing was performed using the Cochran-Mantel Haenszel test, the primary analysis of PASI 75 was performed at the 0.035 significance level. CF101 had an excellent safety profile at all tested dosages with a profile similar to the placebo group. The most common adverse events were infections and gastrointestinal events, and there was no cumulative intolerance over the 32-week dosing period. The study did not meet the primary endpoint of PASI 75 at week 12 (2 mg: 8.5% vs. placebo: 6.9%, P=0.621). However, at week 32, PASI mean percent improvement with CF101 2 mg was 57% (P<0.001) compared to baseline, with linear improvement in PASI 50 (63.5%), 75 (35.5%), 90 (24.7%), and 100 (10.6%). Oral CF101 was found to be safe and very well tolerated, demonstrating evidence of efficacy in patients with moderate to severe plaque psoriasis through 32 weeks of treatment. J Drugs Dermatol. 2016;15(8):931-938.

Resistencia al choque térmico de Y-TZP con fisuras Palmqvist

Directory of Open Access Journals (Sweden)

Fargas Ribas, G.

2003-02-01

Full Text Available The thermal shock response of two tetragonal zirconia polycrystals stabilised with 2.5% molar yttria, with two different levels of fracture toughness, has been investigated. Palmqvist cracks are generated by indentation and the crack extension is quantified by assuming that the residual thermal stresses responsible for its extension during thermal shock are smaller than those acting on the crack immediately after indentation. It is proposed to use a thermal shock resistance parameter that only depends on the crack extension induced by thermal stresses generated during the abrupt changes in temperature. The results are applied to the study of thermal shock resistance and they are compared with experimental results.

Se analiza el comportamiento frente al choque térmico de policristales de circona tetragonal dopados con 2.5% molar de itria (Y-TZP, con dos niveles distintos de tenacidad y con fisuras de indentación del tipo Palmqvist. El proceso de extensión de la fisura se cuantifica suponiendo que las tensiones residuales responsables de su propagación estable durante el choque térmico son inferiores a las presentes en el material inmediatamente después de aplicar la indentación. Se propone la utilización de un parámetro de resistencia al choque térmico que solamente depende de la extensión de las fisuras por efecto de las tensiones térmicas generadas durante el cambio brusco de temperatura. Los resultados del análisis se aplican al estudio del choque térmico y se comparan con los resultados experimentales.

Sports doping: emerging designer and therapeutic β2-agonists.

Science.gov (United States)

Fragkaki, A G; Georgakopoulos, C; Sterk, S; Nielen, M W F

2013-10-21

Beta2-adrenergic agonists, or β2-agonists, are considered essential bronchodilator drugs in the treatment of bronchial asthma, both as symptom-relievers and, in combination with inhaled corticosteroids, as disease-controllers. The use of β2-agonists is prohibited in sports by the World Anti-Doping Agency (WADA) due to claimed anabolic effects, and also, is prohibited as growth promoters in cattle fattening in the European Union. This paper reviews the last seven-year (2006-2012) literature concerning the development of novel β2-agonists molecules either by modifying the molecule of known β2-agonists or by introducing moieties producing indole-, adamantyl- or phenyl urea derivatives. New emerging β2-agonists molecules for future therapeutic use are also presented, intending to emphasize their potential use for doping purposes or as growth promoters in the near future. © 2013.

Overlapping binding site for the endogenous agonist, small-molecule agonists, and ago-allosteric modulators on the ghrelin receptor

DEFF Research Database (Denmark)

Holst, Birgitte; Frimurer, Thomas M; Mokrosinski, Jacek

2008-01-01

A library of robust ghrelin receptor mutants with single substitutions at 22 positions in the main ligand-binding pocket was employed to map binding sites for six different agonists: two peptides (the 28-amino-acid octanoylated endogenous ligand ghrelin and the hexapeptide growth hormone......, and PheVI:23 on the opposing face of transmembrane domain (TM) VI. Each of the agonists was also affected selectively by specific mutations. The mutational map of the ability of L-692,429 and GHRP-6 to act as allosteric modulators by increasing ghrelin's maximal efficacy overlapped with the common....... It is concluded that although each of the ligands in addition exploits other parts of the receptor, a large, common binding site for both small-molecule agonists--including ago-allosteric modulators--and the endogenous agonist is found on the opposing faces of TM-III and -VI of the ghrelin receptor....

Exploring the binding energy profiles of full agonists, partial agonists, and antagonists of the α7 nicotinic acetylcholine receptor.

Science.gov (United States)

Tabassum, Nargis; Ma, Qianyun; Wu, Guanzhao; Jiang, Tao; Yu, Rilei

2017-09-01

Nicotinic acetylcholine receptors (nAChRs) belong to the Cys-loop receptor family and are important drug targets for the treatment of neurological diseases. However, the precise determinants of the binding efficacies of ligands for these receptors are unclear. Therefore, in this study, the binding energy profiles of various ligands (full agonists, partial agonists, and antagonists) were quantified by docking those ligands with structural ensembles of the α7 nAChR exhibiting different degrees of C-loop closure. This approximate treatment of interactions suggested that full agonists, partial agonists, and antagonists of the α7 nAChR possess distinctive binding energy profiles. Results from docking revealed that ligand binding efficacy may be related to the capacity of the ligand to stabilize conformational states with a closed C loop.

The Beta-2-Adrenoreceptor Agonists, Formoterol and Indacaterol, but Not Salbutamol, Effectively Suppress the Reactivity of Human Neutrophils In Vitro

Directory of Open Access Journals (Sweden)

Ronald Anderson

2014-01-01

Full Text Available The clinical relevance of the anti-inflammatory properties of beta-2 agonists remains contentious possibly due to differences in their molecular structures and agonist activities. The current study has compared the effects of 3 different categories of β2-agonists, namely, salbutamol (short-acting, formoterol (long-acting and indacaterol (ultra-long-acting, at concentrations of 1–1000 nM, with human blood neutrophils in vitro. Neutrophils were activated with either N-formyl-L-methionyl-L-leucyl-L-phenylalanine (fMLP, 1 µM or platelet-activating factor (PAF, 200 nM in the absence and presence of the β2-agonists followed by measurement of the generation of reactive oxygen species and leukotriene B4, release of elastase, and expression of the β2-integrin, CR3, using a combination of chemiluminescence, ELISA, colorimetric, and flow cytometric procedures respectively. These were correlated with alterations in the concentrations of intracellular cyclic-AMP and cytosolic Ca2+. At the concentrations tested, formoterol and indacaterol caused equivalent, significant (P<0.05 at 1–10 nM dose-related inhibition of all of the pro-inflammatory activities tested, while salbutamol was much less effective (P<0.05 at 100 nM and higher. Suppression of neutrophil reactivity was accompanied by elevations in intracellular cAMP and accelerated clearance of Ca2+ from the cytosol of activated neutrophils. These findings demonstrate that β2-agonists vary with respect to their suppressive effects on activated neutrophils.

Effect of grinding and aging on subcritical crack growth of a Y-TZP ceramic.

Science.gov (United States)

Amaral, Marina; Weitzel, Isabela Sandim Souza Leite; Silvestri, Tais; Guilardi, Luis Felipe; Pereira, Gabriel Kalil Rocha; Valandro, Luiz Felipe

2018-01-01

This study aimed to investigate slow crack growth (SCG) behavior of a zirconia ceramic after grinding and simulated aging with low-temperature degradation (LTD). Complementary analysis of hardness, surface topography, crystalline phase transformation, and roughness were also measured. Disc-shaped specimens (15 mm Ø × 1.2 mm thick, n = 42) of a full-contour Y-TZP ceramic (Zirlux FC, Amherst) were manufactured according to ISO:6872-2008, and then divided into: Ctrl - as-sintered condition; Ctrl LTD - as-sintered after aging in autoclave (134°C, 2 bar, 20 h); G - ground with coarse diamond bur (grit size 181 μm); G LTD - ground and aged. The SCG parameters were measured by a dynamic biaxial flexural test, which determines the tensile stress versus stress rate under four different rates: 100, 10, 1 and 0.1 MPa/s. LTD led to m-phase content increase, as well as grinding (m-phase content: Ctrl - 0%; G - 12.3%; G LTD - 59.9%; Ctrl LTD - 81%). Surface topography and roughness analyses showed that grinding created an irregular surface (increased roughness) and aging did not promote any relevant surface change. There was no statistical difference on surface hardness among different conditions. The control group presented the lowest strength values in all tested rates. Regarding SCG, ground conditions were less susceptible to SCG, delaying its occurrence. Aging (LTD) caused an increase in SCG susceptibility for the as-sintered condition (i.e. G < G LTD < Ctrl < Ctrl LTD).

Gonadotropin releasing hormone agonists: Expanding vistas

Directory of Open Access Journals (Sweden)

Navneet Magon

2011-01-01

Full Text Available Gonadotropin-releasing hormone (GnRH agonists are derived from native GnRH by amino acid substitution which yields the agonist resistant to degradation and increases its half-life. The hypogonadotropic hypogonadal state produced by GnRH agonists has been often dubbed as "pseudomenopause" or "medical oophorectomy," which are both misnomers. GnRH analogues (GnRH-a work by temporarily "switching off" the ovaries. Ovaries can be "switched off" for the therapy and therapeutic trial of many conditions which include but are not limited to subfertility, endometriosis, adenomyosis, uterine leiomyomas, precocious puberty, premenstrual dysphoric disorder, chronic pelvic pain, or the prevention of menstrual bleeding in special clinical situations. Rapidly expanding vistas of usage of GnRH agonists encompass use in sex reassignment of male to female transsexuals, management of final height in cases of congenital adrenal hyperplasia, and preserving ovarian function in women undergoing cytotoxic chemotherapy. Hypogonadic side effects caused by the use of GnRH agonists can be tackled with use of "add-back" therapy. Goserelin, leuprolide, and nafarelin are commonly used in clinical practice. GnRH-a have provided us a powerful therapeutic approach to the treatment of numerous conditions in reproductive medicine. Recent synthesis of GnRH antagonists with a better tolerability profile may open new avenues for both research and clinical applications. All stakeholders who are partners in women′s healthcare need to join hands to spread awareness so that these drugs can be used to realize their full potential.

Sports doping: Emerging designer and therapeutic B2-agonists

NARCIS (Netherlands)

Fragkaki, A.G.; Georgakopoulos, C.; Sterk, S.S.; Nielen, M.W.F.

2013-01-01

Beta2-adrenergic agonists, or ß2-agonists, are considered essential bronchodilator drugs in the treatment of bronchial asthma, both as symptom-relievers and, in combination with inhaled corticosteroids, as disease-controllers. The use of ß2-agonists is prohibited in sports by the World Anti-Doping

Analysis of BmNPV orf101 disruption: orf101 is essential for mediating budded virus production.

Science.gov (United States)

Chen, Huiqing; Li, Mei; Mai, Weijun; Tang, Qi; Li, Guohui; Chen, Keping; Zhou, Yajing

2014-12-01

In our previous study, Orf101 (Bm101) of Bombyx mori nucleopolyhedrovirus (BmNPV) was identified as a component of the budded virions important for viral late gene expression. In this study we demonstrate that Bm101 is actually a previously unrecognized core gene and that it is essential for mediating budded virus production. To determine the role of Bm101 in the baculovirus life cycle, a Bm101 knockout bacmid containing the BmNPV genome was generated through homologous recombination in Escherichia coli. Furthermore, a Bm101 repair bacmid was constructed by transposing the Bm101 open reading frame with its native promoter region into the polyhedrin locus of the Bm101 knockout bacmid. Bacmid DNA transfection assay revealed that the Bm101 knockout bacmid was unable to produce the infectious budded virus, while the Bm101 repair bacmid rescued this defect, allowing budded-virus titers to reach wild-type levels. Real time PCR analysis indicated that the viral DNA genome in the absence of Bm101 was unaffected in the first 24 h p.t. Thus, studies of a Bm101-null BACmid indicate that Bm101 is required for viral DNA replication during the infection cycle.

Estrogen receptor beta-selective agonists stimulate calcium oscillations in human and mouse embryonic stem cell-derived neurons.

Directory of Open Access Journals (Sweden)

Lili Zhang

2010-07-01

Full Text Available Estrogens are used extensively to treat hot flashes in menopausal women. Some of the beneficial effects of estrogens in hormone therapy on the brain might be due to nongenomic effects in neurons such as the rapid stimulation of calcium oscillations. Most studies have examined the nongenomic effects of estrogen receptors (ER in primary neurons or brain slices from the rodent brain. However, these cells can not be maintained continuously in culture because neurons are post-mitotic. Neurons derived from embryonic stem cells could be a potential continuous, cell-based model to study nongenomic actions of estrogens in neurons if they are responsive to estrogens after differentiation. In this study ER-subtype specific estrogens were used to examine the role of ERalpha and ERbeta on calcium oscillations in neurons derived from human (hES and mouse embryonic stem cells. Unlike the undifferentiated hES cells the differentiated cells expressed neuronal markers, ERbeta, but not ERalpha. The non-selective ER agonist 17beta-estradiol (E(2 rapidly increased [Ca2+]i oscillations and synchronizations within a few minutes. No change in calcium oscillations was observed with the selective ERalpha agonist 4,4',4''-(4-Propyl-[1H]-pyrazole-1,3,5-triyltrisphenol (PPT. In contrast, the selective ERbeta agonists, 2,3-bis(4-Hydroxyphenyl-propionitrile (DPN, MF101, and 2-(3-fluoro-4-hydroxyphenyl-7-vinyl-1,3 benzoxazol-5-ol (ERB-041; WAY-202041 stimulated calcium oscillations similar to E(2. The ERbeta agonists also increased calcium oscillations and phosphorylated PKC, AKT and ERK1/2 in neurons derived from mouse ES cells, which was inhibited by nifedipine demonstrating that ERbeta activates L-type voltage gated calcium channels to regulate neuronal activity. Our results demonstrate that ERbeta signaling regulates nongenomic pathways in neurons derived from ES cells, and suggest that these cells might be useful to study the nongenomic mechanisms of estrogenic compounds.

In vitro shear bond strength of Y-TZP ceramics to different core materials with the use of three primer/resin cement systems.

Science.gov (United States)

Al-Harbi, Fahad A; Ayad, Neveen M; Khan, Zahid A; Mahrous, Amr A; Morgano, Steven M

2016-01-01

Durability of the bond between different core materials and zirconia retainers is an important predictor of the success of a dental prosthesis. Nevertheless, because of its polycrystalline structure, zirconia cannot be etched and bonded to a conventional resin cement. The purpose of this in vitro study was to compare the effects of 3 metal primer/resin cement systems on the shear bond strength (SBS) of 3 core materials bonded to yttria-stabilized tetragonal zirconia polycrystalline (Y-TZP) ceramic retainers. Zirconia ceramic (Cercon) disks (5×3 mm) were airborne-particle abraded, rinsed, and air-dried. Disk-shaped core specimens (7×7 mm) that were prepared of composite resin, Ni-Cr, and zirconia were bonded to the zirconia ceramic disks by using one of 3 metal primer/cement systems: (Z-Prime Plus/BisCem, Zirconia Primer/Multilink Automix, or Clearfil Ceramic Primer/Clearfil SA). SBS was tested in a universal testing machine. Stereomicroscopy was used to evaluate the failure mode of debonded specimens. Data were analyzed using 2-way ANOVA and post hoc analysis using the Scheffe procedure (α=.05). Clearfil SA/Clearfil Ceramic Primer system with an Ni-Cr core yielded the highest SBS value (19.03 MPa), whereas the lowest SBS value was obtained when Multilink Automix/Zirconia Primer system was used with the zirconia core group (4.09 MPa). Differences in mean SBS values among the cement/primer groups were statistically significant, except for Clearfil SA and BisCem with both composite resin and zirconia cores. Differences in mean SBS values among the core subgroups were not statistically significant, except for zirconia core with BisCem, Multilink, and Clearfil SA. The predominant failure mode was adhesive, except for Clearfil SA and BisCem luting agents with composite resin cores, which displayed cohesive failure, and Multilink Automix with a composite resin, core as well as Clearfil SA with Ni-Cr cores, where the debonded specimens of each group displayed a mixed

10 CFR 434.101 - Scope.

Science.gov (United States)

2010-01-01

... 10 Energy 3 2010-01-01 2010-01-01 false Scope. 434.101 Section 434.101 Energy DEPARTMENT OF ENERGY ENERGY CONSERVATION ENERGY CODE FOR NEW FEDERAL COMMERCIAL AND MULTI-FAMILY HIGH RISE RESIDENTIAL BUILDINGS Administration and Enforcement-General § 434.101 Scope. 101.1 This part provides design...

Phase transformation of dental zirconia following artificial aging.

Science.gov (United States)

Lucas, Thomas J; Lawson, Nathaniel C; Janowski, Gregg M; Burgess, John O

2015-10-01

Low-temperature degradation (LTD) of yttria-stabilized zirconia can produce increased surface roughness with a concomitant decrease in strength. This study determined the effectiveness of artificial aging (prolonged boiling/autoclaving) to induce LTD of Y-TZP (yttria-tetragonal zirconia-polycrystals) and used artificial aging for transformation depth progression analyses. The null hypothesis is aging techniques tested produce the same amount of transformation, transformation is not time/temperature dependent and LTD causes a constant transformation throughout the Y-TZP samples. Dental-grade Y-TZP samples were randomly divided into nine subgroups (n = 5): as received, 3.5 and 7 day boiling, 1 bar autoclave (1, 3, 5 h), and 2 bar autoclave (1, 3, 5 h). A 4-h boil treatment (n = 2) was performed post-experiment for completion of data. Transformation was measured using traditional X-ray diffraction and low-angle X-ray diffraction. The fraction of t → m transformation increased with aging time. The 3.5 day boil and 2 bar 5 h autoclave produced similar transformation results, while the 7 day boiling treatment revealed the greatest transformation. The surface layer of the aged specimen underwent the most transformation while all samples displayed decreasing transformation with depth. Surface transformation was evident, which can lead to rougher surfaces and increased wear of opposing dentition/materials. Therefore, wear studies addressing LTD of Y-TZP are needed utilizing accelerated aging. © 2014 Wiley Periodicals, Inc.

Modification of opiate agonist binding by pertussis toxin

Energy Technology Data Exchange (ETDEWEB)

Abood, M.E.; Lee, N.M.; Loh, H.H.

1986-03-05

Opiate agonist binding is decreased by GTP, suggesting the possible involvement of GTP binding proteins in regulation of opiate receptor binding. This possibility was addressed by asking whether pertussis toxin treatment, which results in ADP-ribosylation and modification of G proteins, would alter opiate agonist binding. The striatum was chosen for the initial brain area to be studied, since regulation of opiate action in this area had been shown to be modified by pertussis toxin. Treatment of striatal membranes with pertussis toxin results in up to a 55% decrease in /sup 3/(H)-DADLE binding as compared with membranes treated identically without toxin. This corresponds to a near complete ADP-ribosylation of both G proteins in the striatal membrane. The decrease in agonist binding appears to be due to an altered affinity of the receptor for agonist as opposed to a decrease in the number of sites. This effect of pertussis toxin on opiate agonist binding demonstrates the actual involvement of G proteins in regulation of opiate receptor binding.

Modification of opiate agonist binding by pertussis toxin

International Nuclear Information System (INIS)

Abood, M.E.; Lee, N.M.; Loh, H.H.

1986-01-01

Opiate agonist binding is decreased by GTP, suggesting the possible involvement of GTP binding proteins in regulation of opiate receptor binding. This possibility was addressed by asking whether pertussis toxin treatment, which results in ADP-ribosylation and modification of G proteins, would alter opiate agonist binding. The striatum was chosen for the initial brain area to be studied, since regulation of opiate action in this area had been shown to be modified by pertussis toxin. Treatment of striatal membranes with pertussis toxin results in up to a 55% decrease in 3 (H)-DADLE binding as compared with membranes treated identically without toxin. This corresponds to a near complete ADP-ribosylation of both G proteins in the striatal membrane. The decrease in agonist binding appears to be due to an altered affinity of the receptor for agonist as opposed to a decrease in the number of sites. This effect of pertussis toxin on opiate agonist binding demonstrates the actual involvement of G proteins in regulation of opiate receptor binding

7 CFR 1160.101 - Act.

Science.gov (United States)

2010-01-01

... 7 Agriculture 9 2010-01-01 2009-01-01 true Act. 1160.101 Section 1160.101 Agriculture Regulations... Definitions § 1160.101 Act. Act means the Fluid Milk Promotion Act of 1990, Subtitle H of Title XIX of the Food, Agriculture, Conservation, and Trade Act of 1990, Public Law 101-624, 7 U.S.C. 6401-6417, and any...

Reciprocity of agonistic support in ravens.

Science.gov (United States)

Fraser, Orlaith N; Bugnyar, Thomas

2012-01-01

Cooperative behaviour through reciprocation or interchange of valuable services in primates has received considerable attention, especially regarding the timeframe of reciprocation and its ensuing cognitive implications. Much less, however, is known about reciprocity in other animals, particularly birds. We investigated patterns of agonistic support (defined as a third party intervening in an ongoing conflict to attack one of the conflict participants, thus supporting the other) in a group of 13 captive ravens, Corvus corax. We found support for long-term, but not short-term, reciprocation of agonistic support. Ravens were more likely to support individuals who preened them, kin and dominant group members. These results suggest that ravens do not reciprocate on a calculated tit-for-tat basis, but aid individuals from whom reciprocated support would be most useful and those with whom they share a good relationship. Additionally, dyadic levels of agonistic support and consolation (postconflict affiliation from a bystander to the victim) correlated strongly with each other, but we found no evidence to suggest that receiving agonistic support influences the victim's likelihood of receiving support (consolation) after the conflict ends. Our findings are consistent with an emotionally mediated form of reciprocity in ravens and provide additional support for convergent cognitive evolution in birds and mammals.

The effect of sintering temperature on the 3Y-TZP co-doped with equimolar addition of the yttria and niobia

International Nuclear Information System (INIS)

Fonseca, Flavia Baccaro; Dorat, Daniele Ramos; Melo, Francisco Cristovao Lourenco de; Piorino Neto, Francisco; Reis, Danieli Aparecida

2010-01-01

The aim of this work is to identify the better sintering temperature to densify zirconia co-doped with yttria and niobia and to verify the existence of the stable tetragonal phase (t´) under applied stress at room temperature to be applied as a TBC material. Four compositions with equimolar addition of yttria and niobia in the 3Y-TZP were produced, 13.0 %, 14.5 %, 16.0 % and 17.5 %. The mixtures were prepared in high energy ball milling for 10 minutes and the samples prepared on uniaxial and isostatic pressing. The selected sintering temperatures were 1500 deg C, 1550 deg C, 1600 deg C and 1650 deg C, for 1 hour. Analysis of conventional and high resolution X-Ray Diffraction and measures of specific mass by Archimedes method were performed. Through measures of the specific mass, the best sintering temperature was 1550 deg C, with relative specific mass above 95 %. The x-ray diffraction analysis indicate a probable existence of t´ in all samples. (author)

Biomolecular modification of zirconia surfaces for enhanced biocompatibility

Energy Technology Data Exchange (ETDEWEB)

Hsu, Shih-Kuang; Hsu, Hsueh-Chuan [Department of Dental Technology and Materials Science, Central Taiwan University of Science and Technology, Taichung 40601, Taiwan, ROC (China); Ho, Wen-Fu [Department of Chemical and Materials Engineering, National University of Kaohsiung, Taiwan, ROC (China); Yao, Chun-Hsu [Department of Biomedical Imaging and Radiological Science, China Medical University, Taichung 40402, Taiwan, ROC (China); Chang, Pai-Ling [Taoyuan General Hospital, Taoyuan 33004, Taiwan, ROC (China); Wu, Shih-Ching, E-mail: scwu@ctust.edu.tw [Department of Dental Technology and Materials Science, Central Taiwan University of Science and Technology, Taichung 40601, Taiwan, ROC (China)

2014-12-01

Yttria-tetragonal zirconia polycrystal (Y-TZP) is a preferred biomaterial due to its good mechanical properties. In order to improve the biocompatibility of zirconia, RGD-peptide derived from extracellular matrix proteins was employed to modify the surface of Y-TZP to promote cell adhesion in this study. The surface of Y-TZP specimens was first modified using a hydrothermal method for different lengths of time. The topographies of modified Y-TZP specimens were analyzed by contact angle, XRD, FTIR, AFM, and FE-SEM. The mechanical properties were evaluated using Vickers hardness and three point bending strength. Then, the RGD-peptide was immobilized on the surface of the Y-TZP by chemical treatment. These RGD-peptide immobilized Y-TZP specimens were characterized by FTIR and AFM, and then were cocultured with MG-63 osteoblast cells for biocompatibility assay. The cell morphology and proliferation were evaluated by SEM, WST-1, and ALP activity assay. The XRD results indicated that the phase transition, from tetragonal phase to monoclinic phase, was increased with a longer incubation time of hydrothermal treatment. However, there were no significant differences in mechanical strengths after RGD-peptide was successfully grafted onto the Y-TZP surface. The SEM images showed that the MG-63 cells appeared polygonal, spindle-shaped, and attached on the RGD-peptide immobilized Y-TZP. The proliferation and cellular activities of MG-63 cells on the RGD-peptide immobilized Y-TZP were better than that on the unmodified Y-TZP. From the above results, the RGD-peptide can be successfully grafted onto the hydrothermal modified Y-TZP surface. The RGD-peptide immobilized Y-TZP can increase cell adhesion, and thus, improve the biocompatibility of Y-TZP. - Highlights: • Covalent bonding between peptide and Y-TZP was proposed. • Stable biomimetic structures produced on the surface of zirconia. • The biocompatibility was improved.

41 CFR 101-25.101-3 - Supply through consolidated purchase for direct delivery to use points.

Science.gov (United States)

2010-07-01

... consolidated purchase for direct delivery to use points. 101-25.101-3 Section 101-25.101-3 Public Contracts and... purchase for direct delivery to use points. The following criteria shall govern in determining whether an... following factors requires consolidated purchasing of such items for direct delivery to use points— (1...

Should We Use PPAR Agonists to Reduce Cardiovascular Risk?

Directory of Open Access Journals (Sweden)

Jennifer G. Robinson

2008-01-01

Full Text Available Trials of peroxisome proliferator-activated receptor (PPAR agonists have shown mixed results for cardiovascular prevention. Fibrates are PPAR- agonists that act primarily to improve dyslipidemia. Based on low- and high-density lipoprotein cholesterol (LDL and HDL effects, gemfibrozil may be of greater cardiovascular benefit than expected, fenofibrate performed about as expected, and bezafibrate performed worse than expected. Increases in both cardiovascular and noncardiovascular serious adverse events have been observed with some fibrates. Thiazolidinediones (TZDs are PPAR- agonists used to improve impaired glucose metabolism but also influence lipids. Pioglitazone reduces atherosclerotic events in diabetic subjects, but has no net cardiovascular benefit due to increased congestive heart failure risk. Rosiglitazone may increase the risk of atherosclerotic events, and has a net harmful effect on the cardiovascular system when congestive heart failure is included. The primary benefit of TZDs appears to be the prevention of diabetic microvascular complications. Dual PPAR-/ agonists have had unacceptable adverse effects but more selective agents are in development. PPAR- and pan-agonists are also in development. It will be imperative to prove that future PPAR agonists not only prevent atherosclerotic events but also result in a net reduction on total cardiovascular events without significant noncardiovascular adverse effects with long-term use.

Principles of agonist recognition in Cys-loop receptors

DEFF Research Database (Denmark)

Lynagh, Timothy Peter; Pless, Stephan Alexander

2014-01-01

, functional studies, and X-ray crystallography experiments identified the extracellular interface of adjacent subunits as the principal site of agonist binding. The question of how subtle differences at and around agonist-binding sites of different Cys-loop receptors can accommodate transmitters as chemically...

Aging properties of Kodak type 101 emulsions

Science.gov (United States)

Dohne, B.; Feldman, U.; Neupert, W.

1984-01-01

Aging tests for several batches of Kodak type 101 emulsion show that storage conditions significantly influence how well the film will maintain its sensitometric properties, with sensitivity and density increasing to a maximum during this period. Any further aging may result in higher fog levels and sensitivity loss. It is noted that storage in an environment free of photographically active compounds allows film property optimization, and that film batches with different sensitivities age differently. Emulsions with maximum 1700-A sensitivity are 2.5 times faster than those at the low end of the sensitivity scale. These sensitive emulsions exhibit significantly accelerated changes in aging properties. Their use in space applications requires careful consideration of time and temperature profiles, encouraging the use of less sensitive emulsions when the controllability of these factors is limited.

Long-acting β2-agonists in asthma

DEFF Research Database (Denmark)

Jacobson, Glenn A; Raidal, Sharanne; Hostrup, Morten

2018-01-01

Long-acting β2-agonists (LABAs) such as formoterol and salmeterol are used for prolonged bronchodilatation in asthma, usually in combination with inhaled corticosteroids (ICSs). Unexplained paradoxical asthma exacerbations and deaths have been associated with LABAs, particularly when used without...... and effects on BHR, particularly that (S)-enantiomers of β2-agonists may be deleterious to asthma control. LABAs display enantioselective pharmacokinetics and pharmacodynamics. Biological plausibility of the deleterious effects of β2-agonists (S)-enantiomers is provided by in vitro and in vivo studies from...... mechanism in rapid asthma deaths. More effort should therefore be applied to investigating potential enantiospecific effects of LABAs on safety, specifically bronchoprotection. Safety studies directly assessing the effects of LABA (S)-enantiomers on BHR are long overdue....

47 CFR 101.101 - Frequency availability.

Science.gov (United States)

2010-10-01

... Auxiliary Service—(Part 74) CARS: Cable Television Relay Service—(Part 78) CC: Common Carrier Fixed Point-to...: Digital Electronic Message Service—(Part 101, Subpart G) ISM: Industrial, Scientific & Medical—(Part 18...

48 CFR 32.101 - Authority.

Science.gov (United States)

2010-10-01

... 48 Federal Acquisition Regulations System 1 2010-10-01 2010-10-01 false Authority. 32.101 Section 32.101 Federal Acquisition Regulations System FEDERAL ACQUISITION REGULATION GENERAL CONTRACTING REQUIREMENTS CONTRACT FINANCING Non-Commercial Item Purchase Financing 32.101 Authority. The basic authority...

48 CFR 17.101 - Authority.

Science.gov (United States)

2010-10-01

... 48 Federal Acquisition Regulations System 1 2010-10-01 2010-10-01 false Authority. 17.101 Section 17.101 Federal Acquisition Regulations System FEDERAL ACQUISITION REGULATION CONTRACTING METHODS AND CONTRACT TYPES SPECIAL CONTRACTING METHODS Multiyear Contracting 17.101 Authority. This subpart implements...

5 CFR 831.101 - Administration.

Science.gov (United States)

2010-01-01

... 5 Administrative Personnel 2 2010-01-01 2010-01-01 false Administration. 831.101 Section 831.101 Administrative Personnel OFFICE OF PERSONNEL MANAGEMENT (CONTINUED) CIVIL SERVICE REGULATIONS (CONTINUED) RETIREMENT Administration and General Provisions § 831.101 Administration. (a) OPM has charge of the...

Wear behavior of tetragonal zirconia polycrystal versus titanium and titanium alloy

International Nuclear Information System (INIS)

Kanbara, Tsunemichi; Yajima, Yasutomo; Yoshinari, Masao

2011-01-01

The aim of this study was to clarify the influence of tetragonal zirconia polycrystal (TZP) on the two-body wear behavior of titanium (Ti). Two-body wear tests were performed using TZP, two grades of cp-Ti or Ti alloy in distilled water, and the cross-sectional area of worn surfaces was measured to evaluate the wear behavior. In addition, the surface hardness and coefficient of friction were determined and an electron probe microanalysis performed to investigate the underlying mechanism of wear. The hardness of TZP was much greater than that of Ti. The coefficient of friction between Ti and Ti showed a higher value than the Ti/TZP combination. Ti was more susceptible to wear by both TZP and Ti than TZP, indicating that the mechanism of wear between TZP and Ti was abrasive wear, whereas that between Ti and Ti was adhesive wear. No remarkable difference in the amount of wear in Ti was observed between TZP and Ti as the opposite material, despite the hardness value of Ti being much smaller than that of TZP. (communication)

Small-molecule AT2 receptor agonists

DEFF Research Database (Denmark)

Hallberg, Mathias; Sumners, Colin; Steckelings, U Muscha

2018-01-01

The discovery of the first selective, small-molecule ATR receptor (AT2R) agonist compound 21 (C21) (8) that is now extensively studied in a large variety of in vitro and in vivo models is described. The sulfonylcarbamate derivative 8, encompassing a phenylthiofen scaffold is the drug-like agonist...... with the highest affinity for the AT2R reported to date (Ki = 0.4 nM). Structure-activity relationships (SAR), regarding different biaryl scaffolds and functional groups attached to these scaffolds and with a particular focus on the impact of various para substituents displacing the methylene imidazole group of 8......, are discussed. Furthermore, the consequences of migration of the methylene imidazole group and presumed structural requirements for ligands that are aimed as AT2R agonists (e.g. 8) or AT2R antagonists (e.g. 9), respectively, are briefly addressed. A summary of the pharmacological actions of C21 (8) is also...

7 CFR 1900.101 - General.

Science.gov (United States)

2010-01-01

... 7 Agriculture 12 2010-01-01 2010-01-01 false General. 1900.101 Section 1900.101 Agriculture Regulations of the Department of Agriculture (Continued) RURAL HOUSING SERVICE, RURAL BUSINESS-COOPERATIVE... GENERAL Applicability of Federal Law § 1900.101 General. This subpart provides Agency policy concerning...

24 CFR 904.101 - Introduction.

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2010-04-01

... 24 Housing and Urban Development 4 2010-04-01 2010-04-01 false Introduction. 904.101 Section 904.101 Housing and Urban Development Regulations Relating to Housing and Urban Development (Continued... LOW RENT HOUSING HOMEOWNERSHIP OPPORTUNITIES Turnkey III Program Description § 904.101 Introduction...

5 CFR 430.101 - Authority.

Science.gov (United States)

2010-01-01

... 5 Administrative Personnel 1 2010-01-01 2010-01-01 false Authority. 430.101 Section 430.101 Administrative Personnel OFFICE OF PERSONNEL MANAGEMENT CIVIL SERVICE REGULATIONS PERFORMANCE MANAGEMENT Performance Management § 430.101 Authority. Chapter 43 of title 5, United States Code, provides for the...

7 CFR 786.101 - Administration.

Science.gov (United States)

2010-01-01

... 7 Agriculture 7 2010-01-01 2010-01-01 false Administration. 786.101 Section 786.101 Agriculture Regulations of the Department of Agriculture (Continued) FARM SERVICE AGENCY, DEPARTMENT OF AGRICULTURE SPECIAL PROGRAMS DAIRY DISASTER ASSISTANCE PAYMENT PROGRAM (DDAP-III) § 786.101 Administration. (a) DDAP...

7 CFR 1463.101 - Administration.

Science.gov (United States)

2010-01-01

... 7 Agriculture 10 2010-01-01 2010-01-01 false Administration. 1463.101 Section 1463.101 Agriculture Regulations of the Department of Agriculture (Continued) COMMODITY CREDIT CORPORATION, DEPARTMENT OF... Payment Program § 1463.101 Administration. (a) The program will be administered under the general...

18 CFR 284.101 - Applicability.

Science.gov (United States)

2010-04-01

... 18 Conservation of Power and Water Resources 1 2010-04-01 2010-04-01 false Applicability. 284.101 Section 284.101 Conservation of Power and Water Resources FEDERAL ENERGY REGULATORY COMMISSION, DEPARTMENT... Certain Transportation by Interstate Pipelines § 284.101 Applicability. This subpart implements section...

12 CFR 1805.101 - Summary.

Science.gov (United States)

2010-01-01

... 12 Banks and Banking 7 2010-01-01 2010-01-01 false Summary. 1805.101 Section 1805.101 Banks and Banking COMMUNITY DEVELOPMENT FINANCIAL INSTITUTIONS FUND, DEPARTMENT OF THE TREASURY COMMUNITY DEVELOPMENT FINANCIAL INSTITUTIONS PROGRAM General Provisions § 1805.101 Summary. Under the Community...

Long-acting beta(2)-agonists in management of childhood asthma

DEFF Research Database (Denmark)

Bisgaard, H

2000-01-01

This review assesses the evidence regarding the use of long-acting beta(2)-agonists in the management of pediatric asthma. Thirty double-blind, randomized, controlled trials on the effects of formoterol and salmeterol on lung function in asthmatic children were identified. Single doses of inhaled......, long-acting beta(2)-agonists provide effective bronchodilatation and bronchoprotection when used as intermittent, single-dose treatment of asthma in children, but not when used as regular treatment. Future studies should examine the positioning of long-acting beta(2)-agonists as an "as needed" rescue...... medication instead of short-acting beta(2)-agonists for pediatric asthma management....

47 CFR 101.513 - Transmitter power.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false Transmitter power. 101.513 Section 101.513... SERVICES 24 GHz Service and Digital Electronic Message Service § 101.513 Transmitter power. The transmitter power will be governed by § 101.113. Further, each application must contain an analysis demonstrating...

7 CFR 4287.101 - Introduction.

Science.gov (United States)

2010-01-01

... 7 Agriculture 15 2010-01-01 2010-01-01 false Introduction. 4287.101 Section 4287.101 Agriculture Regulations of the Department of Agriculture (Continued) RURAL BUSINESS-COOPERATIVE SERVICE AND RURAL... § 4287.101 Introduction. (a) This subpart supplements part 4279, subparts A and B, by providing...

14 CFR 1251.101 - Application.

Science.gov (United States)

2010-01-01

... 14 Aeronautics and Space 5 2010-01-01 2010-01-01 false Application. 1251.101 Section 1251.101 Aeronautics and Space NATIONAL AERONAUTICS AND SPACE ADMINISTRATION NONDISCRIMINATION ON BASIS OF HANDICAP General Provisions § 1251.101 Application. This part applies to each recipient of Federal financial...

47 CFR 101.1112 - Definitions.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false Definitions. 101.1112 Section 101.1112... SERVICES Competitive Bidding Procedures for LMDS § 101.1112 Definitions. (a) Scope. The definitions in this... million. (d) Entrepreneur. An entrepreneur is an entity that, together with its affiliates and controlling...

5 CFR 362.101 - Definitions.

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2010-01-01

... 5 Administrative Personnel 1 2010-01-01 2010-01-01 false Definitions. 362.101 Section 362.101... PROGRAM Definitions § 362.101 Definitions. For purposes of this part, An agency means a component within... outstanding record of achievement in an applicable leadership, policy, managerial, professional, or technical...

5 CFR 211.101 - Purpose.

Science.gov (United States)

2010-01-01

... 5 Administrative Personnel 1 2010-01-01 2010-01-01 false Purpose. 211.101 Section 211.101 Administrative Personnel OFFICE OF PERSONNEL MANAGEMENT CIVIL SERVICE REGULATIONS VETERAN PREFERENCE § 211.101 Purpose. The purpose of this part is to define veterans' preference and the administration of preference...

Spinal Cord Injury 101

Medline Plus

Full Text Available ... Topic Resources Peer Counseling Blog About Media Donate Spinal Cord Injury Medical Expert Videos Topics menu Topics Spinal Cord Injury 101 Adult Injuries Spinal Cord Injury 101 ...

Trial Watch: Toll-like receptor agonists for cancer therapy.

Science.gov (United States)

Vacchelli, Erika; Eggermont, Alexander; Sautès-Fridman, Catherine; Galon, Jérôme; Zitvogel, Laurence; Kroemer, Guido; Galluzzi, Lorenzo

2013-08-01

Toll-like receptors (TLRs) have long been known for their ability to initiate innate immune responses upon exposure to conserved microbial components such as lipopolysaccharide (LPS) and double-stranded RNA. More recently, this family of pattern recognition receptors has been attributed a critical role in the elicitation of anticancer immune responses, raising interest in the development of immunochemotherapeutic regimens based on natural or synthetic TLR agonists. In spite of such an intense wave of preclinical and clinical investigation, only three TLR agonists are currently licensed by FDA for use in cancer patients: bacillus Calmette-Guérin (BCG), an attenuated strain of Mycobacterium bovis that operates as a mixed TLR2/TLR4 agonist; monophosphoryl lipid A (MPL), a derivative of Salmonella minnesota that functions as a potent agonist of TLR4; and imiquimod, a synthetic imidazoquinoline that activates TLR7. One year ago, in the August and September issues of OncoImmunology , we described the main biological features of TLRs and discussed the progress of clinical studies evaluating the safety and therapeutic potential of TLR agonists in cancer patients. Here, we summarize the latest developments in this exciting area of research, focusing on preclinical studies that have been published during the last 13 mo and clinical trials launched in the same period to investigate the antineoplastic activity of TLR agonists.

Ascorbic acid enables reversible dopamine receptor 3H-agonist binding

International Nuclear Information System (INIS)

Leff, S.; Sibley, D.R.; Hamblin, M.; Creese, I.

1981-01-01

The effects of ascorbic acid on dopaminergic 3 H-agonist receptor binding were studied in membrane homogenates of bovine anterior pituitary and caudate, and rat striatum. In all tissues virtually no stereospecific binding (defined using 1uM (+)butaclamol) of the 3 H-agonists N-propylnorapomorphine (NPA), apomorphine, or dopamine could be demonstrated in the absence of ascorbic acid. Although levels of total 3 H-agonist binding were three to five times greater in the absence than in the presence of 0.1% ascorbic acid, the increased binding was entirely non-stereospecific. Greater amounts of dopamine-inhibitable 3 H-NPA binding could be demonstrated in the absence of 0.1% ascorbic acid, but this measure of ''specific binding'' was demonstrated not to represent dopamine receptor binding since several other catecholamines and catechol were equipotent with dopamine and more potent than the dopamine agonist (+/-)amino-6,7-dihydroxy-1,2,3,4-tetrahydronapthalene (ADTN) in inhibiting this binding. High levels of dopamine-displaceable 3 H-agonist binding were detected in fresh and boiled homogenates of cerebellum, an area of brain which receives no dopaminergic innervation, further demonstrating the non-specific nature of 3 H-agonist binding in the absence of ascorbic acid. These studies emphasize that under typical assay conditions ascorbic acid is required in order to demonstrate reversible and specific 3 H-agonist binding to dopamine receptors

Agonist-induced affinity alterations of a central nervous system. cap alpha. -bungarotoxin receptor

Energy Technology Data Exchange (ETDEWEB)

Lukas, R.J.; Bennett, E.L.

1979-01-01

The ability of cholinergic agonists to block the specific interaction of ..cap alpha..-bungarotoxin (..cap alpha..-Bgt) with membrane-bound sites derived from rat brain is enhanced when membranes are preincubated with agonist. Thus, pretreatment of ..cap alpha..-Bgt receptors with agonist (but not antagonist) causes transformation of sites to a high-affinity form toward agonist. This change in receptor state occurs with a half-time on the order of minutes, and is fully reversible on dilution of agonist. The results are consistent with the identity of ..cap alpha..-Bgt binding sites as true central nicotinic acetylcholine receptors. Furthermore, this agonist-induced alteration in receptor state may represent an in vitro correlate of physiological desensitization. As determined from the effects of agonist on toxin binding isotherms, and on the rate of toxin binding to specific sites, agonist inhibition of toxin binding to the high-affinity state is non-competitive. This result suggests that there may exist discrete toxin-binding and agonist-binding sites on central toxin receptors.

Spinal Cord Injury 101

Medline Plus

Full Text Available ... Topic Resources Peer Counseling Blog About Media Donate Spinal Cord Injury Medical Expert Videos Topics menu Topics Spinal Cord Injury 101 Adult Injuries Spinal Cord Injury 101 David ...

40 CFR 61.101 - Definitions.

Science.gov (United States)

2010-07-01

... definition of reference man are outlined in the International Commission on Radiological Protection's... 40 Protection of Environment 8 2010-07-01 2010-07-01 false Definitions. 61.101 Section 61.101....101 Definitions. As used in this subpart, all terms not defined here have the meaning given them in...

7 CFR 1220.101 - Act.

Science.gov (United States)

2010-01-01

... 7 Agriculture 10 2010-01-01 2010-01-01 false Act. 1220.101 Section 1220.101 Agriculture... CONSUMER INFORMATION Soybean Promotion and Research Order Definitions § 1220.101 Act. The term Act means the Soybean Promotion, Research, and Consumer Information Act, subtitle E of title XIX, of the Food...

5 CFR 7101.101 - General.

Science.gov (United States)

2010-01-01

... OF THE NATIONAL LABOR RELATIONS BOARD § 7101.101 General. (a) Purpose. In accordance with 5 CFR 2635... responsible for reviewing the Confidential Financial Disclosure Reports filed by designated NLRB employees... 5 Administrative Personnel 3 2010-01-01 2010-01-01 false General. 7101.101 Section 7101.101...

49 CFR 28.101 - Purpose.

Science.gov (United States)

2010-10-01

... 49 Transportation 1 2010-10-01 2010-10-01 false Purpose. 28.101 Section 28.101 Transportation Office of the Secretary of Transportation ENFORCEMENT OF NONDISCRIMINATION ON THE BASIS OF HANDICAP IN PROGRAMS OR ACTIVITIES CONDUCTED BY THE DEPARTMENT OF TRANSPORTATION § 28.101 Purpose. The purpose of this...

5 CFR 10.1 - Definitions.

Science.gov (United States)

2010-01-01

... the General Accounting Office; and (b) 'Merit system principles' means the principles for Federal... 5 Administrative Personnel 1 2010-01-01 2010-01-01 false Definitions. 10.1 Section 10.1... AUTHORITY TO REVIEW PERSONNEL MANAGEMENT PROGRAMS (RULE X) § 10.1 Definitions. For purposes of this rule— (a...

12 CFR 1806.101 - Summary.

Science.gov (United States)

2010-01-01

... 12 Banks and Banking 7 2010-01-01 2010-01-01 false Summary. 1806.101 Section 1806.101 Banks and Banking COMMUNITY DEVELOPMENT FINANCIAL INSTITUTIONS FUND, DEPARTMENT OF THE TREASURY BANK ENTERPRISE AWARD PROGRAM General Provisions § 1806.101 Summary. (a) Under the Bank Enterprise Award Program, the...

The relationship between milling a new silica-doped zirconia and its resistance to low-temperature degradation (LTD): a pilot study.

Science.gov (United States)

Nakamura, Takashi; Usami, Hirofumi; Ohnishi, Hiroshi; Nishida, Hisataka; Tang, Xuehua; Wakabayashi, Kazumichi; Sekino, Tohru; Yatani, Hirofumi

2012-02-03

The aim of this study was to determine the machinability of new silica-doped Y-TZP by CAD/CAM and the resistance to low temperature degradation of the milled sample by comparing with a commercial HIP type Y-TZP material. The copings could be milled from silica-doped Y-TZP blocks without chipping, and there was no significant difference between the two types of Y-TZP materials in either the marginal or the inner gap between the abutment and the coping. After aging, the monoclinic content in the commercial Y-TZP copings increased from 25% before testing to 65%, while that of silica-doped Y-TZP copings slightly increased from 23% to 30%. The silica-doped Y-TZP copings did not have any significant difference in fracture load in a comparison between the control group and the aging group, while the commercial Y-TZP copings had a significantly lower fracture load for the aging group than for the control group.

7 CFR 1150.101 - Act.

Science.gov (United States)

2010-01-01

... 7 Agriculture 9 2010-01-01 2009-01-01 true Act. 1150.101 Section 1150.101 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Marketing Agreements and... Definitions § 1150.101 Act. Act means Title I, Subtitle B, of the Dairy and Tobacco Adjustment Act of 1983...

19 CFR 101.0 - Scope.

Science.gov (United States)

2010-04-01

... 19 Customs Duties 1 2010-04-01 2010-04-01 false Scope. 101.0 Section 101.0 Customs Duties U.S. CUSTOMS AND BORDER PROTECTION, DEPARTMENT OF HOMELAND SECURITY; DEPARTMENT OF THE TREASURY GENERAL PROVISIONS § 101.0 Scope. This part sets forth general regulations governing the authority of Customs...

Activation of the IFMIF prototype accelerator and beam dump by deuterons and protons

Czech Academy of Sciences Publication Activity Database

Simakov, S. P.; Bém, Pavel; Burjan, Václav; Fischer, U.; Forrest, R.A.; Götz, Miloslav; Honusek, Milan; Klein, H.; Kroha, Václav; Novák, Jan; Sauer, A.; Šimečková, Eva; Tiede, R.

2008-01-01

Roč. 83, 10-12 (2008), s. 1543-1547 ISSN 0920-3796 R&D Projects: GA MPO 2A-1TP1/101 Institutional research plan: CEZ:AV0Z10480505 Keywords : IFMIF * Protons and deuterons accelerator * Beam dump Subject RIV: BG - Nuclear, Atomic and Molecular Physics, Colliders Impact factor: 0.828, year: 2008

Hormones and β-Agonists

NARCIS (Netherlands)

Ginkel, van L.A.; Bovee, T.F.H.; Blokland, M.H.; Sterk, S.S.; Smits, N.G.E.; Pleadin, Jelka; Vulić, Ana

2016-01-01

This chapter provides some updated information on contemporary methods for hormone and β-agonist analyses. It deals with the classical approaches for the effective detection and identification of exogenous hormones. The chapter examines specific problems related to control strategies for natural

29 CFR 101.7 - Settlements.

Science.gov (United States)

2010-07-01

... 29 Labor 2 2010-07-01 2010-07-01 false Settlements. 101.7 Section 101.7 Labor Regulations Relating... Section 10 (a) to (i) of the Act and Telegraph Merger Act Cases § 101.7 Settlements. Before any complaint... for the submission and consideration of facts, argument, offers of settlement, or proposals of...

7 CFR 1280.101 - Act.

Science.gov (United States)

2010-01-01

... 7 Agriculture 10 2010-01-01 2010-01-01 false Act. 1280.101 Section 1280.101 Agriculture... INFORMATION ORDER Lamb Promotion, Research, and Information Order Definitions § 1280.101 Act. Act means the Commodity Promotion, Research, and Information Act of 1996 (7 U.S.C. 7411-7425; Pub. L. 104-127; 110 Stat...

12 CFR 410.101 - Purpose.

Science.gov (United States)

2010-01-01

... 12 Banks and Banking 4 2010-01-01 2010-01-01 false Purpose. 410.101 Section 410.101 Banks and Banking EXPORT-IMPORT BANK OF THE UNITED STATES ENFORCEMENT OF NONDISCRIMINATION ON THE BASIS OF HANDICAP IN PROGRAMS OR ACTIVITIES CONDUCTED BY EXPORT-IMPORT BANK OF THE UNITED STATES § 410.101 Purpose...

23 CFR 710.101 - Purpose.

Science.gov (United States)

2010-04-01

... 23 Highways 1 2010-04-01 2010-04-01 false Purpose. 710.101 Section 710.101 Highways FEDERAL HIGHWAY ADMINISTRATION, DEPARTMENT OF TRANSPORTATION RIGHT-OF-WAY AND ENVIRONMENT RIGHT-OF-WAY AND REAL ESTATE General § 710.101 Purpose. The primary purpose of the requirements in this part is to ensure the...

27 CFR 10.1 - General.

Science.gov (United States)

2010-04-01

... 27 Alcohol, Tobacco Products and Firearms 1 2010-04-01 2010-04-01 false General. 10.1 Section 10.1... TREASURY LIQUORS COMMERCIAL BRIBERY Scope of Regulations § 10.1 General. The regulations in this part, issued pursuant to section 105 of the Federal Alcohol Administration Act (27 U.S.C. 205), specify...

33 CFR 135.101 - Purpose.

Science.gov (United States)

2010-07-01

... FINANCIAL RESPONSIBILITY AND COMPENSATION OFFSHORE OIL POLLUTION COMPENSATION FUND Levy of Fees § 135.101 Purpose. (a) The purpose of this subpart is to state the general requirements concerning the levy of fees. ... 33 Navigation and Navigable Waters 2 2010-07-01 2010-07-01 false Purpose. 135.101 Section 135.101...

39 CFR 10.1 - Applicability.

Science.gov (United States)

2010-07-01

... 39 Postal Service 1 2010-07-01 2010-07-01 false Applicability. 10.1 Section 10.1 Postal Service UNITED STATES POSTAL SERVICE THE BOARD OF GOVERNORS OF THE U.S. POSTAL SERVICE RULES OF CONDUCT FOR POSTAL SERVICE GOVERNORS (ARTICLE X) § 10.1 Applicability. This part contains rules of conduct for the...

Modification of certain pharmacological effects of ethanol by lipophilic alpha-1 adrenergic agonists

Energy Technology Data Exchange (ETDEWEB)

Menon, M.K.; Dinovo, E.C.; Haddox, V.G.

1987-09-28

The influence of four centrally-acting alpha-1 adrenoceptor agonists, namely, 2(2-chloro-5-trifluoromethylphenylimino) imidazolidine (St 587), cirazoline, (-) 1,2,3,4-tetrahydro-8-methoxy-5-methylthio-2-naphthalenamine ((-)SKF 89748A) and 2-(2-methylindazol-4-imino)imidazolidine (Sgd 101/75) on the pharmacological effects of ethanol was investigated. All four drugs reduced the duration of ethanol-induced hypnosis in C57B1/6 mice, this effect being proportional to their relative potencies to exert central alpha-1 agonism. In prazosin-pretreated mice, St 587 failed to reduce the hypnotic effect of ethanol, which provided strong evidence for the role of alpha-1 agonism for the hypnosis reducing effect of St 587. Hyperactivity induced in C57B1/6 mice by a subhypnotic dose of ethanol and St 587 was reported earlier. In the present study, St 587, cirazoline and (-)SKF 89748A produced similar response, but no correlation between this effect and ethanol hypnosis blockade could be established. 19 references, 8 figures, 2 tables.

29 CFR 101.34 - Hearing.

Science.gov (United States)

2010-07-01

... 29 Labor 2 2010-07-01 2010-07-01 false Hearing. 101.34 Section 101.34 Labor Regulations Relating... Section 10(k) of the Act § 101.34 Hearing. If the parties have not adjusted the dispute or agreed upon methods of voluntary adjustment, a hearing, usually open to the public, is held before a hearing officer...

Unique interaction pattern for a functionally biased ghrelin receptor agonist

DEFF Research Database (Denmark)

Sivertsen, Bjørn Behrens; Lang, Manja; Frimurer, Thomas M.

2011-01-01

Based on the conformationally constrained D-Trp-Phe-D-Trp (wFw) core of the prototype inverse agonist [D-Arg(1),D-Phe(5),D-Trp(7,9),Leu(11)]substance P, a series of novel, small, peptide-mimetic agonists for the ghrelin receptor were generated. By using various simple, ring-constrained spacers...... connecting the D-Trp-Phe-D-Trp motif with the important C-terminal carboxyamide group, 40 nm agonism potency was obtained and also in one case (wFw-Isn-NH(2), where Isn is isonipecotic acid) ~80% efficacy. However, in contrast to all previously reported ghrelin receptor agonists, the piperidine-constrained w......Fw-Isn-NH(2) was found to be a functionally biased agonist. Thus, wFw-Isn-NH(2) mediated potent and efficacious signaling through the Ga(q) and ERK1/2 signaling pathways, but in contrast to all previous ghrelin receptor agonists it did not signal through the serum response element, conceivably the Ga(12...

41 CFR 101-39.101 - Notice of intention to begin a study.

Science.gov (United States)

2010-07-01

... VEHICLES 39-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.1-Establishment, Modification, and Discontinuance of Interagency Fleet Management Systems § 101-39.101 Notice of intention to begin a study. The Administrator, GSA... develop data and justification as to the feasibility of establishing a fleet management system. The...

Niobium Coatings for the HIE-ISOLDE QWR Superconducting Accelerating Cavities

CERN Document Server

Jecklin, N; Delaup, B; Ferreira, L; Mondino, I; Sublet, A; Therasse, M; Venturini Desolaro, W

2013-01-01

The HIE-ISOLDE (High Intensity and Energy at ISOLDE) project is the upgrade of the existing ISOLDE (Isotope Separator On Line DEvice) facility at CERN, which is dedicated to the production of a large variety of radioactive ion beams for nuclear physics experiments. A new linear accelerator made of 20 ȕ=10.3% and 12 ȕ=6.3% quarter-wave resonators (QWR) superconducting (SC) accelerating cavities at 101 MHz will be built, and in a first phase two cryomodules of 5 high-ȕ cavities each are scheduled to accelerate first beams in 2015. The cavities are made of a copper substrate, with a sputter-coated superconductive niobium (Nb) layer, operated at 4.5 K with an accelerating field of 6 MV/m at 10W Radio-Frequency (RF) losses (Q=4.5· 108). In this paper we will discuss the baseline surface treatment and coating procedure which allows obtaining the required performance, as well as the steps undertaken in order to prepare series production of the required number of cavities guaranteeing their quality and functional...

Active sulforhodamine 101 uptake into hippocampal astrocytes.

Directory of Open Access Journals (Sweden)

Christian Schnell

Full Text Available Sulforhodamine 101 (SR101 is widely used as a marker of astrocytes. In this study we investigated labeling of astrocytes by SR101 in acute slices from the ventrolateral medulla and the hippocampus of transgenic mice expressing EGFP under the control of the astrocyte-specific human GFAP promoter. While SR101 efficiently and specifically labeled EGFP-expressing astrocytes in hippocampus, we found that the same staining procedure failed to label astrocytes efficiently in the ventrolateral medulla. Although carbenoxolone is able to decrease the SR101-labeling of astrocytes in the hippocampus, it is unlikely that SR101 is taken up via gap-junction hemichannels because mefloquine, a blocker for pannexin and connexin hemichannels, was unable to prevent SR101-labeling of hippocampal astrocytes. However, SR101-labeling of the hippocampal astrocytes was significantly reduced by substrates of organic anion transport polypeptides, including estron-3-sulfate and dehydroepiandrosterone sulfate, suggesting that SR101 is actively transported into hippocampal astrocytes.

IEEE Std 101-1987: IEEE guide for the statistical analysis of thermal life test data

International Nuclear Information System (INIS)

Anon.

1992-01-01

This revision of IEEE Std 101-1972 describes statistical analyses for data from thermally accelerated aging tests. It explains the basis and use of statistical calculations for an engineer or scientist. Accelerated test procedures usually call for a number of specimens to be aged at each of several temperatures appreciably above normal operating temperatures. High temperatures are chosen to produce specimen failures (according to specified failure criteria) in typically one week to one year. The test objective is to determine the dependence of median life on temperature from the data, and to estimate, by extrapolation, the median life to be expected at service temperature. This guide presents methods for analyzing such data and for comparing test data on different materials

Acceleration of Radiance for Lighting Simulation by Using Parallel Computing with OpenCL

Energy Technology Data Exchange (ETDEWEB)

Zuo, Wangda; McNeil, Andrew; Wetter, Michael; Lee, Eleanor

2011-09-06

We report on the acceleration of annual daylighting simulations for fenestration systems in the Radiance ray-tracing program. The algorithm was optimized to reduce both the redundant data input/output operations and the floating-point operations. To further accelerate the simulation speed, the calculation for matrix multiplications was implemented using parallel computing on a graphics processing unit. We used OpenCL, which is a cross-platform parallel programming language. Numerical experiments show that the combination of the above measures can speed up the annual daylighting simulations 101.7 times or 28.6 times when the sky vector has 146 or 2306 elements, respectively.

Construction Status of the Beamline for Radio-Isotope Production in the Korea Multi-purpose Accelerator Complex

Energy Technology Data Exchange (ETDEWEB)

Chung, B. H.; Yoon, S. P.; Seol, K. T.; Kim, H. S.; Kwon, H. J.; Cho, Y. S. [Korea Atomic Energy Research Institute, Daejeon (Korea, Republic of)

2015-10-15

The 100-MeV beamline consist of 5 target room, a TR 103 as one of these is operating beamline, and a TR 101 as the other beamline is under construction as shown in Fig. 1. The TR 101 as beamline target room will be used for the high value-added medical isotope production and increased utilization of the proton accelerator. The optical system of the beamline consisted of dipole and quadrupole, and it included beam position monitor (BPM) and current transformer (CT) for beam diagnostics. The beamline was inserted into the carbon block and the aluminum collimator, the end of pipe as beam window was used for the aluminum to reduce the radioactive of materials. The target transfer equipment is being installed for RI production. The RI Beamline was aligned using the laser tracker, and vacuum leak was not detected by the helium leak detector. This facility is expected to the high value-added medical isotope production and increased utilization of the proton accelerator.

Metabolic effects of beta2-agonists in relation to exercise performance

DEFF Research Database (Denmark)

Kalsen, Anders

2015-01-01

athletes. The present PhD thesis is based on four manuscripts in which the acute effects of beta2-agonists on exercise performance were investigated. The aims were 1) to investigate whether supratherapeutic inhalation of beta2-agonists enhances muscle strength, anaerobic performance and aerobic performance......, 2) to uncover the mechanisms behind potential beta2-adrenergic improvements in anaerobic performance, 3) to investigate whether inhalation of beta2-agonists is ergogenic in elite athletes with or without airway hyperresponsiveness (AHR). Results from the studies of the thesis show...... administration of a certain dose, but a further increase in dose does not seem to elicit a greater performance-enhancing effect. Moreover, the effects of beta2-agonists on performance are unaffected by training status and AHR, but athletes with AHR who regularly use beta2-agonists get a reduced ergogenic...

PPARα-Independent Arterial Smooth Muscle Relaxant Effects of PPARα Agonists

Directory of Open Access Journals (Sweden)

Neerupma Silswal

2012-01-01

Full Text Available We sought to determine direct vascular effects of peroxisome proliferator-activated receptor alpha (PPARα agonists using isolated mouse aortas and middle cerebral arteries (MCAs. The PPARα agonists GW7647, WY14643, and gemfibrozil acutely relaxed aortas held under isometric tension and dilated pressurized MCAs with the following order of potency: GW7647≫WY14643>gemfibrozil. Responses were endothelium-independent, and the use of PPARα deficient mice demonstrated that responses were also PPARα-independent. Pretreating arteries with high extracellular K+ attenuated PPARα agonist-mediated relaxations in the aorta, but not in the MCA. In the aorta, the ATP sensitive potassium (KATP channel blocker glibenclamide also impaired relaxations whereas the other K+ channel inhibitors, 4-aminopyridine and Iberiotoxin, had no effect. In aortas, GW7647 and WY14643 elevated cGMP levels by stimulating soluble guanylyl cyclase (sGC, and inhibition of sGC with ODQ blunted relaxations to PPARα agonists. In the MCA, dilations were inhibited by the protein kinase C (PKC activator, phorbol 12,13-dibutyrate, and also by ODQ. Our results demonstrated acute, nonreceptor-mediated relaxant effects of PPARα agonists on smooth muscle of mouse arteries. Responses to PPARα agonists in the aorta involved KATP channels and sGC, whereas in the MCA the PKC and sGC pathways also appeared to contribute to the response.

47 CFR 101.4 - Transition plan.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false Transition plan. 101.4 Section 101.4 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) SAFETY AND SPECIAL RADIO SERVICES FIXED MICROWAVE SERVICES Applications and Licenses General Filing Requirements § 101.4 Transition plan. (a) All systems...

Subtype selective kainic acid receptor agonists

DEFF Research Database (Denmark)

Bunch, Lennart; Krogsgaard-Larsen, Povl

2009-01-01

(S)-Glutamic acid (Glu) is the major excitatory neurotransmitter in the mammalian central nervous system, activating the plethora of glutamate receptors (GluRs). In broad lines, the GluRs are divided into two major classes: the ionotropic Glu receptors (iGluRs) and the metabotropic Glu receptors (m......GluRs). Within the iGluRs, five subtypes (KA1, KA2, iGluR5-7) show high affinity and express full agonist activity upon binding of the naturally occurring amino acid kainic acid (KA). Thus these receptors have been named the KA receptors. This review describes all-to our knowledge-published KA receptor agonists...

Heart rate acceleration with GLP-1 receptor agonists in type 2 diabetes patients : an acute and 12-week randomised, double-blind, placebo-controlled trial

NARCIS (Netherlands)

Smits, Mark M; Tonneijck, Lennart; Muskiet, Marcel H A; Hoekstra, T.; Kramer, Mark H H; Diamant, Michaela; van Raalte, Daniël H

OBJECTIVE: To examine mechanisms underlying resting heart rate (RHR) increments of GLP-1 receptor agonists in type 2 diabetes patients. DESIGN: Acute and 12-week randomised, placebo-controlled, double-blind, single-centre, parallel-group trial. METHODS: In total, 57 type 2 diabetes patients

41 CFR 101-4.105 - Definitions.

Science.gov (United States)

2010-07-01

... PROGRAMS OR ACTIVITIES RECEIVING FEDERAL FINANCIAL ASSISTANCE Introduction § 101-4.105 Definitions. As used... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Definitions. 101-4.105 Section 101-4.105 Public Contracts and Property Management Federal Property Management Regulations System...

34 CFR 101.114 - Expeditious treatment.

Science.gov (United States)

2010-07-01

... 34 Education 1 2010-07-01 2010-07-01 false Expeditious treatment. 101.114 Section 101.114 Education Regulations of the Offices of the Department of Education OFFICE FOR CIVIL RIGHTS, DEPARTMENT OF... § 101.114 Expeditious treatment. Requests for expeditious treatment of matters pending before the...

1 CFR 10.1 - Publication required.

Science.gov (United States)

2010-01-01

... 1 General Provisions 1 2010-01-01 2010-01-01 false Publication required. 10.1 Section 10.1 General Provisions ADMINISTRATIVE COMMITTEE OF THE FEDERAL REGISTER SPECIAL EDITIONS OF THE FEDERAL REGISTER PRESIDENTIAL PAPERS Regular Publication § 10.1 Publication required. The Director publishes a special edition...

49 CFR 1503.101 - TSA requirements.

Science.gov (United States)

2010-10-01

... 49 Transportation 9 2010-10-01 2010-10-01 false TSA requirements. 1503.101 Section 1503.101... Scope of Investigative and Enforcement Procedures § 1503.101 TSA requirements. (a) The investigative and enforcement procedures in this part apply to TSA's investigation and enforcement of violations of TSA...

25 CFR 115.101 - Individual accounts.

Science.gov (United States)

2010-04-01

... 25 Indians 1 2010-04-01 2010-04-01 false Individual accounts. 115.101 Section 115.101 Indians BUREAU OF INDIAN AFFAIRS, DEPARTMENT OF THE INTERIOR FINANCIAL ACTIVITIES TRUST FUNDS FOR TRIBES AND INDIVIDUAL INDIANS IIM Accounts § 115.101 Individual accounts. Except as otherwise provided in this part...

41 CFR 101-1.110 - Deviation.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Deviation. 101-1.110 Section 101-1.110 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101-1.110 Deviation...

47 CFR 101.1505 - Segmentation plan.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false Segmentation plan. 101.1505 Section 101.1505 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) SAFETY AND SPECIAL RADIO SERVICES FIXED MICROWAVE SERVICES Service and Technical Rules for the 70/80/90 GHz Bands § 101.1505 Segmentation plan. (a) An entity...

47 CFR 101.129 - Transmitter location.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false Transmitter location. 101.129 Section 101.129... SERVICES Technical Standards § 101.129 Transmitter location. (a) The applicant must determine, prior to... adequate to render the service proposed. In cases of questionable antenna locations, it is desirable to...

Ecdysone Agonist: New Insecticides with Novel Mode of Action

Directory of Open Access Journals (Sweden)

Y. Andi Trisyono

2002-12-01

Full Text Available Development of insect resistance to insecticide has been the major driving force for the development of new insecticides. Awareness and demand from public for more environmentally friendly insecticides have contributed in shifting the trend from using broad spectrum to selective insecticides. As a result, scientists have looked for new target sites beyond the nervous system. Insect growth regulators (IGRs are more selective insecticides than conventional insecticides, and ecdysone agonists are the newest IGRs being commercialized, e.g. tebufenozide, methoxyfenozide, and halofenozide. Ecdysone agonists bind to the ecdysteroid receptors, and they act similarly to the molting hormone 20-hydroxyecdysone. The binding provides larvae or nymphs with a signal to enter a premature and lethal molting cycle. In addition, the ecdysone agonists cause a reduction in the number of eggs laid by female insects. The ecdysone agonists are being developed as selective biorational insecticides. Tebufenozide and methoxyfenozide are used to control lepidopteran insect pests, whereas halofenozide is being used to control coleopteran insect pests. Their selectivity is due to differences in the binding affinity between these compounds to the receptors in insects from different orders. The selectivity of these compounds makes them candidates to be used in combinations with other control strategies to develop integrated pest management programs in agricultural ecosystems. Key words: new insecticides, selectivity, ecdysone agonists

Improving bioactivity of inert bioceramics by a novel Mg-incorporated solution treatment

Science.gov (United States)

Dehestani, Mahdi; Zemlyanov, Dmitry; Adolfsson, Erik; Stanciu, Lia A.

2017-12-01

Zirconia/alumina ceramics possess outstanding mechanical properties for dental and orthopedic applications, but due to their poor surface bioactivities they exhibit a weak bone-bonding ability. This work proposes an effective 30-min solution treatment which could successfully induce formation of bone-like apatite on the surface of 3Y-TZP and a ternary composite composed of yttria-stabilized zirconia, ceria-stabilized zirconia, and alumina (35 vol% 3Y-TZP + 35 vol% 12Ce-TZP + 30 vol% Al2O3) after 3 weeks immersion in simulated body fluid (SBF). XRD was used for phase identification in the ceramic materials. The influence of solution treatment on the surface chemistry and its role on apatite formation were investigated via SEM, EDS and XPS. In vitro apatite-forming ability for the solution-treated and untreated samples of the composite and individual substrates of 3Y-TZP, 12Ce-TZP, and Al2O3 was evaluated by immersion in SBF. Apatite crystals were formed only on 3Y-TZP and composite substrates, implying that it is mainly the 3Y-TZP constituent that contributes to the bioactivity of the composite. Further, it was found from the XPS analysis that the zirconia material with higher phase stability (12Ce-TZP) produced less Zrsbnd OH functional groups on its surface after solution treatment which accounts for its weaker bioactivity compared to 3Y-TZP.

Main: CRC101 [AT Atlas

Lifescience Database Archive (English)

Full Text Available CRC101 CRC1 Establishment of Chemical Library and Development of Protein Regulation... Technology Chemical library Tetsuo Nagano Graduate School of Pharmaceutical Sciences, The University CRC101.csml ...

Growth Hormone Supplementation in the Luteal Phase Before Microdose GnRH Agonist Flare Protocol for In Vitro Fertilization.

Science.gov (United States)

Dunne, Caitlin; Seethram, Ken; Roberts, Jeffrey

2015-09-01

Growth hormone (GH) acts in both early and late follicular development to stimulate the proliferation and differentiation of granulosa cells and to increase the production of estradiol in animal and human ovaries. Investigators have therefore explored GH supplementation to improve outcomes in women undergoing in vitro fertilization, with the greatest interest in women with diminished ovarian reserve. Recent meta-analyses indicate that GH supplementation can be beneficial for poor responders undergoing IVF. In most studies, GH has been given concomitantly with gonadotropins during the follicular phase; this may not be optimal, since follicular recruitment begins during the preceding luteal phase. We therefore wished to examine the effect of GH supplementation in the luteal phase before controlled ovarian stimulation (COH) with a microdose GnRH agonist flare (MDF) protocol in women undergoing in vitro fertilization. We performed a retrospective matched case-control study of patients undergoing treatment at a private IVF facility between June 2012 and July 2013. Patients identified as poor responders to COH were offered adjuvant GH treatment as part of their ovarian stimulation regimen. The patients in the experimental group chose to take GH, 3.33 mg daily by subcutaneous injection for 14 days, before starting COH. All patients had an MDF stimulation protocol using 450 IU of follicle stimulating hormone (FSH) daily. A total of 42 women were included in the study. There were 14 women in the experimental group (GH) and 28 controls (C) matched for age, BMI, and day 3 FSH level. There was no difference between the groups in clinical pregnancy rate (GH = 29%, C = 32%, P = 0.99), number of mature oocytes retrieved (GH = 2.5, C = 5.0, P = 0.13), cycle cancellation rate (GH = 21%, C = 14%, P = 0.88), duration of COH (GH = 10.1, C = 10.1, P = 0.93), or mean peak estradiol level (GH = 4174 pmol/L, C = 5105 pmol/L, P = 0.44). The administration of growth hormone during the

47 CFR 101.141 - Microwave modulation.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false Microwave modulation. 101.141 Section 101.141... SERVICES Technical Standards § 101.141 Microwave modulation. (a) Microwave transmitters employing digital modulation techniques and operating below 25.25 GHz (except for MVDDS stations in the 12,200-12,700 MHz band...

47 CFR 101.807 - Transmitter power.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false Transmitter power. 101.807 Section 101.807... SERVICES Local Television Transmission Service § 101.807 Transmitter power. Stations in this service will not be authorized to use transmitters having a rated power output in excess of the limits set forth in...

47 CFR 101.1525 - RF safety.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false RF safety. 101.1525 Section 101.1525 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) SAFETY AND SPECIAL RADIO SERVICES FIXED MICROWAVE SERVICES Service and Technical Rules for the 70/80/90 GHz Bands § 101.1525 RF safety. Licensees in the 70...

29 CFR 1926.101 - Hearing protection.

Science.gov (United States)

2010-07-01

... 29 Labor 8 2010-07-01 2010-07-01 false Hearing protection. 1926.101 Section 1926.101 Labor Regulations Relating to Labor (Continued) OCCUPATIONAL SAFETY AND HEALTH ADMINISTRATION, DEPARTMENT OF LABOR... § 1926.101 Hearing protection. (a) Wherever it is not feasible to reduce the noise levels or duration of...

7 CFR 1435.101 - Loan rates.

Science.gov (United States)

2010-01-01

... 7 Agriculture 10 2010-01-01 2010-01-01 false Loan rates. 1435.101 Section 1435.101 Agriculture... AGRICULTURE LOANS, PURCHASES, AND OTHER OPERATIONS SUGAR PROGRAM Sugar Loan Program § 1435.101 Loan rates. (a) The national average loan rate for raw cane sugar produced from domestically grown sugarcane is: 18...

22 CFR 1203.735-101 - Purpose.

Science.gov (United States)

2010-04-01

... CONDUCT General Provisions § 1203.735-101 Purpose. The maintenance of the highest standards of honesty... reporting employment and financial interests. Note: These regulations are codified in State 3 FAM 620, AID... 22 Foreign Relations 2 2010-04-01 2010-04-01 true Purpose. 1203.735-101 Section 1203.735-101...

49 CFR 374.101 - Discrimination prohibited.

Science.gov (United States)

2010-10-01

... 49 Transportation 5 2010-10-01 2010-10-01 false Discrimination prohibited. 374.101 Section 374.101... REGULATIONS Discrimination in Operations of Interstate Motor Common Carriers of Passengers § 374.101 Discrimination prohibited. No motor common carrier of passengers subject to 49 U.S.C. subtitle IV, part B shall...

19 CFR 101.7 - Customs seal.

Science.gov (United States)

2010-04-01

... 19 Customs Duties 1 2010-04-01 2010-04-01 false Customs seal. 101.7 Section 101.7 Customs Duties U.S. CUSTOMS AND BORDER PROTECTION, DEPARTMENT OF HOMELAND SECURITY; DEPARTMENT OF THE TREASURY GENERAL PROVISIONS § 101.7 Customs seal. (a) Design. According to the design furnished by the Department...

19 CFR 10.101 - Immediate delivery.

Science.gov (United States)

2010-04-01

... 19 Customs Duties 1 2010-04-01 2010-04-01 false Immediate delivery. 10.101 Section 10.101 Customs... Importations § 10.101 Immediate delivery. (a) Shipments entitled to immediate delivery. Shipments consigned to... as shipments the immediate delivery of which is necessary within the purview of section 448(b...

Synthesis and Characterization of Reduced Graphene Oxide/Rhodamine 101 (rGO-Rh101) Nanocomposites and Their Heterojunction Performance in rGO-Rh101/ p-Si Device Configuration

Science.gov (United States)

Batır, G. Güven; Arık, Mustafa; Caldıran, Zakir; Turut, Abdulmecit; Aydogan, Sakir

2018-01-01

Reduced graphene oxide (rGO)-rhodamine 101 (Rh101) nanocomposites with different ratios of rGO have been synthesized in aqueous medium by ultrasonic homogenization. The fluorescence of Rh101 as measured using a laser dye with high fluorescence quantum yield was substantially quenched with increasing amount of rGO in the nanocomposite. Formation of rGO-Rh101 nanocomposites was confirmed by x-ray diffraction analysis, scanning electron microscopy, ultraviolet-visible (UV-Vis) spectroscopy, and fluorescence microscopy. Furthermore, rGO-Rh101 nanocomposite/ p-Si heterojunctions were synthesized, all of which showed good rectifying behavior. The electrical characteristics of these devices were analyzed using current-voltage ( I- V) measurements to determine the ideality factor and barrier height. The experimental results confirmed the presence of lateral inhomogeneity in the effective barrier height of the rGO-Rh101 nanocomposite/ p-Si heterojunctions. In addition to I- V measurements, one device was analyzed in more detail using frequency-dependent capacitance-voltage measurements. All electrical measurements were carried out at room temperature and in the dark.

Reconstitution of high-affinity opioid agonist binding in brain membranes

Energy Technology Data Exchange (ETDEWEB)

Remmers, A.E.; Medzihradsky, F. (Univ. of Michigan Medical School, Ann Arbor (United States))

1991-03-15

In synaptosomal membranes from rat brain cortex, the {mu} selective agonist ({sup 3}H)dihydromorphine in the absence of sodium, and the nonselective antagonist ({sup 3}H)naltrexone in the presence of sodium, bound to two populations of opioid receptor sites with K{sub d} values of 0.69 and 8.7 nM for dihydromorphine, and 0.34 and 5.5 nM for naltrexone. The addition of 5 {mu}M guanosine 5{prime}-({gamma}-thio)triphosphate (GTP({gamma}S)) strongly reduced high-affinity agonist but not antagonist binding. Exposure of the membranes to high pH reduced the number of GTP({gamma}-{sup 35}S) binding sites by 90% and low K{sub m}, opioid-sensitive GTPase activity by 95%. In these membranes, high-affinity agonist binding was abolished and modulation of residual binding by GTP({gamma}S) was diminished. Alkali treatment of the glioma cell membranes prior to fusion inhibited most of the low K{sub m} GTPase activity and prevented the reconstitution of agonist binding. The results show that high-affinity opioid agonist binding reflects the ligand-occupied receptor - guanine nucleotide binding protein complex.

48 CFR 804.101 - Contracting officer's signature.

Science.gov (United States)

2010-10-01

... signature. 804.101 Section 804.101 Federal Acquisition Regulations System DEPARTMENT OF VETERANS AFFAIRS GENERAL ADMINISTRATIVE MATTERS Contract Execution 804.101 Contracting officer's signature. (a) If a... signature. ...

Hypertrophic effect of inhaled beta -agonist with and without concurrent exercise training

DEFF Research Database (Denmark)

Jessen, Søren; Onslev, Johan; Lemminger, Anders

2018-01-01

INTRODUCTION: Due to a high prevalence of asthma and exercise-induced bronchoconstriction in elite athletes, there is a high use of beta2 -adrenoceptor agonists (beta2 -agonists) in the athletic population. While anabolic in rodents, no study has been able to detect hypertrophy in humans after...... chronic beta2 -agonist inhalation. METHODS: We investigated if inhaled beta2 -agonist, terbutaline, alters body composition and metabolic rate with and without concurrent exercise training in healthy young men. Sixty-seven participants completed a four-week intervention of daily terbutaline (8×0.5 mg...

29 CFR 541.101 - Business owner.

Science.gov (United States)

2010-07-01

... 29 Labor 3 2010-07-01 2010-07-01 false Business owner. 541.101 Section 541.101 Labor Regulations... Executive Employees § 541.101 Business owner. The term “employee employed in a bona fide executive capacity... equity interest in the enterprise in which the employee is employed, regardless of whether the business...

36 CFR 10.1 - Animals available.

Science.gov (United States)

2010-07-01

... 36 Parks, Forests, and Public Property 1 2010-07-01 2010-07-01 false Animals available. 10.1 Section 10.1 Parks, Forests, and Public Property NATIONAL PARK SERVICE, DEPARTMENT OF THE INTERIOR DISPOSAL OF CERTAIN WILD ANIMALS § 10.1 Animals available. From time to time there are surplus live elk...

9 CFR 101.6 - Cell cultures.

Science.gov (United States)

2010-01-01

... 9 Animals and Animal Products 1 2010-01-01 2010-01-01 false Cell cultures. 101.6 Section 101.6..., SERUMS, TOXINS, AND ANALOGOUS PRODUCTS; ORGANISMS AND VECTORS DEFINITIONS § 101.6 Cell cultures. When used in conjunction with or in reference to cell cultures, which may be referred to as tissue cultures...

Regulation of ventilation and oxygen consumption by delta- and mu-opioid receptor agonists.

Science.gov (United States)

Schaeffer, J I; Haddad, G G

1985-09-01

To study the effect of endorphins on metabolic rate and on the relationship between O2 consumption (VO2) and ventilation, we administered enkephalin analogues (relatively selective delta-receptor agonists) and a morphiceptin analogue (a highly selective mu-receptor agonist) intracisternally in nine unanesthetized chronically instrumented adult dogs. Both delta- and mu-agonists decreased VO2 by 40-60%. delta-Agonists induced a dose-dependent decrease in mean instantaneous minute ventilation (VT/TT) associated with periodic breathing. The decrease in VT/TT started and resolved prior to the decrease and returned to baseline of VO2, respectively. In contrast, the mu-agonists induced an increase in VT/TT associated with rapid shallow breathing. Arterial PCO2 increased and arterial PO2 decreased after both delta- and mu-agonists. Low doses of intracisternal naloxone (0.002-2.0 micrograms/kg) reversed the opioid effect on VT/TT but not on VO2; higher doses of naloxone (5-25 micrograms/kg) reversed both. Naloxone administered alone had no effect on VT/TT or VO2. These data suggest that 1) both delta- and mu-agonists induce alveolar hypoventilation despite a decrease in VO2, 2) this hypoventilation results from a decrease in VT/TT after delta-agonists but an increase in dead space ventilation after mu-agonists, and 3) endorphins do not modulate ventilation and metabolic rate tonically, but we speculate that they may do so in response to stressful stimulation.

FXR agonist activity of conformationally constrained analogs of GW 4064.

Science.gov (United States)

Akwabi-Ameyaw, Adwoa; Bass, Jonathan Y; Caldwell, Richard D; Caravella, Justin A; Chen, Lihong; Creech, Katrina L; Deaton, David N; Madauss, Kevin P; Marr, Harry B; McFadyen, Robert B; Miller, Aaron B; Navas, Frank; Parks, Derek J; Spearing, Paul K; Todd, Dan; Williams, Shawn P; Bruce Wisely, G

2009-08-15

Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2g.

42 CFR 55a.101 - Definitions.

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2010-10-01

... 42 Public Health 1 2010-10-01 2010-10-01 false Definitions. 55a.101 Section 55a.101 Public Health PUBLIC HEALTH SERVICE, DEPARTMENT OF HEALTH AND HUMAN SERVICES GRANTS PROGRAM GRANTS FOR BLACK LUNG CLINICS General Provisions § 55a.101 Definitions. Act, as used in this part, means the Federal Mine Safety...

7 CFR 1400.101 - Minor children.

Science.gov (United States)

2010-01-01

... 7 Agriculture 10 2010-01-01 2010-01-01 false Minor children. 1400.101 Section 1400.101 Agriculture... SUBSEQUENT CROP, PROGRAM, OR FISCAL YEARS Payment Limitation § 1400.101 Minor children. (a) Except as provided in paragraph (b) of this section, payments received by a child under 18 years of age as of April 1...

Characteristics of a cartridge NEG (St101 Zr-Al)

International Nuclear Information System (INIS)

Hisamatsu, Hiromi; Shimamoto, Masayuki; Kanazawa, Ken-ichi; Ishimaru, Hajime

1990-01-01

The report addresses the application of a non-evaporable getter (NEG) pump to an accelerator (storage ring). Tests are performed to determine major characteristics of the non-evaporable getter pump in an effort to provide a method for its efficient use. Test results show that with an St101 cartridge NEG pump, it is possible to produce an ultrahigh vacuum in a system with a surface area of about 10 4 cm 2 through baking at 410K for two hours. Once activated at 1000K, a NEG pump recovers a pumping performance in a subsequent test run at 723K, though the pumping speed decreases by several tens of percent. The St-101 cartridge type NEG pump is at least 2 Pam 3 in pumping capacity for carbon monoxide. The pumping speed decreases with an increasing amount of occluded carbon monoxide. Upon activation, most of the occluded carbon monoxide diffuses into the pump while only little of it is released into the gas phase. Its diffusion through the surface of the NEG pump can occur even at room temperature, indicating that if a leak takes place, the pump would absorb the gas continuously. Thus, if a leak occurs during activation, the pump would occlude a large amount of gas and therefore, activation should be carried out with careful checking for a leak. (N.K.)

MELATONIN DAN MELATONIN RECEPTOR AGONIST SEBAGAI PENANGANAN INSOMNIA PRIMER KRONIS

Directory of Open Access Journals (Sweden)

Ni Luh Putu Ayu Maha Iswari

2013-04-01

Full Text Available Melatonin is a hormone that has an important role in the mechanism of sleep. Hypnotic effects of melatonin and melatonin receptor agonist are mediated via MT1 and MT2 receptors, especially in circadian rhythm pacemaker, suprachiasmatic nucleus, which is worked on the hypothalamic sleep switch. This mechanism is quite different with the GABAergic drugs such as benzodiazepine. Agonist melatonin triggers the initiation of sleep and normalize circadian rhythms so that makes it easier to maintain sleep. The main disadvantage of melatonin in helping sleep maintenance on primary insomnia is that the half life is very short. The solution to this problem is the use of prolonged-release melatonin and melatonin receptor agonist agents such as ramelteon. Melatoninergic agonist does not cause withdrawal effects, dependence, as well as cognitive and psychomotor disorders as often happens on the use of benzodiazepine.  

Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists

DEFF Research Database (Denmark)

Palmer, Daniel; Gonçalves, Juliana P.L.; Hansen, Louise V.

2017-01-01

The melanocortin receptor 4 (MC4R) subtype of the melanocortin receptor family is a target for therapeutics to ameliorate metabolic dysfunction. Endogenous MC4R agonists possess a critical pharmacophore (HFRW), and cyclization of peptide agonists often enhances potency. Thus, 17 cyclized peptides...

Rat Urinary Bladder Carcinogenesis by Dual-Acting PPARα+γ Agonists

Directory of Open Access Journals (Sweden)

Martin B. Oleksiewicz

2008-01-01

Full Text Available Despite clinical promise, dual-acting activators of PPARα and γ (here termed PPARα+γ agonists have experienced high attrition rates in preclinical and early clinical development, due to toxicity. In some cases, discontinuation was due to carcinogenic effect in the rat urothelium, the epithelial layer lining the urinary bladder, ureters, and kidney pelvis. Chronic pharmacological activation of PPARα is invariably associated with cancer in rats and mice. Chronic pharmacological activation of PPARγ can in some cases also cause cancer in rats and mice. Urothelial cells coexpress PPARα as well as PPARγ, making it plausible that the urothelial carcinogenicity of PPARα+γ agonists may be caused by receptor-mediated effects (exaggerated pharmacology. Based on previously published mode of action data for the PPARα+γ agonist ragaglitazar, and the available literature about the role of PPARα and γ in rodent carcinogenesis, we propose a mode of action hypothesis for the carcinogenic effect of PPARα+γ agonists in the rat urothelium, which combines receptor-mediated and off-target cytotoxic effects. The proposed mode of action hypothesis is being explored in our laboratories, towards understanding the human relevance of the rat cancer findings, and developing rapid in vitro or short-term in vivo screening approaches to faciliate development of new dual-acting PPAR agonist compounds.

Identification of novel selective V2 receptor non-peptide agonists.

Science.gov (United States)

Del Tredici, Andria L; Vanover, Kim E; Knapp, Anne E; Bertozzi, Sine M; Nash, Norman R; Burstein, Ethan S; Lameh, Jelveh; Currier, Erika A; Davis, Robert E; Brann, Mark R; Mohell, Nina; Olsson, Roger; Piu, Fabrice

2008-10-30

Peptides with agonist activity at the vasopressin V(2) receptor are used clinically to treat fluid homeostasis disorders such as polyuria and central diabetes insipidus. Of these peptides, the most commonly used is desmopressin, which displays poor bioavailability as well as potent activity at the V(1b) receptor, with possible stress-related adverse effects. Thus, there is a strong need for the development of small molecule chemistries with selective V(2) receptor agonist activity. Using the functional cell-based assay Receptor Selection and Amplification Technology (R-SAT((R))), a screening effort identified three small molecule chemotypes (AC-94544, AC-88324, and AC-110484) with selective agonist activity at the V(2) receptor. One of these compounds, AC-94544, displayed over 180-fold selectivity at the V(2) receptor compared to related vasopressin and oxytocin receptors and no activity at 28 other G protein-coupled receptors (GPCRs). All three compounds also showed partial agonist activity at the V(2) receptor in a cAMP accumulation assay. In addition, in a rat model of central diabetes insipidus, AC-94544 was able to significantly reduce urine output in a dose-dependent manner. Thus, AC-94544, AC-88324, and AC-110484 represent novel opportunities for the treatment of disorders associated with V(2) receptor agonist deficiency.

Effect of Alumina Addition to Zirconia Nano-composite on Low Temperature Degradation Process and Biaxial Strength

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Moluk Aivazi

2016-12-01

Full Text Available Ceramic dental materials have been considered as alternatives to metals for dental implants application. In this respect, zirconia tetragonal stabilized with %3 yttrium, is of great importance among the ceramic materials for endosseous dental implant application. Because of its good mechanical properties and color similar to tooth. The aim and novelty of this study was to design and prepare Y-TZP nano-composite to reduce the degradation process at low temperature by alumina addition and maintaining submicron grain sized. Also, flexural strength of nano-composite samples was evaluated. Toward this purpose, alumina-Y-TZP nano-composites containing 0–30 vol% alumina (denoted as A-Y-TZP 0-30 were fabricated using α-alumina and Y-TZP nano-sized by sintering pressure less method. The synthesized samples were characterized using x-ray diffraction, field emission scanning electron microscopy equipped with energy dispersive x-ray spectroscopy techniques. Nano-composite samples with high density (≥96% and grain sized of ≤ 400 nm was obtained by sintering at 1270 °C for 170 min. After low temperature degradation test (LTD, A-Y-TZP20 and A-Y-TZP30 not showed monoclinic phase and the flexural strength in all of samples were higher than A-Y-TZP0. It was concluded that the grains were remained in submicron sized and A-Y-TZP20 and A-Y-TZP30 did not present biaxial strength reduction after LTD test.

Principles of agonist recognition in Cys-loop receptors

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Timothy eLynagh

2014-04-01

Full Text Available Cys-loop receptors are ligand-gated ion channels that are activated by a structurally diverse array of neurotransmitters, including acetylcholine, serotonin, glycine and GABA. After the term chemoreceptor emerged over 100 years ago, there was some wait until affinity labeling, molecular cloning, functional studies and X-ray crystallography experiments identified the extracellular interface of adjacent subunits as the principal site of agonist binding. The question of how subtle differences at and around agonist-binding sites of different Cys-loop receptors can accommodate transmitters as chemically diverse as glycine and serotonin has been subject to intense research over the last three decades. This review outlines the functional diversity and current structural understanding of agonist-binding sites, including those of invertebrate Cys-loop receptors. Together, this provides a framework to understand the atomic determinants involved in how these valuable therapeutic targets recognize and bind their ligands.

Cyclic fatigue resistance of yttria-stabilized tetragonal zirconia polycrystals with hot isostatic press processing.

Science.gov (United States)

Koyama, Taku; Sato, Toru; Yoshinari, Masao

2012-01-01

This study investigated the influence of surface roughness and cyclic loading on fatigue resistance in Y-TZP subjected to hot isostatic pressing (HIP). Fifty Y-TZP cylinders 3.0 mm in diameter were divided into Group A (polished by centerless method; TZP-CP) or Group B (blasted and acid-etched: TZP-SB150E). Twenty five cp-titanium cylinders (Ti-SB150E) were used as a control. Static and cyclic tests were carried out according to ISO 14801. The cyclic fatigue test was performed in distilled water at 37°C. Surface morphology and roughness as well as crystal phase on the surfaces were also evaluated. Fracture force under the static test was 1,765N (TZP-CP), 1,220N (TZP-SB150E), and 850 N (yield force, Ti-SB150E). Fracture values under the cyclic test decreased to approximately 70% of those under the static tests. These results indicate that HIPed Y-TZP with a 3.0-mm diameter has sufficient durability for application to dental implants.

PROCESSING OF CONCENTRATED AQUEOUS ZIRCONIA-BIOGLASS SLIPS BY SLIP CASTING

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Beltina Leon

2017-03-01

Full Text Available 3 mol% yttria-partially stabilized zirconia (Y-TZP powder and a sol-gel derived CaO- P₂O₅- SiO₂ (64S bioglass, were used to produce Y-TZP- bioglass slip cast compacts. The rheological properties of concentrated aqueous Y-TZP- 64S suspensions prepared with two different glass contents: 10.5 vol% and 19.9 vol%, and ammonium polyacrylate (NH₄PA as dispersant, were investigated and compared with those of Y-TZP. The density of green cast samples was related to the degree of slip dispersion. The substitution of Y-TZP by 64S glass in the mixtures resulted in greater adsorption of NH₄PA; however, the viscosity and yield stress values of Y-TZP-64S slips were higher than those of Y-TZP ones for the solid loadings studied. The increase in the glass content from 10.5 to 19.9 vol% increased the viscosity and yield stress values. The presence of 64S glass in the mixtures resulted in a less dense packing of cast samples.

Partial agonist therapy in schizophrenia: relevance to diminished criminal responsibility.

Science.gov (United States)

Gavaudan, Gilles; Magalon, David; Cohen, Julien; Lançon, Christophe; Léonetti, Georges; Pélissier-Alicot, Anne-Laure

2010-11-01

Pathological gambling (PG), classified in the DSM-IV among impulse control disorders, is defined as inappropriate, persistent gaming for money with serious personal, family, and social consequences. Offenses are frequently committed to obtain money for gambling. Pathological gambling, a planned and structured behavioral disorder, has often been described as a complication of dopamine agonist treatment in patients with Parkinson's disease. It has never been described in patients with schizophrenia receiving dopamine agonists. We present two patients with schizophrenia, previously treated with antipsychotic drugs without any suggestion of PG, who a short time after starting aripiprazole, a dopamine partial agonist, developed PG and criminal behavior, which totally resolved when aripiprazole was discontinued. Based on recent advances in research on PG and adverse drug reactions to dopamine agonists in Parkinson's disease, we postulate a link between aripiprazole and PG in both our patients with schizophrenia and raise the question of criminal responsibility. © 2010 American Academy of Forensic Sciences.

Effect of in vitro aging on the flexural strength and probability to fracture of Y-TZP zirconia ceramics for all-ceramic restorations.

Science.gov (United States)

Siarampi, Eleni; Kontonasaki, Eleana; Andrikopoulos, Konstantinos S; Kantiranis, Nikolaos; Voyiatzis, George A; Zorba, Triantafillia; Paraskevopoulos, Konstantinos M; Koidis, Petros

2014-12-01

Dental zirconia restorations should present long-term clinical survival and be in service within the oral environment for many years. However, low temperature degradation could affect their mechanical properties and survival. The aim of this study was to investigate the effect of in vitro aging on the flexural strength of yttrium-stabilized (Y-TZP) zirconia ceramics for ceramic restorations. One hundred twenty bar-shaped specimens were prepared from two ceramics (ZENO Zr (WI) and IPS e.max(®) ZirCAD (IV)), and loaded until fracture according to ISO 6872. The specimens from each ceramic (nx=60) were divided in three groups (control, aged for 5h, aged for 10h). One-way ANOVA was used to assess statistically significant differences among flexural strength values (Pceramics, however statistically significant was for the WI group (Pceramics presented a t→m phase transformation, with the m-phase increasing from 4 to 5% at 5h to around 15% after 10h. The significant reduction of the flexural strength after 10h of in vitro aging, suggests high fracture probability for one of the zirconia ceramics tested. Copyright © 2014 Academy of Dental Materials. Published by Elsevier Ltd. All rights reserved.

5 CFR 2604.101 - Purpose.

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2010-01-01

... AND SCHEDULE OF FEES FOR THE PRODUCTION OF PUBLIC FINANCIAL DISCLOSURE REPORTS General Provisions... reproduction and mailing of public financial disclosure reports requested by any person. ... 5 Administrative Personnel 3 2010-01-01 2010-01-01 false Purpose. 2604.101 Section 2604.101...

48 CFR 3433.101 - Definitions.

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2010-10-01

... GENERAL CONTRACTING REQUIREMENTS PROTESTS, DISPUTES, AND APPEALS Protests 3433.101 Definitions. Filed, as... Accounting Office (GAO), or the General Services Administration Board of Contract Appeals (GSBCA). ... 48 Federal Acquisition Regulations System 7 2010-10-01 2010-10-01 false Definitions. 3433.101...

Small-molecule agonists for the glucagon-like peptide 1 receptor

DEFF Research Database (Denmark)

Knudsen, Lotte Bjerre; Kiel, Dan; Teng, Min

2007-01-01

and independent agonists. Potency of GLP-1 was not changed by the allosteric agonists, but affinity of GLP-1 for the receptor was increased. The most potent compound identified stimulates glucose-dependent insulin release from normal mouse islets but, importantly, not from GLP-1 receptor knockout mice. Also...

48 CFR 4.101 - Contracting officer's signature.

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2010-10-01

... 48 Federal Acquisition Regulations System 1 2010-10-01 2010-10-01 false Contracting officer's signature. 4.101 Section 4.101 Federal Acquisition Regulations System FEDERAL ACQUISITION REGULATION GENERAL ADMINISTRATIVE MATTERS Contract Execution 4.101 Contracting officer's signature. Only contracting officers shall...

3 CFR 101.4 - National Security Council.

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2010-01-01

... 3 The President 1 2010-01-01 2010-01-01 false National Security Council. 101.4 Section 101.4... PROCEDURES ACT § 101.4 National Security Council. Freedom of Information regulations for the National Security Council appear at 32 CFR Ch. XXI. ...

Performance of metal-organic framework MIL-101 after surfactant modification in the extraction of endocrine disrupting chemicals from environmental water samples.

Science.gov (United States)

Huang, Zhenzhen; Lee, Hian Kee

2015-10-01

The research presented in this paper explored the modification and application of a metal-organic framework, MIL-101, with nonionic surfactant-Triton X-114 in dispersive solid-phase extraction for the preconcentration of four endocrine disrupting chemicals (estrone, 17α-ethynylestradiol, estriol and diethylstilbestrol) from environmental water samples. Triton X-114 molecules could be adsorbed by the hydrophobic surface of the MIL-101 crystals, and thus improved the dispersibility of MIL-101 in aqueous solution by serving as a hydrophilic coating. Cloud point phase separation from Triton X-114 accelerated the separation of extracts from the aqueous matrix. The proposed method combines the favorable attributes of strong adsorption capacity resulting from the porous structure of MIL-101 and self-assembly of Triton X-114 molecules. Post-extraction derivatization using N-methyl-N-(trimethylsilyl)trifluoroacetamide was employed to facilitate the quantitative determination of the extracts by gas chromatography-mass spectrometry. The main factors affecting the preparation of modified MIL-101, and extraction of the analytes, such as the amount of surfactant, the ultrasonic and vortex durations, solution pH and desorption conditions, were investigated in detail. Under the optimized conditions, the present method yielded low limits of detection (0.006-0.023 ng/mL), good linearity from 0.09 to 45 ng/mL (coefficients of determination higher than 0.9980) and acceptable precision (relative standard deviations of 2.2-13%). The surface modified MIL-101 was demonstrated to be effective for the extraction of the selected estrogens from aqueous samples, giving rise to markedly improved extraction performance compared to the unmodified MIL-101. Copyright © 2015 Elsevier B.V. All rights reserved.

Effect of beta-agonists on LAM progression and treatment.

Science.gov (United States)

Le, Kang; Steagall, Wendy K; Stylianou, Mario; Pacheco-Rodriguez, Gustavo; Darling, Thomas N; Vaughan, Martha; Moss, Joel

2018-01-30

Lymphangioleiomyomatosis (LAM), a rare disease of women, is associated with cystic lung destruction resulting from the proliferation of abnormal smooth muscle-like LAM cells with mutations in the tuberous sclerosis complex (TSC) genes TSC1 and/or TSC2 The mutant genes and encoded proteins are responsible for activation of the mechanistic target of rapamycin (mTOR), which is inhibited by sirolimus (rapamycin), a drug used to treat LAM. Patients who have LAM may also be treated with bronchodilators for asthma-like symptoms due to LAM. We observed stabilization of forced expiratory volume in 1 s over time in patients receiving sirolimus and long-acting beta-agonists with short-acting rescue inhalers compared with patients receiving only sirolimus. Because beta-agonists increase cAMP and PKA activity, we investigated effects of PKA activation on the mTOR pathway. Human skin TSC2 +/- fibroblasts or LAM lung cells incubated short-term with isoproterenol (beta-agonist) showed a sirolimus-independent increase in phosphorylation of S6, a downstream effector of the mTOR pathway, and increased cell growth. Cells incubated long-term with isoproterenol, which may lead to beta-adrenergic receptor desensitization, did not show increased S6 phosphorylation. Inhibition of PKA blocked the isoproterenol effect on S6 phosphorylation. Thus, activation of PKA by beta-agonists increased phospho-S6 independent of mTOR, an effect abrogated by beta-agonist-driven receptor desensitization. In agreement, retrospective clinical data from patients with LAM suggested that a combination of bronchodilators in conjunction with sirolimus may be preferable to sirolimus alone for stabilization of pulmonary function.

14 CFR 1264.101 - Definitions.

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2010-01-01

... 14 Aeronautics and Space 5 2010-01-01 2010-01-01 false Definitions. 1264.101 Section 1264.101 Aeronautics and Space NATIONAL AERONAUTICS AND SPACE ADMINISTRATION IMPLEMENTATION OF THE PROGRAM FRAUD CIVIL... representation, certification, affirmation, document, record, or accounting or bookkeeping entry made— (1) With...

40 CFR 97.101 - Purpose.

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2010-07-01

... 40 Protection of Environment 20 2010-07-01 2010-07-01 false Purpose. 97.101 Section 97.101 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) AIR PROGRAMS (CONTINUED) FEDERAL NOX... chapter, as a means of mitigating interstate transport of fine particulates and nitrogen oxides. ...

48 CFR 204.101 - Contracting officer's signature.

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2010-10-01

... 48 Federal Acquisition Regulations System 3 2010-10-01 2010-10-01 false Contracting officer's signature. 204.101 Section 204.101 Federal Acquisition Regulations System DEFENSE ACQUISITION REGULATIONS... officer's signature. Follow the procedures at PGI 204.101 for signature of contract documents. [71 FR 9268...

41 CFR 101-6.204 - Discrimination prohibited.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Discrimination prohibited. 101-6.204 Section 101-6.204 Public Contracts and Property Management Federal Property Management...-Nondiscrimination in Programs Receiving Federal Financial Assistance § 101-6.204 Discrimination prohibited. ...

DSP accelerator for the wavelet compression/decompression of high- resolution images

Energy Technology Data Exchange (ETDEWEB)

Hunt, M.A.; Gleason, S.S.; Jatko, W.B.

1993-07-23

A Texas Instruments (TI) TMS320C30-based S-Bus digital signal processing (DSP) module was used to accelerate a wavelet-based compression and decompression algorithm applied to high-resolution fingerprint images. The law enforcement community, together with the National Institute of Standards and Technology (NISI), is adopting a standard based on the wavelet transform for the compression, transmission, and decompression of scanned fingerprint images. A two-dimensional wavelet transform of the input image is computed. Then spatial/frequency regions are automatically analyzed for information content and quantized for subsequent Huffman encoding. Compression ratios range from 10:1 to 30:1 while maintaining the level of image quality necessary for identification. Several prototype systems were developed using SUN SPARCstation 2 with a 1280 {times} 1024 8-bit display, 64-Mbyte random access memory (RAM), Tiber distributed data interface (FDDI), and Spirit-30 S-Bus DSP-accelerators from Sonitech. The final implementation of the DSP-accelerated algorithm performed the compression or decompression operation in 3.5 s per print. Further increases in system throughput were obtained by adding several DSP accelerators operating in parallel.

Chronic stress accelerates the development of endometriosis in mouse through adrenergic receptor β2.

Science.gov (United States)

Long, Qiqi; Liu, Xishi; Qi, Qiuming; Guo, Sun-Wei

2016-11-01

Does chronic stress in mice accelerate the development of endometriosis, and, if so, through what mechanism? Exposure to chronic stress accelerates the development of endometriosis and exacerbates the endometriosis-associated generalized hyperalgesia, most likely through activation of the adrenoceptor β2 (ADRB2) and cAMP responsive element-binding protein (CREB). Women with endometriosis tend to have higher levels of psychological stress, which is known to impact negatively on health in general and to promote tumor growth and metastasis in particular. Exposure to chronic stress before and after the induction of endometriosis is reported to increase lesion sizes in rodents, but it is unclear whether adrenoceptors are involved or not in the stress-promoted development of endometriosis. Three independent, prospective, randomized mouse experimentations. A total of 184 virgin female Balb/C mice were used. In Experiment 1, the mice were randomly divided into four groups: the control group, which received no stress; the before, after and both groups, which received immobilization stress before, after and both before and after the induction of endometriosis, respectively. In Experiment 2, mice were randomly divided into four groups one day after the induction of endometriosis: phosphate buffer saline (PBS) and propranolol (PROP) groups, which received the mini-pump containing, respectively, PBS only and propranolol (a non-selective ADRB antagonist) but no stress, STR+PROP and STR+PBS groups, which received stress and the mini-pump containing, respectively, propranolol and PBS. The immobilization stress started after the insertion of mini-pumps. In Experiment 3, mice were induced with endometriosis. Three days after the induction, they were randomly divided into four groups: control, ADRAa, ADRB2a, and ADRBa, which received the mini-pump containing solution only, metaraminol (a non-specific α adrenoceptor agonist), tebutaline (a specific ADRB2 agonist), or isoproterenol

48 CFR 9903.101 - Cost Accounting Standards.

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2010-10-01

... 48 Federal Acquisition Regulations System 7 2010-10-01 2010-10-01 false Cost Accounting Standards. 9903.101 Section 9903.101 Federal Acquisition Regulations System COST ACCOUNTING STANDARDS BOARD... ACCOUNTING STANDARDS CONTRACT COVERAGE General 9903.101 Cost Accounting Standards. Public Law 100-679 (41 U.S...

41 CFR 101-4.115 - Assurance required.

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2010-07-01

... EDUCATION PROGRAMS OR ACTIVITIES RECEIVING FEDERAL FINANCIAL ASSISTANCE Introduction § 101-4.115 Assurance... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Assurance required. 101-4.115 Section 101-4.115 Public Contracts and Property Management Federal Property Management Regulations...

5 CFR 2600.101 - Mission and history.

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2010-01-01

... 5 Administrative Personnel 3 2010-01-01 2010-01-01 false Mission and history. 2600.101 Section 2600.101 Administrative Personnel OFFICE OF GOVERNMENT ETHICS ORGANIZATION AND PROCEDURES ORGANIZATION AND FUNCTIONS OF THE OFFICE OF GOVERNMENT ETHICS § 2600.101 Mission and history. (a) The Office of...

41 CFR 50-201.101 - Employees affected.

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2010-07-01

... 41 Public Contracts and Property Management 1 2010-07-01 2010-07-01 true Employees affected. 50-201.101 Section 50-201.101 Public Contracts and Property Management Other Provisions Relating to Public Contracts PUBLIC CONTRACTS, DEPARTMENT OF LABOR 201-GENERAL REGULATIONS § 50-201.101 Employees...

Generalized concentration addition: a method for examining mixtures containing partial agonists.

Science.gov (United States)

Howard, Gregory J; Webster, Thomas F

2009-08-07

Environmentally relevant toxic exposures often consist of simultaneous exposure to multiple agents. Methods to predict the expected outcome of such combinations are critical both to risk assessment and to an accurate judgment of whether combinations are synergistic or antagonistic. Concentration addition (CA) has commonly been used to assess the presence of synergy or antagonism in combinations of similarly acting chemicals, and to predict effects of combinations of such agents. CA has the advantage of clear graphical interpretation: Curves of constant joint effect (isoboles) must be negatively sloped straight lines if the mixture is concentration additive. However, CA cannot be directly used to assess combinations that include partial agonists, although such agents are of considerable interest. Here, we propose a natural extension of CA to a functional form that may be applied to mixtures including full agonists and partial agonists. This extended definition, for which we suggest the term "generalized concentration addition," encompasses linear isoboles with slopes of any sign. We apply this approach to the simple example of agents with dose-response relationships described by Hill functions with slope parameter n=1. The resulting isoboles are in all cases linear, with negative, zero and positive slopes. Using simple mechanistic models of ligand-receptor systems, we show that the same isobole pattern and joint effects are generated by modeled combinations of full and partial agonists. Special cases include combinations of two full agonists and a full agonist plus a competitive antagonist.

7 CFR 4279.101 - Introduction.

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2010-01-01

... 7 Agriculture 15 2010-01-01 2010-01-01 false Introduction. 4279.101 Section 4279.101 Agriculture Regulations of the Department of Agriculture (Continued) RURAL BUSINESS-COOPERATIVE SERVICE AND RURAL... Introduction. (a) Content. This subpart contains loan processing regulations for the Business and Industry (B&I...

Main: PPD101 [AT Atlas

Lifescience Database Archive (English)

Full Text Available PPD101 PPD1 Development of novel affinity tag system for the high-quality productio...uantification, purification and tag removal for a variety of proteins. MPB3|MPB4 Protein Sci. (2008)|Hybridoma. (2008)|J Proteomics. (2010) 18787202|20566373|18847346 PPD101.csml ...

48 CFR 2.101 - Definitions.

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2010-10-01

... 48 Federal Acquisition Regulations System 1 2010-10-01 2010-10-01 false Definitions. 2.101 Section 2.101 Federal Acquisition Regulations System FEDERAL ACQUISITION REGULATION GENERAL DEFINITIONS OF..., recommendations, training and the day-to-day aid of support personnel needed for the successful performance of...

48 CFR 470.101 - Definitions.

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2010-10-01

.... 55314(c), with respect to an agricultural product acquired under this part the lowest aggregate cost for... 48 Federal Acquisition Regulations System 4 2010-10-01 2010-10-01 false Definitions. 470.101 Section 470.101 Federal Acquisition Regulations System DEPARTMENT OF AGRICULTURE FOOD ASSISTANCE PROGRAMS...

48 CFR 2402.101 - Definitions.

Science.gov (United States)

2010-10-01

... GENERAL DEFINITIONS OF WORDS AND TERMS Definitions 2402.101 Definitions. Accounting Office means the Office of Accounting Operations within the Office of the Chief Financial Officer and includes that Office... 48 Federal Acquisition Regulations System 6 2010-10-01 2010-10-01 true Definitions. 2402.101...

14 CFR 101.19 - Rapid deflation device.

Science.gov (United States)

2010-01-01

... 14 Aeronautics and Space 2 2010-01-01 2010-01-01 false Rapid deflation device. 101.19 Section 101.19 Aeronautics and Space FEDERAL AVIATION ADMINISTRATION, DEPARTMENT OF TRANSPORTATION (CONTINUED... BALLOONS Moored Balloons and Kites § 101.19 Rapid deflation device. No person may operate a moored balloon...

41 CFR 101-1.112 - Change lines.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Change lines. 101-1.112 Section 101-1.112 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101-1.112 Change...

41 CFR 105-1.101-50 - Exclusions.

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2010-07-01

... 41 Public Contracts and Property Management 3 2010-07-01 2010-07-01 false Exclusions. 105-1.101-50 Section 105-1.101-50 Public Contracts and Property Management Federal Property Management Regulations System (Continued) GENERAL SERVICES ADMINISTRATION 1-INTRODUCTION 1.1-Regulations System § 105-1.101-50...

41 CFR 101-1.4902 - GSA forms.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true GSA forms. 101-1.4902 Section 101-1.4902 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.49-Illustrations of Forms § 101-1.4902...

32 CFR 101.1 - Reissuance and purpose.

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2010-07-01

... PARTICIPATION IN RESERVE TRAINING PROGRAMS § 101.1 Reissuance and purpose. This part establishes: (a) The criteria and training requirements for satisfactory participation by members of the Reserve components of... 32 National Defense 1 2010-07-01 2010-07-01 false Reissuance and purpose. 101.1 Section 101.1...

41 CFR 101-39.407 - Accident records.

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2010-07-01

...-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.4-Accidents and Claims § 101-39.407 Accident records. If GSA's records... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Accident records. 101-39.407 Section 101-39.407 Public Contracts and Property Management Federal Property Management...

41 CFR 101-27.102-2 - Guidelines.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Guidelines. 101-27.102-2 Section 101-27.102-2 Public Contracts and Property Management Federal Property Management Regulations... Replenishment § 101-27.102-2 Guidelines. Guidelines for implementing the EOQ principle of stock replenishment...

41 CFR 101-25.402 - Motor vehicles.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Motor vehicles. 101-25.402 Section 101-25.402 Public Contracts and Property Management Federal Property Management... Standards § 101-25.402 Motor vehicles. Replacement of motor vehicles shall be in accordance with the...

Synthesis and Characterization Studies of MIL-101

Directory of Open Access Journals (Sweden)

Emine Kaya EKİNCİ

2017-12-01

Full Text Available MIL-101 is a kind of Metal Organic Frameworks (MOFs, which have attracted much attention in the past decade due to its promising application in chemical industries. MIL-101 is also known as “Porous Chromium Terephthalate”. It has very high surface area and pore volume. MIL-101 exhibits exceptional stability against moisture and other chemicals and is composed of coordinately unsaturated Cr- sites with high concentration available for catalysis and adsorption. MIL-101 was synthesized by hydrothermal method and characterized by XRD, nitrogen adsorption and desorption analyses and SEM. XRD patterns show the presence of MIL-101’s crystal structure with high surface area (~2400 m2/g. Nitrogen adsorption-desorption analyzes showed that the material exhibited mesoporous material behavior.

45 CFR 2490.101 - Purpose.

Science.gov (United States)

2010-10-01

... 45 Public Welfare 4 2010-10-01 2010-10-01 false Purpose. 2490.101 Section 2490.101 Public Welfare Regulations Relating to Public Welfare (Continued) JAMES MADISON MEMORIAL FELLOWSHIP FOUNDATION ENFORCEMENT OF NONDISCRIMINATION ON THE BASIS OF HANDICAP IN PROGRAMS OR ACTIVITIES CONDUCTED BY THE JAMES MADISON MEMORIAL...

42 CFR 93.101 - Purpose.

Science.gov (United States)

2010-10-01

... 42 Public Health 1 2010-10-01 2010-10-01 false Purpose. 93.101 Section 93.101 Public Health PUBLIC HEALTH SERVICE, DEPARTMENT OF HEALTH AND HUMAN SERVICES HEALTH ASSESSMENTS AND HEALTH EFFECTS STUDIES OF HAZARDOUS SUBSTANCES RELEASES AND FACILITIES PUBLIC HEALTH SERVICE POLICIES ON RESEARCH MISCONDUCT General...

13 CFR 106.101 - Definitions.

Science.gov (United States)

2010-01-01

... legal consideration. (i) Non-Fee Based SBA-Sponsored Activity Record (Non-Fee Based Record) means a... 13 Business Credit and Assistance 1 2010-01-01 2010-01-01 false Definitions. 106.101 Section 106.101 Business Credit and Assistance SMALL BUSINESS ADMINISTRATION COSPONSORSHIPS, FEE AND NON-FEE BASED...

The Good, the Bad, and the Ugly: Agonistic Behaviour in Juvenile Crocodilians

OpenAIRE

Brien, Matthew L.; Lang, Jeffrey W.; Webb, Grahame J.; Stevenson, Colin; Christian, Keith A.

2013-01-01

We examined agonistic behaviour in seven species of hatchling and juvenile crocodilians held in small groups (N = 4) under similar laboratory conditions. Agonistic interactions occurred in all seven species, typically involved two individuals, were short in duration (5-15 seconds), and occurred between 1600-2200 h in open water. The nature and extent of agonistic interactions, the behaviours displayed, and the level of conspecific tolerance varied among species. Discrete postures, non-contact...

Prolonging survival of corneal transplantation by selective sphingosine-1-phosphate receptor 1 agonist.

Directory of Open Access Journals (Sweden)

Min Gao

Full Text Available Corneal transplantation is the most used therapy for eye disorders. Although the cornea is somewhat an immune privileged organ, immune rejection is still the major problem that reduces the success rate. Therefore, effective chemical drugs that regulate immunoreactions are needed to improve the outcome of corneal transplantations. Here, a sphingosine-1-phosphate receptor 1 (S1P1 selective agonist was systematically evaluated in mouse allogeneic corneal transplantation and compared with the commonly used immunosuppressive agents. Compared with CsA and the non-selective sphingosine 1-phosphate (S1P receptor agonist FTY720, the S1P1 selective agonist can prolong the survival corneal transplantation for more than 30 days with a low immune response. More importantly, the optimal dose of the S1P1 selective agonist was much less than non-selective S1P receptor agonist FTY720, which would reduce the dose-dependent toxicity in drug application. Then we analyzed the mechanisms of the selected S1P1 selective agonist on the immunosuppression. The results shown that the S1P1 selective agonist could regulate the distribution of the immune cells with less CD4+ T cells and enhanced Treg cells in the allograft, moreover the expression of anti-inflammatory cytokines TGF-β1 and IL-10 unregulated which can reduce the immunoreactions. These findings suggest that S1P1 selective agonist may be a more appropriate immunosuppressive compound to effectively prolong mouse allogeneic corneal grafts survival.

34 CFR 101.32 - Signature of documents.

Science.gov (United States)

2010-07-01

... 34 Education 1 2010-07-01 2010-07-01 false Signature of documents. 101.32 Section 101.32 Education Regulations of the Offices of the Department of Education OFFICE FOR CIVIL RIGHTS, DEPARTMENT OF EDUCATION... Documents § 101.32 Signature of documents. The signature of a party, authorized officer, employee or...

12 CFR 708b.101 - Mergers generally.

Science.gov (United States)

2010-01-01

... 12 Banks and Banking 6 2010-01-01 2010-01-01 false Mergers generally. 708b.101 Section 708b.101 Banks and Banking NATIONAL CREDIT UNION ADMINISTRATION REGULATIONS AFFECTING CREDIT UNIONS MERGERS OF FEDERALLY-INSURED CREDIT UNIONS; VOLUNTARY TERMINATION OR CONVERSION OF INSURED STATUS Mergers § 708b.101...

41 CFR 101-27.206-3 - Packaging.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Packaging. 101-27.206-3 Section 101-27.206-3 Public Contracts and Property Management Federal Property Management Regulations...-Management of Shelf-Life Materials § 101-27.206-3 Packaging. To the extent feasible and economical, shelf...

25 CFR 101.15 - Penalties on default.

Science.gov (United States)

2010-04-01

... 25 Indians 1 2010-04-01 2010-04-01 false Penalties on default. 101.15 Section 101.15 Indians BUREAU OF INDIAN AFFAIRS, DEPARTMENT OF THE INTERIOR FINANCIAL ACTIVITIES LOANS TO INDIANS FROM THE REVOLVING LOAN FUND § 101.15 Penalties on default. Unless otherwise provided in the loan agreement between...

41 CFR 101-1.104-1 - Publication.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Publication. 101-1.104-1 Section 101-1.104-1 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101-1.104-1...

41 CFR 101-1.104-2 - Distribution.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Distribution. 101-1.104-2 Section 101-1.104-2 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101-1.104-2...

21 CFR 101.18 - Misbranding of food.

Science.gov (United States)

2010-04-01

... 21 Food and Drugs 2 2010-04-01 2010-04-01 false Misbranding of food. 101.18 Section 101.18 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR HUMAN CONSUMPTION FOOD LABELING General Provisions § 101.18 Misbranding of food. (a) Among...

7 CFR 43.101 - Meaning of words.

Science.gov (United States)

2010-01-01

... 7 Agriculture 2 2010-01-01 2010-01-01 false Meaning of words. 43.101 Section 43.101 Agriculture Regulations of the Department of Agriculture AGRICULTURAL MARKETING SERVICE (Standards, Inspections, Marketing... SAMPLING PLANS Definitions § 43.101 Meaning of words. Words used in this subpart in the singular form shall...

7 CFR 42.101 - Meaning of words.

Science.gov (United States)

2010-01-01

... 7 Agriculture 2 2010-01-01 2010-01-01 false Meaning of words. 42.101 Section 42.101 Agriculture Regulations of the Department of Agriculture AGRICULTURAL MARKETING SERVICE (Standards, Inspections, Marketing... CONDITION OF FOOD CONTAINERS Definitions § 42.101 Meaning of words. Words used in this part in the singular...

32 CFR 935.101 - Seizure of property.

Science.gov (United States)

2010-07-01

... 32 National Defense 6 2010-07-01 2010-07-01 false Seizure of property. 935.101 Section 935.101 National Defense Department of Defense (Continued) DEPARTMENT OF THE AIR FORCE TERRITORIAL AND INSULAR REGULATIONS WAKE ISLAND CODE Criminal Actions § 935.101 Seizure of property. Any property seized in connection...

Low temperature synthesis of {tau}-zirconium hydrogenophosphate [{tau}-Zr(HPO{sub 4}){sub 2}] and a new sodic form obtained by ion exchange

Energy Technology Data Exchange (ETDEWEB)

Fernandez-Valverde, Suilma M., E-mail: suilma.fernandez@inin.gob.mx [Depto. de Quimica, Instituto Nacional de Investigaciones Nucleares, A.P. 18-1027, Mexico D.F. C.P. 11801 (Mexico); Contreras-Ramirez, Aida [Depto. de Quimica, Instituto Nacional de Investigaciones Nucleares, A.P. 18-1027, Mexico D.F. C.P. 11801 (Mexico); Depto. de Tecnologia de Materiales, Instituto Nacional de Investigaciones Nucleares, A.P. 18-1027, Mexico D.F. C.P. 11801 (Mexico); Facultad de Ciencias, Universidad Autonoma del Estado de Mexico, Piedras Blancas El Cerrillo, Tlachaloya Estado de Mexico, CP.5000 (Mexico); Ordonez-Regil, Eduardo [Depto. de Quimica, Instituto Nacional de Investigaciones Nucleares, A.P. 18-1027, Mexico D.F. C.P. 11801 (Mexico); Fernandez-Garcia, M. Eufemia [Depto. de Tecnologia de Materiales, Instituto Nacional de Investigaciones Nucleares, A.P. 18-1027, Mexico D.F. C.P. 11801 (Mexico); Perez-Alvarez, Mario [Depto. de Ambientales, Instituto Nacional de Investigaciones Nucleares, A.P. 18-1027, Mexico D.F. C.P. 11801 (Mexico)

2013-02-15

A new method for the synthesis of 3-D {tau}-zirconium hydrogenophosphate (TZP) was developed using solid-state reactions at low temperature and atmospheric pressure in a nitrogen atmosphere in a two-hour reaction time. The characterization of the compound was performed using X-ray diffraction, infrared spectroscopy, scanning electron microscopy, energy dispersive X-ray spectroscopy, differential scanning calorimetric, thermochemical analysis and X-ray photoelectron spectroscopy. A sodic form of the compound obtained by the immersion of TZP in a sodium hydroxide solution was characterized using the same techniques along with neutron activation analysis. The XPS spectra confirm the binding energy value for sodium-oxygen, and the XRD diffraction reveals the formation of a new sodium compound. - Graphical abstract: DRX, XPS and MEB of {tau}-zirconium hydrogenophosphate and its sodic form on the surface of TZP. Highlights: Black-Right-Pointing-Pointer New method for the syntheses of 3-D {tau}-zirconium hydrogenophosphate (TZP). Black-Right-Pointing-Pointer A sodic form of the TZP was obtained by the immersion of TZP in a sodium hydroxide. Black-Right-Pointing-Pointer The sodium compound is only formed on the TZP surface.

Highly efficient capture of iodine by Cu/MIL-101

Science.gov (United States)

Qi, Bingbing; Liu, Ying; Zheng, Tao; Gao, Qianhong; Yan, Xuewu; Jiao, Yan; Yang, Yi

2018-02-01

In order to improve the uptake capacity of MIL-101 for iodine, Cu nanoparticles doped MIL-101 were successfully synthesized through a facile method. The obtained Cu/MIL-101 was characterized by SEM, XRD, EDS, TEM, IR, TGA and BET to examine the chemical and thermal stabilities. The capture experiments for the adsorbents showed that the capture capacity of Cu/MIL-101 for volatile iodine is 342 wt%, which is higher than that of pure MIL-101. An I2 uptake of 342 wt% is the highest value reported among metal-organic frameworks. Furthermore, Cu/MIL-101 has a cycle ratio of 95% after three cycles and exhibits a better cyclicity than pure MIL-101. Meanwhile, Cu/MIL-101 shows an excellent reversible adsorption of iodine in solution.

18 CFR 4.101 - Applicability.

Science.gov (United States)

2010-04-01

... PROJECT COSTS Exemption of Small Hydroelectric Power Projects of 5 Megawatts or Less § 4.101 Applicability... the Federal Power Act (Act), including licensing, for small hydroelectric power projects as defined in... 18 Conservation of Power and Water Resources 1 2010-04-01 2010-04-01 false Applicability. 4.101...

12 CFR 19.101 - Delegation to OFIA.

Science.gov (United States)

2010-01-01

... 12 Banks and Banking 1 2010-01-01 2010-01-01 false Delegation to OFIA. 19.101 Section 19.101 Banks and Banking COMPTROLLER OF THE CURRENCY, DEPARTMENT OF THE TREASURY RULES OF PRACTICE AND PROCEDURE Procedural Rules for OCC Adjudications § 19.101 Delegation to OFIA. Unless otherwise ordered by the...

7 CFR 1437.101 - Actual production history.

Science.gov (United States)

2010-01-01

... 7 Agriculture 10 2010-01-01 2010-01-01 false Actual production history. 1437.101 Section 1437.101... Determining Yield Coverage Using Actual Production History § 1437.101 Actual production history. Actual production history (APH) is the unit's record of crop yield by crop year for the APH base period. The APH...

41 CFR 101-5.306 - Economic feasibility.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Economic feasibility. 101... AND COMPLEXES 5.3-Federal Employee Health Services § 101-5.306 Economic feasibility. (a) The studies... § 101-5.104. (b) Each determination to provide health services will be governed by the principles stated...

Long-acting beta 2-agonists in chronic obstructive pulmonary disease.

Science.gov (United States)

Llewellyn-Jones, Carol

2002-01-01

Until recently, the use of long-acting beta 2-agonists in chronic obstructive pulmonary disease has been understated. There is now evidence that they may offer benefits beyond bronchodilation. This article reviews the management of chronic obstructive pulmonary disease and looks at the place of long-acting beta 2-agonists as a first-line treatment option.

Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity

DEFF Research Database (Denmark)

Goncalves de Azavedo, Carlos M. B. P.; Watterson, Kenneth R; Wargent, Ed T

2016-01-01

The free fatty acid receptor 4 (FFA4 or GPR120) has appeared as an interesting potential target for the treatment of metabolic disorders. At present, most FFA4 ligands are carboxylic acids that are assumed to mimic the endogenous long-chain fatty acid agonists. Here, we report preliminary structure......-activity relationship studies of a previously disclosed non-acidic sulfonamide FFA4 agonist. Mutagenesis studies indicate that the compounds are orthosteric agonists despite the absence of a carboxylate function. The preferred compounds showed full agonist activity on FFA4 and complete selectivity over FFA1, although...... a significant fraction of these non-carboxylic acids also showed partial antagonistic activity on FFA1. Studies in normal and diet-induced obese (DIO) mice with the preferred compound 34 showed improved glucose tolerance after oral dosing in an oral glucose tolerance test. Chronic dosing of 34 in DIO mice...

Radiosensitizing Effects of Ectopic miR-101 on Non–Small-Cell Lung Cancer Cells Depend on the Endogenous miR-101 Level

International Nuclear Information System (INIS)

Chen, Susie; Wang Hongyan; Ng, Wooi Loon; Curran, Walter J.; Wang Ya

2011-01-01

Purpose: Previously, we showed that ectopic miR-101 could sensitize human tumor cells to radiation by targeting ATM and DNA-PK catalytic subunit (DNA-PKcs) to inhibit DNA repair, as the endogenous miR-101 levels are low in tumors in general. However, the heterogeneity of human cancers may result in an exception. The purpose of this study was to test the hypothesis that a few tumor cell lines with a high level of endogenous miR-101 would prove less response to ectopic miR-101. Methods and Materials: Fourteeen non–small-cell lung cancer (NSCLC) cell lines and one immortalized non-malignant lung epithelial cell line (NL20) were used for comparing endogenous miR-101 levels by real-time reverse transcription–polymerase chain reaction. Based on the different miR-101 levels, four cell lines with different miR-101 levels were chosen for transfection with a green fluorescent protein–lentiviral plasmid encoding miR-101. The target protein levels were measured by using Western blotting. The radiosensitizing effects of ectopic miR-101 on these NSCLC cell lines were determined by a clonogenic assay and xenograft mouse model. Results: The endogenous miR-101 level was similar or lower in 13 NSCLC cell lines but was 11-fold higher in one cell line (H157) than in NL20 cells. Although ectopic miR-101 efficiently decreased the ATM and DNA-PKcs levels and increased the radiosensitization level in H1299, H1975, and A549 cells, it did not change the levels of the miR-101 targets or radiosensitivity in H157 cells. Similar results were observed in xenograft mice. Conclusions: A small number of NSCLC cell lines could have a high level of endogenous miR-101. The ectopic miR-101 was able to radiosensitize most NSCLC cells, except for the NSCLC cell lines that had a much higher endogenous miR-101 level. These results suggest that when we choose one miRNA as a therapeutic tool, the endogenous level of the miRNA in each tumor should be considered.

Radiosensitizing Effects of Ectopic miR-101 on Non-Small-Cell Lung Cancer Cells Depend on the Endogenous miR-101 Level

Energy Technology Data Exchange (ETDEWEB)

Chen, Susie; Wang Hongyan; Ng, Wooi Loon; Curran, Walter J. [Department of Radiation Oncology, School of Medicine and the Winship Cancer Institute, Emory University, Atlanta, GA (United States); Wang Ya, E-mail: ywang94@emory.edu [Department of Radiation Oncology, School of Medicine and the Winship Cancer Institute, Emory University, Atlanta, GA (United States)

2011-12-01

Purpose: Previously, we showed that ectopic miR-101 could sensitize human tumor cells to radiation by targeting ATM and DNA-PK catalytic subunit (DNA-PKcs) to inhibit DNA repair, as the endogenous miR-101 levels are low in tumors in general. However, the heterogeneity of human cancers may result in an exception. The purpose of this study was to test the hypothesis that a few tumor cell lines with a high level of endogenous miR-101 would prove less response to ectopic miR-101. Methods and Materials: Fourteeen non-small-cell lung cancer (NSCLC) cell lines and one immortalized non-malignant lung epithelial cell line (NL20) were used for comparing endogenous miR-101 levels by real-time reverse transcription-polymerase chain reaction. Based on the different miR-101 levels, four cell lines with different miR-101 levels were chosen for transfection with a green fluorescent protein-lentiviral plasmid encoding miR-101. The target protein levels were measured by using Western blotting. The radiosensitizing effects of ectopic miR-101 on these NSCLC cell lines were determined by a clonogenic assay and xenograft mouse model. Results: The endogenous miR-101 level was similar or lower in 13 NSCLC cell lines but was 11-fold higher in one cell line (H157) than in NL20 cells. Although ectopic miR-101 efficiently decreased the ATM and DNA-PKcs levels and increased the radiosensitization level in H1299, H1975, and A549 cells, it did not change the levels of the miR-101 targets or radiosensitivity in H157 cells. Similar results were observed in xenograft mice. Conclusions: A small number of NSCLC cell lines could have a high level of endogenous miR-101. The ectopic miR-101 was able to radiosensitize most NSCLC cells, except for the NSCLC cell lines that had a much higher endogenous miR-101 level. These results suggest that when we choose one miRNA as a therapeutic tool, the endogenous level of the miRNA in each tumor should be considered.

34 CFR 101.85 - Offer of proof.

Science.gov (United States)

2010-07-01

... 34 Education 1 2010-07-01 2010-07-01 false Offer of proof. 101.85 Section 101.85 Education... PRACTICE AND PROCEDURE FOR HEARINGS UNDER PART 100 OF THIS TITLE Hearing Procedures § 101.85 Offer of proof. An offer of proof made in connection with an objection taken to any ruling of the presiding officer...

19 CFR 101.6 - Hours of business.

Science.gov (United States)

2010-04-01

... 19 Customs Duties 1 2010-04-01 2010-04-01 false Hours of business. 101.6 Section 101.6 Customs... GENERAL PROVISIONS § 101.6 Hours of business. Except as specified in paragraphs (a) through (g) of this section, each CBP office shall be open for the transactions of general CBP business between the hours of 8...

29 CFR 101.18 - Investigation of petition.

Science.gov (United States)

2010-07-01

... 29 Labor 2 2010-07-01 2010-07-01 false Investigation of petition. 101.18 Section 101.18 Labor... Under Section 9(c) of the Act and Petitions for Clarification of Bargaining Units and for Amendment of Certifications Under Section 9(b) of the Act § 101.18 Investigation of petition. (a) Upon receipt of the petition...

Contamination with retinoic acid receptor agonists in two rivers in the Kinki region of Japan.

Science.gov (United States)

Inoue, Daisuke; Nakama, Koki; Sawada, Kazuko; Watanabe, Taro; Takagi, Mai; Sei, Kazunari; Yang, Min; Hirotsuji, Junji; Hu, Jianying; Nishikawa, Jun-ichi; Nakanishi, Tsuyoshi; Ike, Michihiko

2010-04-01

This study was conducted to investigate the agonistic activity against human retinoic acid receptor (RAR) alpha in the Lake Biwa-Yodo River and the Ina River in the Kinki region of Japan. To accomplish this, a yeast two-hybrid assay was used to elucidate the spatial and temporal variations and potential sources of RARalpha agonist contamination in the river basins. RARalpha agonistic activity was commonly detected in the surface water samples collected along two rivers at different periods, with maximum all-trans retinoic acid (atRA) equivalents of 47.6 ng-atRA/L and 23.5 ng-atRA/L being observed in Lake Biwa-Yodo River and Ina River, respectively. The results indicated that RARalpha agonists are always present and widespread in the rivers. Comparative investigation of RARalpha and estrogen receptor alpha agonistic activities at 20 stations along each river revealed that the spatial variation pattern of RARalpha agonist contamination was entirely different from that of the estrogenic compound contamination. This suggests that the effluent from municipal wastewater treatment plants, a primary source of estrogenic compounds, seemed not to be the cause of RARalpha agonist contamination in the rivers. Fractionation using high performance liquid chromatography (HPLC) directed by the bioassay found two bioactive fractions from river water samples, suggesting the presence of at least two RARalpha agonists in the rivers. Although a trial conducted to identify RARalpha agonists in the major bioactive fraction was not completed as part of this study, comparison of retention times in HPLC analysis and quantification with liquid chromatography-mass spectrometry analysis revealed that the major causative contaminants responsible for the RARalpha agonistic activity were not RAs (natural RAR ligands) and 4-oxo-RAs, while 4-oxo-RAs were identified as the major RAR agonists in sewage in Beijing, China. These findings suggest that there are unknown RARalpha agonists with high

Targeted Delivery of LXR Agonist Using a Site-Specific Antibody-Drug Conjugate.

Science.gov (United States)

Lim, Reyna K V; Yu, Shan; Cheng, Bo; Li, Sijia; Kim, Nam-Jung; Cao, Yu; Chi, Victor; Kim, Ji Young; Chatterjee, Arnab K; Schultz, Peter G; Tremblay, Matthew S; Kazane, Stephanie A

2015-11-18

Liver X receptor (LXR) agonists have been explored as potential treatments for atherosclerosis and other diseases based on their ability to induce reverse cholesterol transport and suppress inflammation. However, this therapeutic potential has been hindered by on-target adverse effects in the liver mediated by excessive lipogenesis. Herein, we report a novel site-specific antibody-drug conjugate (ADC) that selectively delivers a LXR agonist to monocytes/macrophages while sparing hepatocytes. The unnatural amino acid para-acetylphenylalanine (pAcF) was site-specifically incorporated into anti-CD11a IgG, which binds the α-chain component of the lymphocyte function-associated antigen 1 (LFA-1) expressed on nearly all monocytes and macrophages. An aminooxy-modified LXR agonist was conjugated to anti-CD11a IgG through a stable, cathepsin B cleavable oxime linkage to afford a chemically defined ADC. The anti-CD11a IgG-LXR agonist ADC induced LXR activation specifically in human THP-1 monocyte/macrophage cells in vitro (EC50-27 nM), but had no significant effect in hepatocytes, indicating that payload delivery is CD11a-mediated. Moreover, the ADC exhibited higher-fold activation compared to a conventional synthetic LXR agonist T0901317 (Tularik) (3-fold). This novel ADC represents a fundamentally different strategy that uses tissue targeting to overcome the limitations of LXR agonists for potential use in treating atherosclerosis.

Allosteric enhancers, allosteric agonists and ago-allosteric modulators: where do they bind and how do they act?

DEFF Research Database (Denmark)

Schwartz, Thue W; Holst, Birgitte

2007-01-01

Many small-molecule agonists also display allosteric properties. Such ago-allosteric modulators act as co-agonists, providing additive efficacy--instead of partial antagonism--and they can affect--and often improve--the potency of the endogenous agonist. Surprisingly, the apparent binding sites...... different binding modes. In another, dimeric, receptor scenario, the endogenous agonist binds to one protomer while the ago-allosteric modulator binds to the other, 'allosteric' protomer. It is suggested that testing for ago-allosteric properties should be an integral part of the agonist drug discovery...... process because a compound that acts with--rather than against--the endogenous agonist could be an optimal agonist drug....

The treatment of Parkinson's disease with dopamine agonists

Directory of Open Access Journals (Sweden)

Frank, Wilhelm

2008-06-01

Full Text Available Parkinson’s disease is a chronic degenerative organic disease with unknown causes. A disappearance of cells with melanin in the substantia nigra is considered as biological artefact of the disease, which causes a degenerative loss of neurons in the corpus striatum of mesencephalon. This structure produces also the transmitter substance dopamine. Due to this disappearance of cells dopamine is not produced in a sufficient quantity which is needed for movement of the body. The questions of this report are concerned the efficiency and safety of a treatment with dopamine agonists. Furthermore the cost-effectiveness is investigated as well as ethic questions. The goal is to give recommendation for the use of dopamine agonists to the German health system. A systematic literature search was done. The identified studies have different methodological quality and investigate different hypothesis and different outcome criteria. Therefore a qualitative method of information synthesis was chosen. Since the introduction of L-Dopa in the 1960´s it is considered as the most effective substance to reduce all the cardinal symptoms of Parkinson disease. This substance was improved in the course of time. Firstly some additional substances were given (decarbonxylase inhibitors, catechol-o-transferase inhibitors (COMT-inhibitors, monoaminoxydase-inhibitors (MAO-inhibitors and NMDA-antagonists (N-Methyl-d-aspartat-antagonists. In the practical therapy of Parkinson dopamine agonists play an important role, because they directly use the dopamine receptors. The monotherapy of Parkinson disease is basically possible and is used in early stages of the disease. Clinical practise has shown, that an add on therapy with dopamine agonists can led to a reduction of the dose of L-dopa and a reduction of following dyskinesia. The studies for effectiveness include studies for the initial therapy, monotherapy and add-on-therapy. Basically there is a good effectiveness of dopamine

Dopamine agonist activity of EMD 23,448

International Nuclear Information System (INIS)

Martin, G.E.; Pettibone, D.J.

1985-01-01

EMD 23,448 was examined in tests of dopaminergic function and was found to be an atypical dopamine (DA) agonist. EMD 23,448 was a weak or inactive DA agonist when examined in tests of normal postsynaptic DA receptor function: production of stereotypy in the rat (ED 50 greater than sign 5.0 mg/kg.i.p.); production of emesis in beagles (minimum effective dose = 81μg/kg i.v.); and, enhanced locomotor activity of the mouse (no excitation in doses 3 H]-apomorphine binding to rat striatal membranes (Ki, 205 nM). On the other hand, this indolyl-3-butylamine did activate supersensitive postsynaptic DA receptors. Specifically, it elicited contralateral turning in rats with a unilateral 6-hydroxydopamine lesion of the substantia nigra (ED 50 value = 0.9 mg/kg) and did elicit stereotypy in rats given chronic daily haloperidol treatments. EMD 23,448 also exerted pharmacological effects in tests designed to measure activation of dopamine autoreceptors. It inhibited the γ-butyrolactone-induced increase in striatal dopa levels (ED 50 = 1 mg/kg i.p.) and produced a dose-related fall in the locomotor activity of the mouse. The results are discussed and contrasted with data derived for apomorphine and the putatively selective autoreceptor agonist (+-)-3-PPP. (Author)

48 CFR 2905.101 - Methods of disseminating information.

Science.gov (United States)

2010-10-01

... information. 2905.101 Section 2905.101 Federal Acquisition Regulations System DEPARTMENT OF LABOR ACQUISITION PLANNING PUBLICIZING CONTRACT ACTIONS Dissemination of Information 2905.101 Methods of disseminating... dissemination of information concerning procurement actions. The Division of Acquisition Management Services...

Analysis of agonist dissociation constants as assessed by functional antagonism in guinea pig left atria

International Nuclear Information System (INIS)

Molenaar, P.; Malta, E.

1986-01-01

In electrically driven guinea pig left atria, positive inotropic responses to (-)-isoprenaline and the selective beta 1-adrenoceptor agonist RO363 were obtained in the absence and in the presence of the functional antagonists adenosine, carbachol, gallopamil, nifedipine, and Ro 03-7894. Each of the functional antagonists reduced the maximum response to both agonists and produced nonparallel rightward shifts in the cumulative concentration effect curves. For both agonists, dissociation constants (KA) were calculated using the equation described by Furchgott (1966) for irreversible antagonism. For RO363, which is a partial agonist with high agonist activity, the equations outlined for functional interaction by Mackay (1981) were also employed to calculate KA values. The KA values obtained by each method were compared with the dissociation constants (KD) for the two agonists determined from their ability to displace the radioligand (-)-[ 125 I]iodocyanopindolol from beta 1-adrenoceptors in guinea pig left atrial membrane preparations. The estimates of KA varied substantially from KD values. The KD values were taken as more accurate estimates of the true values for the dissociation constants because a high degree of correlation exists between pKD and pD2 values for a number of other beta-adrenoceptor agonists that behave as partial agonists and between pKD and pKB values for a number of beta-adrenoceptor antagonists. Thus, it appears that there are serious limitations in the current theory for using functional antagonism as a means of obtaining agonist dissociation constants

Inhibition by TRPA1 agonists of compound action potentials in the frog sciatic nerve

Energy Technology Data Exchange (ETDEWEB)

Matsushita, Akitomo; Ohtsubo, Sena; Fujita, Tsugumi; Kumamoto, Eiichi, E-mail: kumamote@cc.saga-u.ac.jp

2013-04-26

Highlights: •TRPA1 agonists inhibited compound action potentials in frog sciatic nerves. •This inhibition was not mediated by TRPA1 channels. •This efficacy was comparable to those of lidocaine and cocaine. •We found for the first time an ability of TRPA1 agonists to inhibit nerve conduction. -- Abstract: Although TRPV1 and TRPM8 agonists (vanilloid capsaicin and menthol, respectively) at high concentrations inhibit action potential conduction, it remains to be unknown whether TRPA1 agonists have a similar action. The present study examined the actions of TRPA1 agonists, cinnamaldehyde (CA) and allyl isothiocyanate (AITC), which differ in chemical structure from each other, on compound action potentials (CAPs) recorded from the frog sciatic nerve by using the air-gap method. CA and AITC concentration-dependently reduced the peak amplitude of the CAP with the IC{sub 50} values of 1.2 and 1.5 mM, respectively; these activities were resistant to a non-selective TRP antagonist ruthenium red or a selective TRPA1 antagonist HC-030031. The CA and AITC actions were distinct in property; the latter but not former action was delayed in onset and partially reversible, and CA but not AITC increased thresholds to elicit CAPs. A CAP inhibition was seen by hydroxy-α-sanshool (by 60% at 0.05 mM), which activates both TRPA1 and TRPV1 channels, a non-vanilloid TRPV1 agonist piperine (by 20% at 0.07 mM) and tetrahydrolavandulol (where the six-membered ring of menthol is opened; IC{sub 50} = 0.38 mM). It is suggested that TRPA1 agonists as well as TRPV1 and TRPM8 agonists have an ability to inhibit nerve conduction without TRP activation, although their agonists are quite different in chemical structure from each other.

Low-dose add-back therapy during postoperative GnRH agonist treatment

Directory of Open Access Journals (Sweden)

Hsiao-Wen Tsai

2016-02-01

Conclusion: Low dose add-back therapy could effectively ameliorate hypoestrogenic side effects and simultaneously maintain the therapeutic response of GnRH agonist treatment. The treatment dropout was lower compared with a regular dose. Therefore, low dose add-back therapy can be considered a treatment choice during postoperative GnRH agonist treatment.

34 CFR 101.79 - Cross-examination.

Science.gov (United States)

2010-07-01

... 34 Education 1 2010-07-01 2010-07-01 false Cross-examination. 101.79 Section 101.79 Education...-examination. A witness may be cross-examined on any matter material to the proceeding without regard to the scope of his direct examination. ...

[The antigravity suit, chamberless type, as a means of increasing orthostatic tolerance after water immersion hypokinesis and acceleration].

Science.gov (United States)

Shul'zhenko, E B; Kozlova, V G; Kurdin, K A; Iarov, A S; Plokhova, V G

1983-01-01

Orthostatic tolerance after 7-day dry immersion and head-to-feet acceleration was investigated on test subjects with and without an antigravity suit of bladderless type. With the suit on, the 20 min tilt test at 70 degrees prior to immersion induced less marked changes than without the suit. When the suit was on, cardiovascular reactions to tilt tests after immersion and acceleration improved. The maximum heart rate decreased from 135 +/- 4 to 101 +/- 5 beats/min (p less than 0.01), minimum stroke volume increased from 29 +/- 2 to 41 +/- 3 ml (p less than 0.05), and pulse pressure grew. Thus, an antigravity suit may help increase initial orthostatic tolerance and maintain it after the combined effect of simulated hypogravity and acceleration.

Scaffold-based pan-agonist design for the PPARα, PPARβ and PPARγ receptors.

Directory of Open Access Journals (Sweden)

Li-Song Zhang

Full Text Available As important members of nuclear receptor superfamily, Peroxisome proliferator-activated receptors (PPAR play essential roles in regulating cellular differentiation, development, metabolism, and tumorigenesis of higher organisms. The PPAR receptors have 3 identified subtypes: PPARα, PPARβ and PPARγ, all of which have been treated as attractive targets for developing drugs to treat type 2 diabetes. Due to the undesirable side-effects, many PPAR agonists including PPARα/γ and PPARβ/γ dual agonists are stopped by US FDA in the clinical trials. An alternative strategy is to design novel pan-agonist that can simultaneously activate PPARα, PPARβ and PPARγ. Under such an idea, in the current study we adopted the core hopping algorithm and glide docking procedure to generate 7 novel compounds based on a typical PPAR pan-agonist LY465608. It was observed by the docking procedures and molecular dynamics simulations that the compounds generated by the core hopping and glide docking not only possessed the similar functions as the original LY465608 compound to activate PPARα, PPARβ and PPARγ receptors, but also had more favorable conformation for binding to the PPAR receptors. The additional absorption, distribution, metabolism and excretion (ADME predictions showed that the 7 compounds (especially Cpd#1 hold high potential to be novel lead compounds for the PPAR pan-agonist. Our findings can provide a new strategy or useful insights for designing the effective pan-agonists against the type 2 diabetes.

The good, the bad, and the ugly: agonistic behaviour in juvenile crocodilians.

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Matthew L Brien

Full Text Available We examined agonistic behaviour in seven species of hatchling and juvenile crocodilians held in small groups (N = 4 under similar laboratory conditions. Agonistic interactions occurred in all seven species, typically involved two individuals, were short in duration (5-15 seconds, and occurred between 1600-2200 h in open water. The nature and extent of agonistic interactions, the behaviours displayed, and the level of conspecific tolerance varied among species. Discrete postures, non-contact and contact movements are described. Three of these were species-specific: push downs by C. johnstoni; inflated tail sweeping by C. novaeguineae; and, side head striking combined with tail wagging by C. porosus. The two long-snouted species (C. johnstoni and G. gangeticus avoided contact involving the head and often raised the head up out of the way during agonistic interactions. Several behaviours not associated with aggression are also described, including snout rubbing, raising the head up high while at rest, and the use of vocalizations. The two most aggressive species (C. porosus, C. novaeguineae appeared to form dominance hierarchies, whereas the less aggressive species did not. Interspecific differences in agonistic behaviour may reflect evolutionary divergence associated with morphology, ecology, general life history and responses to interspecific conflict in areas where multiple species have co-existed. Understanding species-specific traits in agonistic behaviour and social tolerance has implications for the controlled raising of different species of hatchlings for conservation, management or production purposes.

Structure and biological activity of endogenous and synthetic agonists of GPR119

Science.gov (United States)

Tyurenkov, I. N.; Ozerov, A. A.; Kurkin, D. V.; Logvinova, E. O.; Bakulin, D. A.; Volotova, E. V.; Borodin, D. D.

2018-02-01

A G-protein-coupled receptor, GPR119, is a promising pharmacological target for a new class of hypoglycaemic drugs with an original mechanism of action, namely, increase in the glucose-dependent incretin and insulin secretion. In 2005, the first ligands were found and in the subsequent years, a large number of GPR119 agonists were synthesized in laboratories in various countries; the safest and most promising agonists have entered phase I and II clinical trials as agents for the treatment of type 2 diabetes mellitus and obesity. The review describes the major endogenous GPR119 agonists and the main trends in the design and modification of synthetic structures for increasing the hypoglycaemic activity. The data on synthetic agonists are arranged according to the type of the central core of the molecules. The bibliography includes 104 references.

Interleukin-24 as a target cytokine of environmental aryl hydrocarbon receptor agonist exposure in the lung

Energy Technology Data Exchange (ETDEWEB)

Luo, Yueh-Hsia; Kuo, Yu-Chun; Tsai, Ming-Hsien; Ho, Chia-Chi; Tsai, Hui-Ti; Hsu, Chin-Yu; Chen, Yu-Cheng; Lin, Pinpin, E-mail: pplin@nhri.org.tw

2017-06-01

Exposure to environmental aryl hydrocarbon receptor (AhR) agonists, such as halogenated aromatic hydrocarbons and polycyclic aromatic hydrocarbons (PAHs), has great impacts on the development of various lung diseases. As emerging molecular targets for AhR agonists, cytokines may contribute to the inflammatory or immunotoxic effects of environmental AhR agonists. However, general cytokine expression may not specifically indicate environmental AhR agonist exposure. By comparing cytokine and chemokine expression profiles in human lung adenocarcinoma cell line CL5 treated with AhR agonists and the non-AhR agonist polychlorinated biphenyl (PCB) 39, we identified a target cytokine of environmental AhR agonist exposure of in the lungs. Thirteen cytokine and chemokine genes were altered in the AhR agonists-treated cells, but none were altered in the PCB39-treated cells. Interleukin (IL)-24 was the most highly induced gene among AhR-modulated cytokines. Cotreatment with AhR antagonist completely prevented IL-24 induction by AhR agonists in the CL5 cells. Knockdown AhR expression with short-hairpin RNA (shRNA) significantly reduced benzo[a]pyrene (BaP)-induced IL-24 mRNA levels. We further confirmed that gene transcription, but not mRNA stability, was involved in IL-24 upregulation by BaP. Particulate matter (PM) in the ambient air contains some PAHs and is reported to activate AhR. Oropharyngeal aspiration of PM significantly increased IL-24 levels in lung epithelia and in bronchoalveolar lavage fluid of mice 4 weeks after treatment. Thus, our data suggests that IL-24 is a pulmonary exposure target cytokine of environmental AhR agonists. - Graphical abstract: (A) Cytokine and chemokine gene expressions were examined in CL5 cells treated with AhR and non-AhR agonists. Thirteen cytokines and chemokines genes were altered in the AhR agonist-treated cells, but not in the non-AhR agonist-treated cells. IL-24 was the most highly induced gene among the AhR-modulated cytokines. (B

47 CFR 0.101 - Functions of the office.

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2010-10-01

... 47 Telecommunication 1 2010-10-01 2010-10-01 false Functions of the office. 0.101 Section 0.101 Telecommunication FEDERAL COMMUNICATIONS COMMISSION GENERAL COMMISSION ORGANIZATION Organization Office of Communications Business Opportunities § 0.101 Functions of the office. (a) The Office of Communications Business...

41 CFR 101-4.140 - Dissemination of policy.

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2010-07-01

... EDUCATION PROGRAMS OR ACTIVITIES RECEIVING FEDERAL FINANCIAL ASSISTANCE Introduction § 101-4.140... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Dissemination of policy. 101-4.140 Section 101-4.140 Public Contracts and Property Management Federal Property Management...

40 CFR 141.101 - Use of bottled water.

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2010-07-01

... 40 Protection of Environment 22 2010-07-01 2010-07-01 false Use of bottled water. 141.101 Section 141.101 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) WATER PROGRAMS (CONTINUED) NATIONAL PRIMARY DRINKING WATER REGULATIONS Use of Non-Centralized Treatment Devices § 141.101...

Do Agonistic Motives Matter More Than Anger? Three Studies of Cardiovascular Risk in Adolescents

Science.gov (United States)

Ewart, Craig K.; Elder, Gavin J.; Smyth, Joshua M.; Sliwinski, Martin J.; Jorgensen, Randall S.

2011-01-01

Objective Three motivational profiles have been associated with recurring psychological stress in low-income youth and young adults: Striving to control others (agonistic striving), striving to control the self (transcendence striving), and not asserting control (dissipated striving); Agonistic Striving has been associated with elevated ambulatory blood pressure during daily activities. Three studies tested the hypotheses that: (1) Agonistic Striving is associated with poor anger regulation, and (2) Agonistic Striving and poor anger regulation interactively elevate blood pressure. Design Motivational profiles, anger regulation, and ambulatory blood pressure were assessed in a multiethnic sample of 264 urban youth. Main outcome measures (1) Anger regulation/recovery during laboratory challenge; (2) anger / blood pressure during daily activities (48 hours). Results and conclusion Replication of the profiles in distant cities showed they occur with similar frequency across differences of region, race, and gender. Analyses controlling for body size, race, and gender revealed that individuals with the Agonistic Striving profile had higher ambulatory pressure, especially during social encounters. They became more openly angry and aggressive when challenged, but did not exhibit difficulty regulating anger in the laboratory, nor did they feel more angry during monitoring. However, individuals with the Agonistic Striving profile who did display poor anger regulation in the lab had the highest blood pressure; deficient self-regulatory capability amplified the positive association between Agonistic Striving and cardiovascular risk in both genders and all ethnic groups. Although anger is thought to increase cardiovascular risk, present findings suggest that anger and elevated blood pressure are co-effects of agonistic struggles to control others. PMID:21534673

Non-nucleotide Agonists Triggering P2X7 Receptor Activation and Pore Formation

Directory of Open Access Journals (Sweden)

Francesco Di Virgilio

2018-02-01

Full Text Available The P2X7 receptor (P2X7R is a ligand-gated plasma membrane ion channel belonging to the P2X receptor subfamily activated by extracellular nucleotides. General consensus holds that the physiological (and maybe the only agonist is ATP. However, scattered evidence generated over the last several years suggests that ATP might not be the only agonist, especially at inflammatory sites. Solid data show that NAD+ covalently modifies the P2X7R of mouse T lymphocytes, thus lowering the ATP threshold for activation. Other structurally unrelated agents have been reported to activate the P2X7R via a poorly understood mechanism of action: (a the antibiotic polymyxin B, possibly a positive allosteric P2X7R modulator, (b the bactericidal peptide LL-37, (c the amyloidogenic β peptide, and (d serum amyloid A. Some agents, such as Alu-RNA, have been suggested to activate the P2X7R acting on the intracellular N- or C-terminal domains. Mode of P2X7R activation by these non-nucleotide ligands is as yet unknown; however, these observations raise the intriguing question of how these different non-nucleotide ligands may co-operate with ATP at inflammatory or tumor sites. New information obtained from the cloning and characterization of the P2X7R from exotic mammalian species (e.g., giant panda and data from recent patch-clamp studies are strongly accelerating our understanding of P2X7R mode of operation, and may provide hints to the mechanism of activation of P2X7R by non-nucleotide ligands.

41 CFR 101-6.205-3 - Elementary and secondary schools.

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2010-07-01

... schools. 101-6.205-3 Section 101-6.205-3 Public Contracts and Property Management Federal Property...-Nondiscrimination in Programs Receiving Federal Financial Assistance § 101-6.205-3 Elementary and secondary schools. The requirements of §§ 101-6.205-1 and 101-6.205-2 with respect to any elementary or secondary school...

41 CFR 101-4.120 - Transfers of property.

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2010-07-01

... EDUCATION PROGRAMS OR ACTIVITIES RECEIVING FEDERAL FINANCIAL ASSISTANCE Introduction § 101-4.120 Transfers... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Transfers of property. 101-4.120 Section 101-4.120 Public Contracts and Property Management Federal Property Management...

41 CFR 101-1.103 - FPMR temporary regulations.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true FPMR temporary regulations. 101-1.103 Section 101-1.103 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101...

41 CFR 101-1.106 - Applicability of FPMR.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Applicability of FPMR. 101-1.106 Section 101-1.106 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101...

48 CFR 2922.101-3 - Reporting labor disputes.

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2010-10-01

... 48 Federal Acquisition Regulations System 7 2010-10-01 2010-10-01 false Reporting labor disputes. 2922.101-3 Section 2922.101-3 Federal Acquisition Regulations System DEPARTMENT OF LABOR SOCIOECONOMIC PROGRAMS APPLICATION OF LABOR LAWS TO GOVERNMENT ACQUISITIONS Basic Labor Policies 2922.101-3 Reporting...

41 CFR 101-4.540 - Advertising.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Advertising. 101-4.540... Employment in Education Programs or Activities Prohibited § 101-4.540 Advertising. A recipient shall not in any advertising related to employment indicate preference, limitation, specification, or...

41 CFR 101-39.002 - Applicability.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Applicability. 101-39.002 Section 101-39.002 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS AVIATION, TRANSPORTATION, AND MOTOR VEHICLES 39-INTERAGENCY FLEET...

41 CFR 101-39.205 - [Reserved

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2010-07-01

... FEDERAL PROPERTY MANAGEMENT REGULATIONS AVIATION, TRANSPORTATION, AND MOTOR VEHICLES 39-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.2-GSA Interagency Fleet Management System Services § 101-39.205 [Reserved] ... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true [Reserved] 101-39.205...

40 CFR 430.101 - Specialized definitions.

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2010-07-01

... 40 Protection of Environment 29 2010-07-01 2010-07-01 false Specialized definitions. 430.101 Section 430.101 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) EFFLUENT GUIDELINES....01 of this part shall apply to this subpart. (b) Noncorrugating medium furnish subdivision mills are...

49 CFR 212.101 - Program principles.

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2010-10-01

... 49 Transportation 4 2010-10-01 2010-10-01 false Program principles. 212.101 Section 212.101 Transportation Other Regulations Relating to Transportation (Continued) FEDERAL RAILROAD ADMINISTRATION... principles. (a) The purpose of the national railroad safety program is to promote safety in all areas of...

Dopamine agonist activity of EMD 23,448

Energy Technology Data Exchange (ETDEWEB)

Martin, G E; Pettibone, D J [Merck Sharp and Dohme Research Laboratories, West Point, Pennsylvania (USA). Dept. of Pharmacology

1985-01-01

EMD 23,448 was examined in tests of dopaminergic function and was found to be an atypical dopamine (DA) agonist. EMD 23,448 was a weak or inactive DA agonist when examined in tests of normal postsynaptic DA receptor function: production of stereotypy in the rat (ED/sub 50/ greater than sign 5.0 mg/kg.i.p.); production of emesis in beagles (minimum effective dose = 81..mu..g/kg i.v.); and, enhanced locomotor activity of the mouse (no excitation in doses <=50 mg/i.p.). Moreover, EMD 23,448 was relatively weak in competing for (/sup 3/H)-apomorphine binding to rat striatal membranes (Ki, 205 nM). On the other hand, this indolyl-3-butylamine did activate supersensitive postsynaptic DA receptors. Specifically, it elicited contralateral turning in rats with a unilateral 6-hydroxydopamine lesion of the substantia nigra (ED/sub 50/ value = 0.9 mg/kg) and did elicit stereotypy in rats given chronic daily haloperidol treatments. EMD 23,448 also exerted pharmacological effects in tests designed to measure activation of dopamine autoreceptors. It inhibited the ..gamma..-butyrolactone-induced increase in striatal dopa levels (ED/sub 50/ = 1 mg/kg i.p.) and produced a dose-related fall in the locomotor activity of the mouse. The results are discussed and contrasted with data derived for apomorphine and the putatively selective autoreceptor agonist (+-)-3-PPP.

41 CFR 101-26.000 - Scope of part.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Scope of part. 101-26.000 Section 101-26.000 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND PROGRAM § 101-26...

41 CFR 101-1.100 - Scope of subpart.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Scope of subpart. 101-1.100 Section 101-1.100 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101-1.100...

41 CFR 101-26.607 - Billings.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Billings. 101-26.607 Section 101-26.607 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND PROGRAM 26.6...

41 CFR 101-26.301 - Applicability.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Applicability. 101-26.301 Section 101-26.301 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND PROGRAM 26.3...

41 CFR 101-26.504 - [Reserved

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true [Reserved] 101-26.504 Section 101-26.504 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND PROGRAM 26.5-GSA...

41 CFR 101-26.601 - [Reserved

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true [Reserved] 101-26.601 Section 101-26.601 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND PROGRAM 26.6...

9 CFR 101.2 - Administrative terminology.

Science.gov (United States)

2010-01-01

... toxic to microorganisms, e.g., antibiotics), or analogous products at any stage of production, shipment... 9 Animals and Animal Products 1 2010-01-01 2010-01-01 false Administrative terminology. 101.2 Section 101.2 Animals and Animal Products ANIMAL AND PLANT HEALTH INSPECTION SERVICE, DEPARTMENT OF...

47 CFR 101.1405 - Channeling plan.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false Channeling plan. 101.1405 Section 101.1405 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) SAFETY AND SPECIAL RADIO SERVICES FIXED MICROWAVE... Channeling plan. Each license shall have one spectrum block of 500 megahertz per geographic area that can be...

41 CFR 101-4.310 - Recruitment.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Recruitment. 101-4.310... Admission and Recruitment Prohibited § 101-4.310 Recruitment. (a) Nondiscriminatory recruitment. A recipient... recruitment and admission of students. A recipient may be required to undertake additional recruitment efforts...

41 CFR 101-4.500 - Employment.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Employment. 101-4.500... Employment in Education Programs or Activities Prohibited § 101-4.500 Employment. (a) General. (1) No person... subjected to discrimination in employment, or recruitment, consideration, or selection therefor, whether...

41 CFR 101-6.202 - Purpose.

Science.gov (United States)

2010-07-01

... FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 6-MISCELLANEOUS REGULATIONS 6.2-Nondiscrimination in Programs Receiving Federal Financial Assistance § 101-6.202 Purpose. The purpose of this subpart is to... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Purpose. 101-6.202...

Dopamine agonists and risk: impulse control disorders in Parkinson's disease.

Science.gov (United States)

Voon, Valerie; Gao, Jennifer; Brezing, Christina; Symmonds, Mkael; Ekanayake, Vindhya; Fernandez, Hubert; Dolan, Raymond J; Hallett, Mark

2011-05-01

Impulse control disorders are common in Parkinson's disease, occurring in 13.6% of patients. Using a pharmacological manipulation and a novel risk taking task while performing functional magnetic resonance imaging, we investigated the relationship between dopamine agonists and risk taking in patients with Parkinson's disease with and without impulse control disorders. During functional magnetic resonance imaging, subjects chose between two choices of equal expected value: a 'Sure' choice and a 'Gamble' choice of moderate risk. To commence each trial, in the 'Gain' condition, individuals started at $0 and in the 'Loss' condition individuals started at -$50 below the 'Sure' amount. The difference between the maximum and minimum outcomes from each gamble (i.e. range) was used as an index of risk ('Gamble Risk'). Sixteen healthy volunteers were behaviourally tested. Fourteen impulse control disorder (problem gambling or compulsive shopping) and 14 matched Parkinson's disease controls were tested ON and OFF dopamine agonists. Patients with impulse control disorder made more risky choices in the 'Gain' relative to the 'Loss' condition along with decreased orbitofrontal cortex and anterior cingulate activity, with the opposite observed in Parkinson's disease controls. In patients with impulse control disorder, dopamine agonists were associated with enhanced sensitivity to risk along with decreased ventral striatal activity again with the opposite in Parkinson's disease controls. Patients with impulse control disorder appear to have a bias towards risky choices independent of the effect of loss aversion. Dopamine agonists enhance sensitivity to risk in patients with impulse control disorder possibly by impairing risk evaluation in the striatum. Our results provide a potential explanation of why dopamine agonists may lead to an unconscious bias towards risk in susceptible individuals.

41 CFR 101-27.404 - Review of items.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Review of items. 101-27.404 Section 101-27.404 Public Contracts and Property Management Federal Property Management...-Elimination of Items From Inventory § 101-27.404 Review of items. Except for standby or reserve stocks, items...

41 CFR 101-39.4900 - Scope of subpart.

Science.gov (United States)

2010-07-01

...-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.49-Forms § 101-39.4900 Scope of subpart. This subpart provides the... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Scope of subpart. 101-39.4900 Section 101-39.4900 Public Contracts and Property Management Federal Property Management...

19 CFR 101.2 - Authority of Customs officers.

Science.gov (United States)

2010-04-01

... 19 Customs Duties 1 2010-04-01 2010-04-01 false Authority of Customs officers. 101.2 Section 101.2 Customs Duties U.S. CUSTOMS AND BORDER PROTECTION, DEPARTMENT OF HOMELAND SECURITY; DEPARTMENT OF THE TREASURY GENERAL PROVISIONS § 101.2 Authority of Customs officers. (a) Supremacy of delegated authority...

Detection of glucocorticoid receptor agonists in effluents from sewage treatment plants in Japan.

Science.gov (United States)

Suzuki, Go; Sato, Kentaro; Isobe, Tomohiko; Takigami, Hidetaka; Brouwer, Abraham; Nakayama, Kei

2015-09-15

Glucocorticoids (GCs) are widely used as anti-inflammatory drugs. Our previous study demonstrated that several GCs such as cortisol and dexamethasone (Dex) were frequently detected in effluents collected from Japanese sewage treatment plants (STPs) in 2012. In this study, we used the GC-Responsive Chemical-Activated LUciferase gene eXpression (GR-CALUX) assay to elucidate GC receptor (GR) agonistic activities of ten pure synthetic GCs and selected STP effluents in Japan for assessment of the risks associated with the presence of GR agonists. The tested GCs demonstrated dose-dependent agonistic effects in the GR-CALUX assay and their EC50 values were calculated for estimation of relative potencies (REPs) compared to Dex. The GR agonistic potency was in the rank of: clobetasol propionate > clobetasone butyrate > betamethasone 17-valerate > difluprednate > betamethasone 17,21-dipropionate > Dex > betamethasone > 6α-methylprednisolone > prednisolone > cortisol. The GR agonistic activity in STP effluents as measured in Dex-equivalent (Dex-EQ) activities ranged from effluents in Japan. Copyright © 2015 Elsevier B.V. All rights reserved.

Platelet-activating factor receptor agonists mediate xeroderma pigmentosum A photosensitivity.

Science.gov (United States)

Yao, Yongxue; Harrison, Kathleen A; Al-Hassani, Mohammed; Murphy, Robert C; Rezania, Samin; Konger, Raymond L; Travers, Jeffrey B

2012-03-16

To date, oxidized glycerophosphocholines (Ox-GPCs) with platelet-activating factor (PAF) activity produced non-enzymatically have not been definitively demonstrated to mediate any known disease processes. Here we provide evidence that these Ox-GPCs play a pivotal role in the photosensitivity associated with the deficiency of the DNA repair protein xeroderma pigmentosum type A (XPA). It should be noted that XPA-deficient cells are known to have decreased antioxidant defenses. These studies demonstrate that treatment of human XPA-deficient fibroblasts with the pro-oxidative stressor ultraviolet B (UVB) radiation resulted in increased reactive oxygen species and PAF receptor (PAF-R) agonistic activity in comparison with gene-corrected cells. The UVB irradiation-generated PAF-R agonists were inhibited by antioxidants. UVB irradiation of XPA-deficient (Xpa-/-) mice also resulted in increased PAF-R agonistic activity and skin inflammation in comparison with control mice. The increased UVB irradiation-mediated skin inflammation and TNF-α production in Xpa-/- mice were blocked by systemic antioxidants and by PAF-R antagonists. Structural characterization of PAF-R-stimulating activity in UVB-irradiated XPA-deficient fibroblasts using mass spectrometry revealed increased levels of sn-2 short-chain Ox-GPCs along with native PAF. These studies support a critical role for PAF-R agonistic Ox-GPCs in the pathophysiology of XPA photosensitivity.

Long-term outcome of patients with macroprolactinomas initially treated with dopamine agonists

NARCIS (Netherlands)

Kars, Marleen; Pereira, Alberto M.; Smit, Johannes W.; Romijn, Johannes A.

2009-01-01

Dopamine agonists are the first line therapy for the treatment of prolactinomas. The aim of this study was to assess the outcome of macroprolactinomas during long-term follow-up after initial treatment with dopamine agonists. Retrospective follow-up study. We included 72 consecutive patients (age

An orphan G-protein-coupled receptor causes human gigantism and/or acromegaly: Molecular biology and clinical correlations.

Science.gov (United States)

Trivellin, Giampaolo; Hernández-Ramírez, Laura C; Swan, Jeremy; Stratakis, Constantine A

2018-04-01

X-linked acrogigantism (X-LAG) is a recently described form of familial or sporadic pituitary gigantism characterized by very early onset GH and IGF-1 excess, accelerated growth velocity, gigantism and/or acromegaloid features. Germline or somatic microduplications of the Xq26.3 chromosomal region, invariably involving the GPR101 gene, constitute the genetic defect leading to X-LAG. GPR101 encodes a class A G protein-coupled receptor that activates the 3',5'-cyclic adenosine monophosphate signaling pathway. Highly expressed in the central nervous system, the main physiological function and ligand of GPR101 remain unknown, but it seems to play a role in the normal development of the GHRH-GH axis. Early recognition of X-LAG cases is imperative because these patients require clinical management that differs from that of other patients with acromegaly or gigantism. Medical treatment with pegvisomant seems to be the best approach, since X-LAG tumors are resistant to the treatment with somatostatin analogues and dopamine agonists; surgical cure requires near-total hypophysectomy. Currently, the efforts of our research focus on the identification of GPR101 ligands; in addition, the long-term follow-up of X-LAG patients is of extreme interest as this is expected to lead to better understanding of GPR101 effects on human pathophysiology. Copyright © 2018. Published by Elsevier Ltd.

The therapeutic potential of nicotinic acetylcholine receptor agonists for pain control.

Science.gov (United States)

Decker, M W; Meyer, M D; Sullivan, J P

2001-10-01

Due to the limitations of currently available analgesics, a number of novel alternatives are currently under investigation, including neuronal nicotinic acetylcholine receptor (nAChR) agonists. During the 1990s, the discovery of the antinociceptive properties of the potent nAChR agonist epibatidine in rodents sparked interest in the analgesic potential of this class of compounds. Although epibatidine also has several mechanism-related toxicities, the identification of considerable nAChR diversity suggested that the toxicities and therapeutic actions of the compound might be mediated by distinct receptor subtypes. Consistent with this view, a number of novel nAChR agonists with antinociceptive activity and improved safety profiles in preclinical models have now been identified, including A-85380, ABT-594, DBO-83, SIB-1663 and RJR-2403. Of these, ABT-594 is the most advanced and is currently in Phase II clinical evaluation. Nicotinically-mediated antinociception has been demonstrated in a variety of rodent pain models and is likely mediated by the activation of descending inhibitory pathways originating in the brainstem with the predominant high-affinity nicotine site in brain, the alpha4beta2 subtype, playing a critical role. Thus, preclinical findings suggest that nAChR agonists have the potential to be highly efficacious treatments in a variety of pain states. However, clinical proof-of-principle studies will be required to determine if nAChR agonists are active in pathological pain.

47 CFR 101.1425 - RF safety.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false RF safety. 101.1425 Section 101.1425 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) SAFETY AND SPECIAL RADIO SERVICES FIXED MICROWAVE... safety. MVDDS stations in the 12.2-12.7 GHz frequency band do not operate with output powers that equal...

A neurokinin 3 receptor-selective agonist accelerates pulsatile luteinizing hormone secretion in lactating cattle.

Science.gov (United States)

Nakamura, Sho; Wakabayashi, Yoshihiro; Yamamura, Takashi; Ohkura, Satoshi; Matsuyama, Shuichi

2017-07-01

Pulsatile gonadotropin-releasing hormone (GnRH) secretion, which is indispensable for follicular development, is suppressed in lactating dairy and beef cattle. Neurokinin B (NKB) neurons in the arcuate nucleus of the hypothalamus are considered to play an essential role in generating the pulsatile mode of GnRH/luteinizing hormone (LH) secretion. The present study aimed to clarify the role of NKB-neurokinin 3 receptor (NK3R) signaling in the pulsatile pattern of GnRH/gonadotropin secretion in postpartum lactating cattle. We examined the effects of the administration of an NK3R-selective agonist, senktide, on gonadotropin secretion in lactating cattle. The lactating cattle, at approximately 7 days postpartum, were intravenously infused with senktide (30 or 300 nmol/min) or vehicle for 24 h. The administration of 30 or 300 nmol/min senktide significantly increased LH pulse frequency compared to in the control group during 0-4 or 20-24 h after infusion, respectively. Moreover, LH and follicle-stimulating hormone levels were gradually increased by 300 nmol/min administration of senktide during the 0-4-h sampling period. Ultrasonography of the ovaries was performed to identify the first postpartum ovulation in senktide-administered lactating cattle. The interval from calving to first postpartum ovulation was significantly shorter in the 300 nmol/min senktide-administered group than in the control group. Taken together, these findings suggest that senktide infusion elicits an increase in LH pulse frequency that may stimulate follicular development and, in turn, induce the first postpartum ovulation in lactating cattle. © The Authors 2017. Published by Oxford University Press on behalf of Society for the Study of Reproduction. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

Effects of (-)-S-2,8-dimethyl-3-methylene-1-oxa-8-azaspiro[4,5]decane L-tartrate monohydrate (YM796), a novel muscarinic agonist, on disturbance of passive avoidance learning behavior in drug-treated and senescence-accelerated mice.

Science.gov (United States)

Suzuki, M; Yamaguchi, T; Ozawa, Y; Ohyama, M; Yamamoto, M

1995-11-01

Effects of YM796 (-)-S-2,8-dimethyl-3-methylene-1-oxa-8-azaspiro[4,5]decane L-tartrate monohydrate; a novel muscarinic agonist, were observed on disturbance of passive avoidance learning behavior in drug- (protein synthesis inhibitor and anticholinergic drugs) treated and senescence-accelerated mice in comparison with those of a muscarinic agonist (AF102B) and acetylcholinesterase inhibitors (E2020 (1-benzyl-4-[(5,6-dimethoxy-1-indanone-2-yl) methyl] piperidene hydrochloride), NIK247 [9-amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta(b)-quinoline monohydrate hydrochloride], THA (9-amino-1,2,3,4-tetrahydroacridine) and physostigmine). All tested drugs administered before training significantly prolonged the shortened latency of step-through induced by the protein synthesis inhibitor cycloheximide (150 mg/kg s.c.). This shortened latency was also significantly prolonged when YM796 was administered immediately after training, but not when administered before the test trial. The ameliorating effect of YM796 on the impairment in learning behavior by cycloheximide was significantly suppressed by pirenzepine (0.1 micrograms/mouse i.c.v.). When administered before training, all test drugs prolonged the shortened latency of step-through induced by treatment with the anticholinergic drugs [scopolamine (1 mg/kg s.c.) and hemicholinium-3 (0.3 microgram/mouse i.c.v.)], suggesting that they ameliorated the impairment of learning behavior. This shortened latency in scopolamine-treated mice was also significantly prolonged by YM796, AF102B, E2020, NIK247 and physostigmine when administered immediately after training, but not when administered before the test trial. The pharmacological actions of YM796 administered immediately after training and before the test trial in hemicholinium-3-treated mice were similar to those in scopolamine-treated mice.(ABSTRACT TRUNCATED AT 250 WORDS)

Silencing of ACO decreases reproduction and energy metabolism in triazophos-treated female brown plant hoppers, Nilaparvata lugens Stål (Hemiptera: Delphacidae).

Science.gov (United States)

Liu, Zong-Yu; Jiang, Yi-Ping; Li, Lei; You, Lin-Lin; Wu, You; Xu, Bin; Ge, Lin-Quan; Wu, Jin-Cai

2016-03-01

The brown plant hopper (BPH), Nilaparvata lugens Stål (Hemiptera: Delphacidae), is a major pest affecting rice in Asia, and outbreaks of this pest are closely linked to pesticide-induced stimulation of reproduction. Therefore, the BPH is a classic example of a resurgent pest. However, the effects of different genes on the regulation of pesticide-induced reproductive stimulation in the BPH are unclear. In this study, the regulatory effects of acyl-coenzyme A oxidase (ACO) on the reproduction and biochemistry of the BPH were investigated with gene silencing. The number of eggs laid per female by triazophos (TZP)+dsACO BPH females was significantly lower than those of TZP-treated (without ACO silencing) or TZP+GFP females (negative control), with the number of eggs decreasing by 30.8% (from 529.5 to 366.3) and 32.0% (from 540.5 to 366.3), respectively. The preoviposition period, oviposition period, and longevity of the TZP-treated females were also influenced by dsACO treatment. Additionally, the amounts of crude fat, protein, and some fatty acids (oleic acid, palmitic acid, linoleic acid, stearic acid, and myristoleic acid) in TZP+dsACO females were significantly lower than in TZP-treated females. Thus, ACO is one of the key genes regulating the TZP-induced stimulation of reproduction in BPH females. Copyright © 2015 Elsevier Inc. All rights reserved.

29 CFR 101.11 - Administrative law judge's decision.

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2010-07-01

... 29 Labor 2 2010-07-01 2010-07-01 false Administrative law judge's decision. 101.11 Section 101.11... Practice Cases Under Section 10 (a) to (i) of the Act and Telegraph Merger Act Cases § 101.11 Administrative law judge's decision. (a) At the conclusion of the hearing the administrative law judge prepares a...

42 CFR 84.101 - Man test 5; requirements.

Science.gov (United States)

2010-10-01

... 42 Public Health 1 2010-10-01 2010-10-01 false Man test 5; requirements. 84.101 Section 84.101 Public Health PUBLIC HEALTH SERVICE, DEPARTMENT OF HEALTH AND HUMAN SERVICES OCCUPATIONAL SAFETY AND HEALTH RESEARCH AND RELATED ACTIVITIES APPROVAL OF RESPIRATORY PROTECTIVE DEVICES Self-Contained Breathing Apparatus § 84.101 Man test 5; requirements....

Anisotropic chemical etching of semipolar {101-bar 1-bar}/{101-bar +1} ZnO crystallographic planes: polarity versus dangling bonds

International Nuclear Information System (INIS)

Palacios-Lidon, E; Perez-GarcIa, B; Colchero, J; Vennegues, P; Zuniga-Perez, J; Munoz-Sanjose, V

2009-01-01

ZnO thin films grown by metal-organic vapor phase epitaxy along the nonpolar [112-bar] direction and exhibiting semipolar {101-bar 1-bar}/{101-bar +1} facets have been chemically etched with HCl. In order to get an insight into the influence of the ZnO wurtzite structure in the chemical reactivity of the material, Kelvin probe microscopy and convergent beam electron diffraction have been employed to unambiguously determine the absolute polarity of the facets, showing that {101-bar +1} facets are unstable upon etching in an HCl solution and transform into (000+1)/{101-bar 1-bar} planes. In contrast, {101-bar 1-bar} undergo homogeneous chemical etching perpendicular to the initial crystallographic plane. The observed etching behavior has been explained in terms of surface oxygen dangling bond density, suggesting that the macroscopic polarity plays a secondary role in the etching process.

Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist.

Science.gov (United States)

Presley, Chaela; Abidi, Ammaar; Suryawanshi, Satyendra; Mustafa, Suni; Meibohm, Bernd; Moore, Bob M

2015-08-01

Cannabinoid receptor 2 agonists and inverse agonists are emerging as new therapeutic options for a spectrum of autoimmune-related disease. Of particular interest, is the ability of CB2 ligands to regulate microglia function in neurodegenerative diseases and traumatic brain injury. We have previously reported the receptor affinity of 3',5'-dichloro-2,6-dihydroxy-biphenyl-4-yl)-phenyl-methanone (SMM-189) and the characterization of the beneficial effects of SMM-189 in the mouse model of mild traumatic brain injury. Herein, we report the further characterization of SMM-189 as a potent and selective CB2 inverse agonist, which acts as a noncompetitive inhibitor of CP 55,940. The ability of SMM-189 to regulate microglial activation, in terms of chemokine expression and cell morphology, has been determined. Finally, we have determined that SMM-189 possesses acceptable biopharmaceutical properties indicating that the triaryl class of CB2 inverse agonists are viable compounds for continued preclinical development for the treatment of neurodegenerative disorders and traumatic brain injury.

41 CFR 101-30.202 - Policies.

Science.gov (United States)

2010-07-01

... associated with, but never included as a part of the national stock number. These management codes or symbols... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Policies. 101-30.202 Section 101-30.202 Public Contracts and Property Management Federal Property Management Regulations System...

17 CFR 300.101 - Individual accounts.

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2010-04-01

... 17 Commodity and Securities Exchanges 3 2010-04-01 2010-04-01 false Individual accounts. 300.101... Customers of Sipc Members § 300.101 Individual accounts. (a) Except as otherwise provided in these rules... deemed his individual accounts, shall be combined so as to constitute a single account of a separate...

41 CFR 101-4.510 - Recruitment.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Recruitment. 101-4.510... Employment in Education Programs or Activities Prohibited § 101-4.510 Recruitment. (a) Nondiscriminatory recruitment and hiring. A recipient shall not discriminate on the basis of sex in the recruitment and hiring...

41 CFR 101-29.210 - Product.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Product. 101-29.210... FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 29-FEDERAL PRODUCT DESCRIPTIONS 29.2-Definitions § 101-29.210 Product. The term product is any end item, either manufactured or produced, and also...

18 CFR 1304.101 - Nonnavigable houseboats.

Science.gov (United States)

2010-04-01

.... 1304.101 Section 1304.101 Conservation of Power and Water Resources TENNESSEE VALLEY AUTHORITY APPROVAL OF CONSTRUCTION IN THE TENNESSEE RIVER SYSTEM AND REGULATION OF STRUCTURES AND OTHER ALTERATIONS... on a boat hull or on two or more pontoons; (2) Equipped with a motor and rudder controls located at a...

48 CFR 50.101-1 - Authority.

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2010-10-01

... 48 Federal Acquisition Regulations System 1 2010-10-01 2010-10-01 false Authority. 50.101-1... EXTRAORDINARY CONTRACTUAL ACTIONS AND THE SAFETY ACT Extraordinary Contractual Actions 50.101-1 Authority. (a... following agencies to exercise the authority conferred by Pub. L. 85-804 and to delegate it to other...

41 CFR 101-4.405 - Housing.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Housing. 101-4.405... Education Programs or Activities Prohibited § 101-4.405 Housing. (a) Generally. A recipient shall not, on... offer different services or benefits related to housing, except as provided in this section (including...

41 CFR 101-8.717 - Mediation.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Mediation. 101-8.717... FINANCIAL ASSISTANCE 8.7-Discrimination Prohibited on the Basis of Age § 101-8.717 Mediation. (a) GSA promptly refers to the mediation agency designated by the Secretary, HHS, all sufficient complaints that...

Interactions of dopaminergic agonists and antagonists with dopaminergic D3 binding sites in rat striatum. Evidence that [3H]dopamine can label a high affinity agonist-binding state of the D1 dopamine receptor

International Nuclear Information System (INIS)

Leff, S.E.; Creese, I.

1985-01-01

The interactions of dopaminergic agonists and antagonists with 3 H-agonist labeled D3 dopaminergic binding sites of rat striatum have been characterized by radioligand-binding techniques. When the binding of [ 3 H]dopamine and [ 3 H]apomorphine to D2 dopamine receptors is blocked by the inclusion of D2 selective concentrations of unlabeled spiroperidol or domperidone, these ligands appear to label selectively the previously termed D3 binding site. Antagonist/[ 3 H]dopamine competition curves are of uniformly steep slope (nH . 1.0), suggesting the presence of a single D3 binding site. The relative potencies of antagonists to inhibit D3 specific [ 3 H]dopamine binding are significantly correlated with their potencies to block D1 dopamine receptors as measured by the inhibition of both dopamine-stimulated adenylate cyclase and [ 3 H]flupentixol-binding activities. The affinities of agonists to inhibit D3 specific [ 3 H]dopamine binding are also correlated with estimates of these agonists affinities for the high affinity binding component of agonist/[ 3 H]flupentixol competition curves. Both D3 specific [ 3 H] dopamine binding and the high affinity agonist-binding component of dopamine/[ 3 H]flupentixol competition curves show a similar sensitivity to guanine nucleotides. Taken together, these data strongly suggest that the D3 binding site is related to a high affinity agonist-binding state of the D1 dopamine receptor

Systematic review: cardiovascular safety profile of 5-HT(4) agonists developed for gastrointestinal disorders.

Science.gov (United States)

Tack, J; Camilleri, M; Chang, L; Chey, W D; Galligan, J J; Lacy, B E; Müller-Lissner, S; Quigley, E M M; Schuurkes, J; De Maeyer, J H; Stanghellini, V

2012-04-01

The nonselective 5-HT(4) receptor agonists, cisapride and tegaserod have been associated with cardiovascular adverse events (AEs). To perform a systematic review of the safety profile, particularly cardiovascular, of 5-HT(4) agonists developed for gastrointestinal disorders, and a nonsystematic summary of their pharmacology and clinical efficacy. Articles reporting data on cisapride, clebopride, prucalopride, mosapride, renzapride, tegaserod, TD-5108 (velusetrag) and ATI-7505 (naronapride) were identified through a systematic search of the Cochrane Library, Medline, Embase and Toxfile. Abstracts from UEGW 2006-2008 and DDW 2008-2010 were searched for these drug names, and pharmaceutical companies approached to provide unpublished data. Retrieved articles on pharmacokinetics, human pharmacodynamics and clinical data with these 5-HT(4) agonists, are reviewed and summarised nonsystematically. Articles relating to cardiac safety and tolerability of these agents, including any relevant case reports, are reported systematically. Two nonselective 5-HT(4) agonists had reports of cardiovascular AEs: cisapride (QT prolongation) and tegaserod (ischaemia). Interactions with, respectively, the hERG cardiac potassium channel and 5-HT(1) receptor subtypes have been suggested to account for these effects. No cardiovascular safety concerns were reported for the newer, selective 5-HT(4) agonists prucalopride, velusetrag, naronapride, or for nonselective 5-HT(4) agonists with no hERG or 5-HT(1) affinity (renzapride, clebopride, mosapride). 5-HT(4) agonists for GI disorders differ in chemical structure and selectivity for 5-HT(4) receptors. Selectivity for 5-HT(4) over non-5-HT(4) receptors may influence the agent's safety and overall risk-benefit profile. Based on available evidence, highly selective 5-HT(4) agonists may offer improved safety to treat patients with impaired GI motility. © 2012 Blackwell Publishing Ltd.

Systematic review: cardiovascular safety profile of 5-HT4 agonists developed for gastrointestinal disorders

Science.gov (United States)

Tack, J; Camilleri, M; Chang, L; Chey, W D; Galligan, J J; Lacy, B E; Müller-Lissner, S; Quigley, E M M; Schuurkes, J; Maeyer, J H; Stanghellini, V

2012-01-01

Summary Background The nonselective 5-HT4 receptor agonists, cisapride and tegaserod have been associated with cardiovascular adverse events (AEs). Aim To perform a systematic review of the safety profile, particularly cardiovascular, of 5-HT4 agonists developed for gastrointestinal disorders, and a nonsystematic summary of their pharmacology and clinical efficacy. Methods Articles reporting data on cisapride, clebopride, prucalopride, mosapride, renzapride, tegaserod, TD-5108 (velusetrag) and ATI-7505 (naronapride) were identified through a systematic search of the Cochrane Library, Medline, Embase and Toxfile. Abstracts from UEGW 2006–2008 and DDW 2008–2010 were searched for these drug names, and pharmaceutical companies approached to provide unpublished data. Results Retrieved articles on pharmacokinetics, human pharmacodynamics and clinical data with these 5-HT4 agonists, are reviewed and summarised nonsystematically. Articles relating to cardiac safety and tolerability of these agents, including any relevant case reports, are reported systematically. Two nonselective 5-HT4 agonists had reports of cardiovascular AEs: cisapride (QT prolongation) and tegaserod (ischaemia). Interactions with, respectively, the hERG cardiac potassium channel and 5-HT1 receptor subtypes have been suggested to account for these effects. No cardiovascular safety concerns were reported for the newer, selective 5-HT4 agonists prucalopride, velusetrag, naronapride, or for nonselective 5-HT4 agonists with no hERG or 5-HT1 affinity (renzapride, clebopride, mosapride). Conclusions 5-HT4 agonists for GI disorders differ in chemical structure and selectivity for 5-HT4 receptors. Selectivity for 5-HT4 over non-5-HT4 receptors may influence the agent's safety and overall risk–benefit profile. Based on available evidence, highly selective 5-HT4 agonists may offer improved safety to treat patients with impaired GI motility. PMID:22356640

Genetics 101 --The Hereditary Material of Life

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... of this page please turn Javascript on. Feature: Genetics 101 Genetics 101 — The Hereditary Material of Life Past Issues / Summer 2013 Table of Contents Genetics is the study of heredity, the process in ...

In silico discovery of novel Retinoic Acid Receptor agonist structures

Directory of Open Access Journals (Sweden)

Samuels Herbert H

2001-06-01

Full Text Available Abstract Background Several Retinoic Acid Receptors (RAR agonists have therapeutic activity against a variety of cancer types; however, unacceptable toxicity profiles have hindered the development of drugs. RAR agonists presenting novel structural and chemical features could therefore open new avenues for the discovery of leads against breast, lung and prostate cancer or leukemia. Results We have analysed the induced fit of the active site residues upon binding of a known ligand. The derived binding site models were used to dock over 150,000 molecules in silico (or virtually to the structure of the receptor with the Internal Coordinates Mechanics (ICM program. Thirty ligand candidates were tested in vitro. Conclusions Two novel agonists resulting from the predicted receptor model were active at 50 nM. One of them displays novel structural features which may translate into the development of new ligands for cancer therapy.

The convulsive and electroencephalographic changes produced by nonpeptidic delta-opioid agonists in rats: comparison with pentylenetetrazol.

Science.gov (United States)

Jutkiewicz, Emily M; Baladi, Michelle G; Folk, John E; Rice, Kenner C; Woods, James H

2006-06-01

delta-Opioid agonists produce convulsions and antidepressant-like effects in rats. It has been suggested that the antidepressant-like effects are produced through a convulsant mechanism of action either through overt convulsions or nonconvulsive seizures. This study evaluated the convulsive and seizurogenic effects of nonpeptidic delta-opioid agonists at doses that previously were reported to produce antidepressant-like effects. In addition, delta-opioid agonist-induced electroencephalographic (EEG) and behavioral changes were compared with those produced by the chemical convulsant pentylenetetrazol (PTZ). For these studies, EEG changes were recorded using a telemetry system before and after injections of the delta-opioid agonists [(+)-4-[(alphaR)-alpha-[(2S,5R)-2,5-dimethyl-4-(2-propenyl)-1-piperazinyl]-(3-methoxyphenyl)methyl]-N,N-diethylbenz (SNC80) and [(+)-4-[alpha(R)-alpha-[(2S,5R)-2,5-dimethyl-4-(2-propenyl)-1-piperazinyl]-(3-hydroxyphenyl)methyl]-N,N-diethylbenzamide [(+)-BW373U86]. Acute administration of nonpeptidic delta-opioid agonists produced bilateral ictal and paroxysmal spike and/or sharp wave discharges. delta-Opioid agonists produced brief changes in EEG recordings, and tolerance rapidly developed to these effects; however, PTZ produced longer-lasting EEG changes that were exacerbated after repeated administration. Studies with antiepileptic drugs demonstrated that compounds used to treat absence epilepsy blocked the convulsive effects of nonpeptidic delta-opioid agonists. Overall, these data suggest that delta-opioid agonist-induced EEG changes are not required for the antidepressant-like effects of these compounds and that neural circuitry involved in absence epilepsy may be related to delta-opioid agonist-induced convulsions. In terms of therapeutic development, these data suggest that it may be possible to develop delta-opioid agonists devoid of convulsive properties.

Magnetic permeability of stainless steel for use in accelerator beam transport systems

International Nuclear Information System (INIS)

Wilson, N.G.; Bunch, P.

1991-01-01

High-vacuum beam transport tubes are being designed for use in an accelerator under development at Los Alamos. In areas such as weld-heat-affected zones, the tubes will require localized magnetic permeability of less than 1.02. Seven austenitic stainless steel candidates, 304L, 310, 316L, 317LN, 20Cb-3, Nitronic 33, and Nitronic 40, have been evaluated to determine their permeability in cold-worked, annealed, and weld-affected zones. 310 and 20Cb-3 showed permeability after welding of less than 1.01. 1 ref., 1 fig., 1 tab

PPAR Agonists and Metabolic Syndrome: An Established Role?

Directory of Open Access Journals (Sweden)

Margherita Botta

2018-04-01

Full Text Available Therapeutic approaches to metabolic syndrome (MetS are numerous and may target lipoproteins, blood pressure or anthropometric indices. Peroxisome proliferator-activated receptors (PPARs are involved in the metabolic regulation of lipid and lipoprotein levels, i.e., triglycerides (TGs, blood glucose, and abdominal adiposity. PPARs may be classified into the α, β/δ and γ subtypes. The PPAR-α agonists, mainly fibrates (including newer molecules such as pemafibrate and omega-3 fatty acids, are powerful TG-lowering agents. They mainly affect TG catabolism and, particularly with fibrates, raise the levels of high-density lipoprotein cholesterol (HDL-C. PPAR-γ agonists, mainly glitazones, show a smaller activity on TGs but are powerful glucose-lowering agents. Newer PPAR-α/δ agonists, e.g., elafibranor, have been designed to achieve single drugs with TG-lowering and HDL-C-raising effects, in addition to the insulin-sensitizing and antihyperglycemic effects of glitazones. They also hold promise for the treatment of non-alcoholic fatty liver disease (NAFLD which is closely associated with the MetS. The PPAR system thus offers an important hope in the management of atherogenic dyslipidemias, although concerns regarding potential adverse events such as the rise of plasma creatinine, gallstone formation, drug–drug interactions (i.e., gemfibrozil and myopathy should also be acknowledged.

Suppression of atherosclerosis by synthetic REV-ERB agonist

Energy Technology Data Exchange (ETDEWEB)

Sitaula, Sadichha [Department of Molecular Therapeutics, The Scripps Research Institute, Jupiter, FL 33458 (United States); Billon, Cyrielle [Department of Pharmacological & Physiological Science, Saint Louis University School of Medicine, St. Louis, MO 63104 (United States); Kamenecka, Theodore M.; Solt, Laura A. [Department of Molecular Therapeutics, The Scripps Research Institute, Jupiter, FL 33458 (United States); Burris, Thomas P., E-mail: burristp@slu.edu [Department of Pharmacological & Physiological Science, Saint Louis University School of Medicine, St. Louis, MO 63104 (United States)

2015-05-08

The nuclear receptors for heme, REV-ERBα and REV-ERBβ, play important roles in the regulation of metabolism and inflammation. Recently it was demonstrated that reduced REV-ERBα expression in hematopoetic cells in LDL receptor null mice led to increased atherosclerosis. We sought to determine if synthetic REV-ERB agonists that we have developed might have the ability to suppress atherosclerosis in this model. A previously characterized synthetic REV-ERB agonist, SR9009, was used to determine if activation of REV-ERB activity would affect atherosclerosis in LDL receptor deficient mice. Atherosclerotic plaque size was significantly reduced (p < 0.05) in mice administered SR9009 (100 mg/kg) for seven weeks compared to control mice (n = 10 per group). SR9009 treatment of bone marrow-derived mouse macrophages (BMDM) reduced the polarization of BMDMs to proinflammatory M1 macrophage while increasing the polarization of BMDMs to anti-inflammatory M2 macrophages. Our results suggest that pharmacological targeting of REV-ERBs may be a viable therapeutic option for treatment of atherosclerosis. - Highlights: • Synthetic REV-ERB agonist treatment reduced atherosclerosis in a mouse model. • Pharmacological activation of REV-ERB decreased M1 macrophage polarization. • Pharmacological activation of REV-ERB increased M2 macrophage polarization.

Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.

Directory of Open Access Journals (Sweden)

Yiyi Sun

Full Text Available Adiponectin, the adipose-derived hormone, plays an important role in the suppression of metabolic disorders that can result in type 2 diabetes, obesity, and atherosclerosis. It has been shown that up-regulation of adiponectin or adiponectin receptor has a number of therapeutic benefits. Given that it is hard to convert the full size adiponectin protein into a viable drug, adiponectin receptor agonists could be designed or identified using high-throughput screening. Here, we report on the development of a two-step screening process to identify adiponectin agonists. First step, we developed a high throughput screening assay based on fluorescence polarization to identify adiponectin ligands. The fluorescence polarization assay reported here could be adapted to screening against larger small molecular compound libraries. A natural product library containing 10,000 compounds was screened and 9 hits were selected for validation. These compounds have been taken for the second-step in vitro tests to confirm their agonistic activity. The most active adiponectin receptor 1 agonists are matairesinol, arctiin, (--arctigenin and gramine. The most active adiponectin receptor 2 agonists are parthenolide, taxifoliol, deoxyschizandrin, and syringin. These compounds may be useful drug candidates for hypoadiponectin related diseases.

48 CFR 653.101-70 - Policy.

Science.gov (United States)

2010-10-01

... 48 Federal Acquisition Regulations System 4 2010-10-01 2010-10-01 false Policy. 653.101-70 Section 653.101-70 Federal Acquisition Regulations System DEPARTMENT OF STATE CLAUSES AND FORMS FORMS General... exclusion of any form in accordance with FAR subpart 1.4 and 601.470. [53 FR 26180, July 11, 1988, as...

Influence of surface treatment of yttria-stabilized tetragonal zirconia polycrystal with hot isostatic pressing on cyclic fatigue strength.

Science.gov (United States)

Iijima, Toshihiko; Homma, Shinya; Sekine, Hideshi; Sasaki, Hodaka; Yajima, Yasutomo; Yoshinari, Masao

2013-01-01

Hot isostatic pressing processed yttria-stabilized tetragonal zirconia polycrystal (HIP Y-TZP) has the potential for application to implants due to its high mechanical performance. The aim of this study was to investigate the influence of surface treatment of HIP Y-TZP on cyclic fatigue strength. HIP Y-TZP specimens were subjected to different surface treatments. Biaxial flexural strength was determined by both static and cyclic fatigue testing. In the cyclic fatigue test, the load was applied at a frequency of 10 Hz for 10(6) cycles in distilled water at 37°C. The surface morphology, roughness, and crystal phase of the surfaces were also evaluated. The cyclic fatigue strength (888 MPa) of HIP Y-TZP with sandblasting and acid-etching was more than twice that of Y-TZP as specified in ISO 13356 for surgical implants (320 MPa), indicating the clinical potential of this material.

Agonist-induced desensitization of adenylyl cyclase in Y1 adrenocortical tumor cells

International Nuclear Information System (INIS)

Olson, M.F.; Tsao, J.; Pon, D.J.; Schimmer, B.P.

1991-01-01

Y1 adrenocortical tumor cells (Y1DS) and Y1 mutants resistant to ACTH-induced desensitization of adenylyl cyclase (Y1DR) were transfected with a gene encoding the mouse beta 2-adrenergic receptor (beta 2-AR). Transfectants expressed beta 2-ARs that were able to stimulate adenylyl cyclase activity and steroid biosynthesis. These transfectants were used to explore the basis for the DR mutation in Y1 cells. The authors demonstrate that beta-adrenergic agonists desensitize the adenylyl cyclase system in transfected Y1DS cells whereas transfected Y1DR cells are resistant to desensitization by beta-adrenergic agonists. The fate of the beta 2-ARs during desensitization was evaluated by photoaffinity labelling with [125I]iodocyanopindolol diazerine. Desensitization of Y1DS transfectants was accompanied by a modest loss in receptor density that was insufficient to account for the complete loss of responsiveness to beta-adrenergic agonists. The extent of receptor loss induced by beta-adrenergic agonists in Y1DR transfectants exceeded that in the Y1DS transfectants indicating that the mutation which protects Y1DR cells from agonist-induced desensitization is prior to receptor down-regulation in the desensitization pathway. From these results we infer that ACTH and isoproterenol desensitize adenylyl cyclase by a common pathway and that receptor loss is not a major component of the desensitization process in these cells

PPAR agonists reduce steatosis in oleic acid-overloaded HepaRG cells

International Nuclear Information System (INIS)

Rogue, Alexandra; Anthérieu, Sébastien; Vluggens, Aurore; Umbdenstock, Thierry; Claude, Nancy; Moureyre-Spire, Catherine de la; Weaver, Richard J.; Guillouzo, André

2014-01-01

Although non-alcoholic fatty liver disease (NAFLD) is currently the most common form of chronic liver disease there is no pharmacological agent approved for its treatment. Since peroxisome proliferator-activated receptors (PPARs) are closely associated with hepatic lipid metabolism, they seem to play important roles in NAFLD. However, the effects of PPAR agonists on steatosis that is a common pathology associated with NAFLD, remain largely controversial. In this study, the effects of various PPAR agonists, i.e. fenofibrate, bezafibrate, troglitazone, rosiglitazone, muraglitazar and tesaglitazar on oleic acid-induced steatotic HepaRG cells were investigated after a single 24-hour or 2-week repeat treatment. Lipid vesicles stained by Oil-Red O and triglycerides accumulation caused by oleic acid overload, were decreased, by up to 50%, while fatty acid oxidation was induced after 2-week co-treatment with PPAR agonists. The greatest effects on reduction of steatosis were obtained with the dual PPARα/γ agonist muraglitazar. Such improvement of steatosis was associated with up-regulation of genes related to fatty acid oxidation activity and down-regulation of many genes involved in lipogenesis. Moreover, modulation of expression of some nuclear receptor genes, such as FXR, LXRα and CAR, which are potent actors in the control of lipogenesis, was observed and might explain repression of de novo lipogenesis. Conclusion: Altogether, our in vitro data on steatotic HepaRG cells treated with PPAR agonists correlated well with clinical investigations, bringing a proof of concept that drug-induced reversal of steatosis in human can be evaluated in in vitro before conducting long-term and costly in vivo studies in animals and patients. - Highlights: • There is no pharmacological agent approved for the treatment of NAFLD. • This study demonstrates that PPAR agonists can reduce fatty acid-induced steatosis. • Some nuclear receptors appear to be potent actors in the control

PPAR agonists reduce steatosis in oleic acid-overloaded HepaRG cells

Energy Technology Data Exchange (ETDEWEB)

Rogue, Alexandra [Inserm UMR 991, 35043 Rennes Cedex (France); Université de Rennes 1, Faculté des Sciences Pharmaceutiques et Biologiques, 35043 Rennes Cedex (France); Biologie Servier, Gidy (France); Anthérieu, Sébastien; Vluggens, Aurore [Inserm UMR 991, 35043 Rennes Cedex (France); Université de Rennes 1, Faculté des Sciences Pharmaceutiques et Biologiques, 35043 Rennes Cedex (France); Umbdenstock, Thierry [Technologie Servier, Orléans (France); Claude, Nancy [Institut de Recherches Servier, Courbevoie (France); Moureyre-Spire, Catherine de la; Weaver, Richard J. [Biologie Servier, Gidy (France); Guillouzo, André, E-mail: Andre.Guillouzo@univ-rennes1.fr [Inserm UMR 991, 35043 Rennes Cedex (France); Université de Rennes 1, Faculté des Sciences Pharmaceutiques et Biologiques, 35043 Rennes Cedex (France)

2014-04-01

Although non-alcoholic fatty liver disease (NAFLD) is currently the most common form of chronic liver disease there is no pharmacological agent approved for its treatment. Since peroxisome proliferator-activated receptors (PPARs) are closely associated with hepatic lipid metabolism, they seem to play important roles in NAFLD. However, the effects of PPAR agonists on steatosis that is a common pathology associated with NAFLD, remain largely controversial. In this study, the effects of various PPAR agonists, i.e. fenofibrate, bezafibrate, troglitazone, rosiglitazone, muraglitazar and tesaglitazar on oleic acid-induced steatotic HepaRG cells were investigated after a single 24-hour or 2-week repeat treatment. Lipid vesicles stained by Oil-Red O and triglycerides accumulation caused by oleic acid overload, were decreased, by up to 50%, while fatty acid oxidation was induced after 2-week co-treatment with PPAR agonists. The greatest effects on reduction of steatosis were obtained with the dual PPARα/γ agonist muraglitazar. Such improvement of steatosis was associated with up-regulation of genes related to fatty acid oxidation activity and down-regulation of many genes involved in lipogenesis. Moreover, modulation of expression of some nuclear receptor genes, such as FXR, LXRα and CAR, which are potent actors in the control of lipogenesis, was observed and might explain repression of de novo lipogenesis. Conclusion: Altogether, our in vitro data on steatotic HepaRG cells treated with PPAR agonists correlated well with clinical investigations, bringing a proof of concept that drug-induced reversal of steatosis in human can be evaluated in in vitro before conducting long-term and costly in vivo studies in animals and patients. - Highlights: • There is no pharmacological agent approved for the treatment of NAFLD. • This study demonstrates that PPAR agonists can reduce fatty acid-induced steatosis. • Some nuclear receptors appear to be potent actors in the control

National instrument 51-101 : new rules are coming

Energy Technology Data Exchange (ETDEWEB)

Story, C.A. [Fraser Milner Casgrain LLP, Calgary, AB (Canada)

2003-07-01

This paper provides general information about National Instrument 51-101 developed by the Alberta Securities Commission. NI 51-101 requires public companies to file an annual statement regarding estimated oil and gas reserves and related information. The report must be accompanied by an independent qualified evaluator's report and any other information regarding oil and gas activities. NI 51-101 incorporates reserves definitions developed by the reserves committee at the Canadian Institute of Mining, Metallurgy and Petroleum (CIM). The paper also outlines some of the issues that should be considered in purchases, sales, mergers, and acquisitions. This paper described the timing and transition of NI 51-101 and included a list of information that must be disclosed in the annual statement. Materiality standards, and material change disclosure was also described along with issuer obligations. It was noted that NI 51-101 will impact prospectus disclosures as well as memorandum disclosures.

27 CFR 70.101 - Bad checks.

Science.gov (United States)

2010-04-01

... 27 Alcohol, Tobacco Products and Firearms 2 2010-04-01 2010-04-01 false Bad checks. 70.101 Section....101 Bad checks. If any check or money order in payment of any amount receivable under Title 26 of the... appropriate TTB officer that such check was tendered in good faith and that such person had reasonable cause...

41 CFR 101-45.002 - Gold.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Gold. 101-45.002 Section... PERSONAL PROPERTY § 101-45.002 Gold. (a) Gold will be sold in accordance with this section and part 102-38 of the Federal Management Regulation. (b) Sales of gold shall be processed to— (1) Use the sealed bid...

Investigation of the mechanism of radioprotective action of adrenoceptor agonists

International Nuclear Information System (INIS)

Kulinskij, V.I.; Klimova, A.D.; Yashunskij, V.G.; Alpatova, T.V.; 4205700SU)

1986-01-01

α-Adrenoceptor agonists of both main groups, i.e. arylalkylamines and imidazolines, have a pronounced radioprotective effect. Their chemical analogs, which fail to stimulate α-adrenoceptors, do not protect mice. The effect of phenylephrine, adrenaline, and noradrenaline comes into play via α 1 -adrenoceptors and that of clonidine, via α 2 -adrenoceptors and also via α 1 -adrenoceptors. Adrenoceptor agonists can probably manifest their radioprotective action via both subtypes of α-adrenoceptors. Possible intracellular mechanisms of the radioprotective action are discussed

Pregnancy outcome in delayed start antagonist versus microdose flare GnRH agonist protocol in poor responders undergoing IVF/ICSI: An RCT

Directory of Open Access Journals (Sweden)

Robab Davar

2018-04-01

Full Text Available Background: Over the years, many article on different aspects of pathogenesis and management of poor ovarian responders have been published but there is no clear guideline for treating themyet. Objective: This study was designated to compare the effectiveness of a delayed start protocol with gonadotropin-releasing hormone (GnRH antagonist and microdose flare-up GnRH agonist protocol in poor ovarian responders. Materials and Methods: This randomized clinical trial consisted of 100 poor ovarian responder women in assisted reproductive technologies cycles. They were divided randomly in delayed-start antagonist protocol (with estrogen priming followed by early follicular-phase GnRH antagonist treatment for 7 days before ovarian stimulation and microdose flare-up GnRH agonist protocol. The main outcome was clinical pregnancy rate and second outcome was the number of retrieved oocytes, mature oocytes, 2PN number, fertilization rate, and implantation rate. Results: Fertilization rate, clinical pregnancy rate, and ongoing pregnancy rates were not significantly different between the two studied protocols. Number of retrieved oocytes (5.10±3.41 vs. 3.08±2.51 with p=0.002, mature oocytes (4.32±2.69 vs. 2.34±1.80 with p=0.003, number of 2PN (3.94±1.80 vs. 2.20±1.01 with p=0.001 and implantation rate (19.40% vs. 10.30% with p=0.022 were significantly higher in delayed antagonist group. Conclusion: The delayed-start protocol can improve ovarian response in poor responders by stimulating and synchronizing follicle development

Engineering of radioimmunoassay (RIA) IP10.1

International Nuclear Information System (INIS)

Hari Nurcahyadi

2010-01-01

Engineering of Radioimmunoassay (RIA) IP10.1 is an innovative by PRPN - BATAN in 2010. Innovations made to the device IP10.1 RIA is the sample changer system, sample changer system on the device RIA IP10.1 applied 2 linear axis system (X, Z) with AC servo motor. In the RIA IP10.1 also use 5 pieces of the detector, so the enumeration process 50 (Fifty) sample is expected to be faster. Like its predecessor, The whole enumeration, data collection procedures and mechanisms operating within this system is entirely controlled by a PC via an electronic module. Electronics module consists of a high voltage module, amplifier and signal processor module, the module enumerators, low-voltage module, the module driver motor controller and a USB interface. The data acquisition and communication system using a USB port with the computer. (author)

Beam dynamics studies of the ISOLDE post-accelerator for the high intensity and energy upgrade

CERN Document Server

Fraser, M A

2012-01-01

The High Intensity and Energy (HIE) project represents a major upgrade of the ISOLDE (On-Line Isotope Mass Separator) nuclear facility at CERN with a mandate to significantly increase the energy, intensity and quality of the radioactive nuclear beams provided to the European nuclear physics community for research at the forefront of topics such as nuclear structure physics and nuclear astrophysics. The HIE-ISOLDE project focuses on the upgrade of the existing Radioactive ion beam EXperiment (REX) post-accelerator with the addition of a 40MVsuperconducting linac comprising 32 niobium sputter-coated copper quarter-wave cavities operating at 101.28 MHz and at an accelerating gradient close to 6 MV/m. The energy of post-accelerated radioactive nuclear beams will be increased from the present ceiling of 3 MeV/u to over 10 MeV/u, with full variability in energy, and will permit, amongst others, Coulomb interaction and few-nucleon transfer reactions to be carried out on the full inventory of radionuclides available ...

Beam Dynamics Studies of the ISOLDE Post-accelerator for the High Intensity and Energy Upgrade

CERN Document Server

Fraser, Matthew Alexander; Pasini, M

2012-01-01

The High Intensity and Energy (HIE) project represents a major upgrade of the ISOLDE (On-Line Isotope Mass Separator) nuclear facility at CERN with a mandate to significantly increase the energy, intensity and quality of the radioactive nuclear beams provided to the European nuclear physics community for research at the forefront of topics such as nuclear structure physics and nuclear astrophysics. The HIE-ISOLDE project focuses on the upgrade of the existing Radioactive ion beam EXperiment (REX) post-accelerator with the addition of a 40MVsuperconducting linac comprising 32 niobium sputter-coated copper quarter-wave cavities operating at 101.28 MHz and at an accelerating gradient close to 6 MV/m. The energy of post-accelerated radioactive nuclear beams will be increased from the present ceiling of 3 MeV/u to over 10 MeV/u, with full variability in energy, and will permit, amongst others, Coulomb interaction and few-nucleon transfer reactions to be carried out on the full inventory of radionuclides available ...

CCNA routing and switching review guide exams 100-101, 200-101, and 200-120

CERN Document Server

Lammle, Todd

2013-01-01

Todd Lammle's focused, concise review guide, updated for the latest CCNA exams CCNA is one of the most sought after certifications for IT professionals. If you're preparing for the CCNA Routing and Switching certification, this Sybex review guide offers the best quick review available. Organized by exam objective, it's the perfect supplement to other learning tools, including the Sybex CCNA Routing and Switching Study Guide (ISBN: 9781118749616). All exam topics from exams 100-101, 200-101, and 200-120 are thoroughly covered, and additional study materials including bonus exams, electronic f

47 CFR 101.105 - Interference protection criteria.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 5 2010-10-01 2010-10-01 false Interference protection criteria. 101.105 Section 101.105 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) SAFETY AND SPECIAL RADIO.... (ii) To accommodate co-primary Direct Broadcast Satellite Service earth stations, an MVDDS...

48 CFR 3003.101-3 - Agency regulations.

Science.gov (United States)

2010-10-01

....101-3 Section 3003.101-3 Federal Acquisition Regulations System DEPARTMENT OF HOMELAND SECURITY, HOMELAND SECURITY ACQUISITION REGULATION (HSAR) GENERAL IMPROPER BUSINESS PRACTICES AND PERSONAL CONFLICTS... Security regulations governing the conduct and responsibilities of employees are contained in 5 CFR part...

41 CFR 101-25.108 - Multiyear subscriptions for publications.

Science.gov (United States)

2010-07-01

... for publications. 101-25.108 Section 101-25.108 Public Contracts and Property Management Federal...-GENERAL 25.1-General Policies § 101-25.108 Multiyear subscriptions for publications. Subscriptions for periodicals, newspapers, and other publications for which it is known in advance that a continuing requirement...

[Effects of GLP-1 receptor agonists on carbohydrate metabolism control].

Science.gov (United States)

Fernández-García, José Carlos; Colomo, Natalia; Tinahones, Francisco José

2014-09-01

Glucagon-like peptide-1 (GLP-1) receptor agonists are a new group of drugs for the treatment of type 2 diabetes mellitus (DM2). In the present article, we review the available evidence on the efficacy of GLP-1 receptor agonists as glucose-lowering agents, their place in therapeutic algorithms, and the clinical factors associated with a favorable treatment response. Finally, we describe the clinical characteristics of patients who may benefit from these drugs. Copyright © 2014 Elsevier España, S.L.U. All rights reserved.

UCB-NE-101 user's manual

International Nuclear Information System (INIS)

Lee, W.W.L.

1989-02-01

The purpose of this manual is to provide users of UCB-NE-101 with the information necessary to use UCB-NE-101 effectively. UCB-NE-101 calculates the concentration of solubility-limited species as a function of space and time and its mass flux rates from a waste sphere buried in a nuclear waste repository in water-saturated rock. The waste is surrounded by one type of rock, and some distance away, there is another type of rock. The inner layer of rock can be a backfill around a nuclear waste package and the outer layer the natural rock. The mass flux calculated is at the interface of the two layers. The species concentration calculated is in the inner layer. A constant concentration of the species, usually the solubility, is specified at the waste sphere/inner layer interface. Dissolution and transport is governed by the solubility of the species, and diffusion in the porous media. 1 ref., 1 fig

5 CFR 838.101 - Purpose and scope.

Science.gov (United States)

2010-01-01

... 5 Administrative Personnel 2 2010-01-01 2010-01-01 false Purpose and scope. 838.101 Section 838.101 Administrative Personnel OFFICE OF PERSONNEL MANAGEMENT (CONTINUED) CIVIL SERVICE REGULATIONS (CONTINUED) COURT ORDERS AFFECTING RETIREMENT BENEFITS Court Orders Generally Organization and Structure of...

48 CFR 3003.101 - Standards of conduct.

Science.gov (United States)

2010-10-01

... 48 Federal Acquisition Regulations System 7 2010-10-01 2010-10-01 false Standards of conduct. 3003.101 Section 3003.101 Federal Acquisition Regulations System DEPARTMENT OF HOMELAND SECURITY, HOMELAND SECURITY ACQUISITION REGULATION (HSAR) GENERAL IMPROPER BUSINESS PRACTICES AND PERSONAL CONFLICTS OF...

3 CFR 101.2 - Office of Management and Budget.

Science.gov (United States)

2010-01-01

... 3 The President 1 2010-01-01 2010-01-01 false Office of Management and Budget. 101.2 Section 101.2... PROCEDURES ACT § 101.2 Office of Management and Budget. Freedom of Information regulations for the Office of Management and Budget appear at 5 CFR Ch. III. ...

41 CFR 101-4.100 - Purpose and effective date.

Science.gov (United States)

2010-07-01

... EDUCATION PROGRAMS OR ACTIVITIES RECEIVING FEDERAL FINANCIAL ASSISTANCE Introduction § 101-4.100 Purpose and... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Purpose and effective date. 101-4.100 Section 101-4.100 Public Contracts and Property Management Federal Property Management...

41 CFR 101-4.125 - Effect of other requirements.

Science.gov (United States)

2010-07-01

... EDUCATION PROGRAMS OR ACTIVITIES RECEIVING FEDERAL FINANCIAL ASSISTANCE Introduction § 101-4.125 Effect of... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Effect of other requirements. 101-4.125 Section 101-4.125 Public Contracts and Property Management Federal Property Management...

41 CFR 101-4.130 - Effect of employment opportunities.

Science.gov (United States)

2010-07-01

... EDUCATION PROGRAMS OR ACTIVITIES RECEIVING FEDERAL FINANCIAL ASSISTANCE Introduction § 101-4.130 Effect of... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Effect of employment opportunities. 101-4.130 Section 101-4.130 Public Contracts and Property Management Federal Property Management...

41 CFR 101-1.109 - Numbering in FPMR System.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Numbering in FPMR System. 101-1.109 Section 101-1.109 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101...

41 CFR 101-1.105 - Authority for FPMR System.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Authority for FPMR System. 101-1.105 Section 101-1.105 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101...

41 CFR 101-1.111 - Retention of FPMR amendments.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Retention of FPMR amendments. 101-1.111 Section 101-1.111 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS GENERAL 1-INTRODUCTION 1.1-Regulation System § 101...

41 CFR 101-39.402 - Recommendations for disciplinary action.

Science.gov (United States)

2010-07-01

... VEHICLES 39-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.4-Accidents and Claims § 101-39.402 Recommendations for... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Recommendations for disciplinary action. 101-39.402 Section 101-39.402 Public Contracts and Property Management Federal Property...

Development and validation of a high-performance liquid chromatography method for the quantification of talazoparib in rat plasma: Application to plasma protein binding studies.

Science.gov (United States)

Hidau, Mahendra Kumar; Kolluru, Srikanth; Palakurthi, Srinath

2018-02-01

A sensitive and selective RP-HPLC method has been developed and validated for the quantification of a highly potent poly ADP ribose polymerase inhibitor talazoparib (TZP) in rat plasma. Chromatographic separation was performed with isocratic elution method. Absorbance for TZP was measured with a UV detector (SPD-20A UV-vis) at a λ max of 227 nm. Protein precipitation was used to extract the drug from plasma samples using methanol-acetonitrile (65:35) as the precipitating solvent. The method proved to be sensitive and reproducible over a 100-2000 ng/mL linearity range with a lower limit of quantification (LLQC) of 100 ng/mL. TZP recovery was found to be >85%. Following analytical method development and validation, it was successfully employed to determine the plasma protein binding of TZP. TZP has a high level of protein binding in rat plasma (95.76 ± 0.38%) as determined by dialysis method. Copyright © 2017 John Wiley & Sons, Ltd.

21 CFR 99.101 - Information that may be disseminated.

Science.gov (United States)

2010-04-01

... 21 Food and Drugs 1 2010-04-01 2010-04-01 false Information that may be disseminated. 99.101 Section 99.101 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Information To Be Disseminated § 99.101 Information that may be disseminated. (a) A manufacturer may...

41 CFR 101-25.106 - Servicing of office machines.

Science.gov (United States)

2010-07-01

... machines. 101-25.106 Section 101-25.106 Public Contracts and Property Management Federal Property...-General Policies § 101-25.106 Servicing of office machines. (a) The determination as to whether office machines are to be serviced by use of annual maintenance contracts or per-call arrangements shall be made...

41 CFR 101-27.507 - Transportation and other costs.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Transportation and other costs. 101-27.507 Section 101-27.507 Public Contracts and Property Management Federal Property... MANAGEMENT 27.5-Return of GSA Stock Items § 101-27.507 Transportation and other costs. Transportation costs...

Metal organic framework MIL-101(Cr) for dehydration reactions

Indian Academy of Sciences (India)

Porous chromium terephthalate MIL-101 (Cr-MIL-101) has been prepared by direct method under hydrothermal conditions and characterized using X-ray diffraction, N2 sorption, TGA and FT-IR. The nitrogen adsorption-desorption isotherm shows that the Cr-MIL-101 possesses BET specific surface area of 2563 m2/g.

PPARα agonists up-regulate organic cation transporters in rat liver cells

International Nuclear Information System (INIS)

Luci, Sebastian; Geissler, Stefanie; Koenig, Bettina; Koch, Alexander; Stangl, Gabriele I.; Hirche, Frank; Eder, Klaus

2006-01-01

It has been shown that clofibrate treatment increases the carnitine concentration in the liver of rats. However, the molecular mechanism is still unknown. In this study, we observed for the first time that treatment of rats with the peroxisome proliferator activated receptor (PPAR)-α agonist clofibrate increases hepatic mRNA concentrations of organic cation transporters (OCTNs)-1 and -2 which act as transporters of carnitine into the cell. In rat hepatoma (Fao) cells, treatment with WY-14,643 also increased the mRNA concentration of OCTN-2. mRNA concentrations of enzymes involved in carnitine biosynthesis were not altered by treatment with the PPARα agonists in livers of rats and in Fao cells. We conclude that PPARα agonists increase carnitine concentrations in livers of rats and cells by an increased uptake of carnitine into the cell but not by an increased carnitine biosynthesis

Characterization of 12 GnRH peptide agonists - a kinetic perspective.

Science.gov (United States)

Nederpelt, Indira; Georgi, Victoria; Schiele, Felix; Nowak-Reppel, Katrin; Fernández-Montalván, Amaury E; IJzerman, Adriaan P; Heitman, Laura H

2016-01-01

Drug-target residence time is an important, yet often overlooked, parameter in drug discovery. Multiple studies have proposed an increased residence time to be beneficial for improved drug efficacy and/or longer duration of action. Currently, there are many drugs on the market targeting the gonadotropin-releasing hormone (GnRH) receptor for the treatment of hormone-dependent diseases. Surprisingly, the kinetic receptor-binding parameters of these analogues have not yet been reported. Therefore, this project focused on determining the receptor-binding kinetics of 12 GnRH peptide agonists, including many marketed drugs. A novel radioligand-binding competition association assay was developed and optimized for the human GnRH receptor with the use of a radiolabelled peptide agonist, [(125) I]-triptorelin. In addition to radioligand-binding studies, a homogeneous time-resolved FRET Tag-lite™ method was developed as an alternative assay for the same purpose. Two novel competition association assays were successfully developed and applied to determine the kinetic receptor-binding characteristics of 12 high-affinity GnRH peptide agonists. Results obtained from both methods were highly correlated. Interestingly, the binding kinetics of the peptide agonists were more divergent than their affinities with residence times ranging from 5.6 min (goserelin) to 125 min (deslorelin). Our research provides new insights by incorporating kinetic, next to equilibrium, binding parameters in current research and development that can potentially improve future drug discovery targeting the GnRH receptor. © 2015 The British Pharmacological Society.

41 CFR 101-27.503 - Allowable credit.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Allowable credit. 101-27.503 Section 101-27.503 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 27-INVENTORY MANAGEMENT 27.5...

41 CFR 101-26.311 - Frustrated shipments.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Frustrated shipments. 101-26.311 Section 101-26.311 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND...

41 CFR 101-26.310 - Ordering errors.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Ordering errors. 101-26.310 Section 101-26.310 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND...

41 CFR 101-26.304 - Substitution policy.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Substitution policy. 101-26.304 Section 101-26.304 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND...

41 CFR 101-26.507 - Security equipment.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Security equipment. 101-26.507 Section 101-26.507 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND...

5 CFR 890.101 - Definitions; time computations.

Science.gov (United States)

2010-01-01

... 5 Administrative Personnel 2 2010-01-01 2010-01-01 false Definitions; time computations. 890.101....101 Definitions; time computations. (a) In this part, the terms annuitant, carrier, employee, employee... in section 8901 of title 5, United States Code, and supplement the following definitions: Appropriate...

41 CFR 101-39.103 - Agency appeals.

Science.gov (United States)

2010-07-01

...-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.1-Establishment, Modification, and Discontinuance of Interagency Fleet... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Agency appeals. 101-39.103 Section 101-39.103 Public Contracts and Property Management Federal Property Management...

41 CFR 101-39.104-2 - Reimbursement.

Science.gov (United States)

2010-07-01

...-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.1-Establishment, Modification, and Discontinuance of Interagency Fleet... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Reimbursement. 101-39.104-2 Section 101-39.104-2 Public Contracts and Property Management Federal Property Management...

47 CFR 25.101 - Basis and scope.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 2 2010-10-01 2010-10-01 false Basis and scope. 25.101 Section 25.101 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) COMMON CARRIER SERVICES SATELLITE COMMUNICATIONS... 501(c)(6) of the International Maritime Satellite Telecommunications Act, and titles I through III of...

The Natural Carotenoid Crocetin and the Synthetic Tellurium Compound AS101 Protect the Ovary against Cyclophosphamide by Modulating SIRT1 and Mitochondrial Markers

Directory of Open Access Journals (Sweden)

Giovanna Di Emidio

2017-01-01

Full Text Available Cancer therapies are associated with increased infertility risk due to accelerated reproductive aging. Oxidative stress (OS is a potential mechanism behind ovarian toxicity by cyclophosphamide (CPM, the most ovotoxic anticancer drug. An important sensor of OS is SIRT1, a NAD+-dependent deacetylase which regulates cellular defence and cell fate. This study investigated whether the natural carotenoid crocetin and the synthetic compound AS101 protect the ovary against CPM by modulating SIRT1 and mitochondrial markers. We found that the number of primordial follicles of female CD1 mice receiving crocetin plus CPM increased when compared with CPM alone and similar to AS101, whose protective effects are known. SIRT1 increased in CPM mouse ovaries revealing the occurrence of OS. Similarly, mitochondrial SIRT3 rose, whilst SOD2 and the mitochondrial biogenesis activator PGC1-α decreased, suggesting the occurrence of mitochondrial damage. Crocetin and AS101 administration prevented SIRT1 burst suggesting that preservation of redox balance can help the ovary to counteract ovarian damage by CPM. Decreased SIRT3 and increased SOD2 and PGC1-α in mice receiving crocetin or AS101 prior to CPM provide evidence for mitochondrial protection. Present results improve the knowledge of ovarian damage by CPM and may help to develop interventions for preserving fertility in cancer patients.

Discovery of Azetidinone Acids as Conformationally-Constrained Dual PPARalpha/gamma Agonists

Energy Technology Data Exchange (ETDEWEB)

Wang, W.; Devasthale, P; Farrelly, D; Gu, L; Harrity, T; Cap, M; Chu, C; Kunselman, L; Morgan, N; et. al.

2008-01-01

A novel class of azetidinone acid-derived dual PPAR{alpha}/{gamma} agonists has been synthesized for the treatment of diabetes and dyslipidemia. The preferred stereochemistry in this series for binding and functional agonist activity against both PPARa and PPAR? receptors was shown to be 3S,4S. Synthesis, in vitro and in vivo activities of compounds in this series are described. A high-yielding method for N-arylation of azetidinone esters is also described.

41 CFR 101-27.102-1 - Applicability.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Applicability. 101-27.102-1 Section 101-27.102-1 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 27-INVENTORY MANAGEMENT 27.1...

41 CFR 101-26.501-8 - [Reserved

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true [Reserved] 101-26.501-8 Section 101-26.501-8 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND PROGRAM...

41 CFR 101-26.607-2 - Adjustments.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Adjustments. 101-26.607-2 Section 101-26.607-2 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND PROGRAM...

41 CFR 101-26.506-2 - Limitations.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Limitations. 101-26.506-2 Section 101-26.506-2 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND PROGRAM...

41 CFR 101-26.607-1 - Payments.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Payments. 101-26.607-1 Section 101-26.607-1 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND PROGRAM...

5 CFR 2638.101 - Authority and purpose.

Science.gov (United States)

2010-01-01

... 2638.101 Administrative Personnel OFFICE OF GOVERNMENT ETHICS GOVERNMENT ETHICS OFFICE OF GOVERNMENT ETHICS AND EXECUTIVE AGENCY ETHICS PROGRAM RESPONSIBILITIES General Provisions § 2638.101 Authority and... IV of the Ethics in Government Act of 1978 (Pub. L. 95-521, as amended) (“the Act”). (b) Purpose...

41 CFR 101-29.213 - Commercial product.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Commercial product. 101... Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 29-FEDERAL PRODUCT DESCRIPTIONS 29.2-Definitions § 101-29.213 Commercial product. A commercial product is any item, component, or...

Evaluation of radioactivity in the bodies of mice induced by neutron exposure from an epi-thermal neutron source of an accelerator-based boron neutron capture therapy system

Science.gov (United States)

NAKAMURA, Satoshi; IMAMICHI, Shoji; MASUMOTO, Kazuyoshi; ITO, Masashi; WAKITA, Akihisa; OKAMOTO, Hiroyuki; NISHIOKA, Shie; IIJIMA, Kotaro; KOBAYASHI, Kazuma; ABE, Yoshihisa; IGAKI, Hiroshi; KURITA, Kazuyoshi; NISHIO, Teiji; MASUTANI, Mitsuko; ITAMI, Jun

2017-01-01

This study aimed to evaluate the residual radioactivity in mice induced by neutron irradiation with an accelerator-based boron neutron capture therapy (BNCT) system using a solid Li target. The radionuclides and their activities were evaluated using a high-purity germanium (HP-Ge) detector. The saturated radioactivity of the irradiated mouse was estimated to assess the radiation protection needs for using the accelerator-based BNCT system. 24Na, 38Cl, 80mBr, 82Br, 56Mn, and 42K were identified, and their saturated radioactivities were (1.4 ± 0.1) × 102, (2.2 ± 0.1) × 101, (3.4 ± 0.4) × 102, 2.8 ± 0.1, 8.0 ± 0.1, and (3.8 ± 0.1) × 101 Bq/g/mA, respectively. The 24Na activation rate at a given neutron fluence was found to be consistent with the value reported from nuclear-reactor-based BNCT experiments. The induced activity of each nuclide can be estimated by entering the saturated activity of each nuclide, sample mass, irradiation time, and proton current into the derived activation equation in our accelerator-based BNCT system. PMID:29225308

CCNA routing and switching study guide exams 100-101, 200-101, and 200-120

CERN Document Server

Lammle, Todd

2013-01-01

Prepare for the new CCNA exams with this Todd Lammle study guide Cisco author, speaker, and trainer Todd Lammle is considered the authority on all things networking, and his books have sold almost a million copies worldwide. This all-purpose CCNA study guide methodically covers all the objectives of the ICND1 (100-101) and ICND2 (200-101) exams as well as providing additional insight for those taking CCNA Composite (200-120) exam. It thoroughly examines operation of IP data networks, LAN switching technologies, IP addressing (IPv4/IPv6), IP routing technologies, IP services, network device s

41 CFR 101-27.209-1 - GSA stock items.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true GSA stock items. 101-27.209-1 Section 101-27.209-1 Public Contracts and Property Management Federal Property Management...-Management of Shelf-Life Materials § 101-27.209-1 GSA stock items. Shelf-life items that meet the criteria...

Estradiol agonists inhibit human LoVo colorectal-cancer cell proliferation and migration through p53.

Science.gov (United States)

Hsu, Hsi-Hsien; Kuo, Wei-Wen; Ju, Da-Tong; Yeh, Yu-Lan; Tu, Chuan-Chou; Tsai, Ying-Lan; Shen, Chia-Yao; Chang, Sheng-Huang; Chung, Li-Chin; Huang, Chih-Yang

2014-11-28

To investigate the effects of 17β-estradiol via estrogen receptors (ER) or direct administration of ER agonists on human colorectal cancer. LoVo cells were established from the Bioresource Collection and Research Center and cultured in phenol red-free DMEM (Sigma, United States). To investigate the effects of E2 and/or ER selective agonists on cellular proliferation, LoVo colorectal cells were treated with E2 or ER-selective agonists for 24 h and 48 h and subjected to the MTT (Sigma) assay to find the concentration. And investigate the effects of E2 and/or ER selective agonists on cell used western immunoblotting to find out the diversification of signaling pathways. In order to observe motility and migration the wound healing assay and a transwell chamber (Neuro Probe) plate were tased. For a quantitative measure, we counted the number of migrating cells to the wound area post-wounding for 24 h. We further examined the cellular migration-regulating factors urokinase-type plasminogen activator (u-PA), tissue-type plasminogen activator (t-PA) and matrix metalloproteinase (MMP)-9 in human LoVo cells so gelatin zymography that we used and gelatinolytic activity was visualized by Coomassie blue staining. And these results are presented as means ± SE, and statistical comparisons were made using Student's t-test. The structure was first compared with E2 and ER agonists. We then treated the LoVo cells with E2 and ER agonists (10(-8) mol/L) for 24 h and 48 h and subsequently measured the cell viability using MTT assay. Our results showed that treatment with 17β-estradiol and/or ER agonists in human LoVo colorectal cancer cells activated p53 and then up-regulated p21 and p27 protein levels, subsequently inhibiting the downstream target gene, cyclin D1, which regulates cell proliferation. Taken together, our findings demonstrate the anti-tumorigenesis effects of 17β-estradiol and/or ER agonists and suggest that these compounds may prove to be a potential alternative

7 CFR 765.101 - Borrower graduation requirements.

Science.gov (United States)

2010-01-01

... reasonable rates and terms. (b) The Agency may require partial or full graduation. (1) In a partial... 7 Agriculture 7 2010-01-01 2010-01-01 false Borrower graduation requirements. 765.101 Section 765..., DEPARTMENT OF AGRICULTURE SPECIAL PROGRAMS DIRECT LOAN SERVICING-REGULAR Borrower Graduation § 765.101...

33 CFR 101.515 - TWIC/Personal Identification.

Science.gov (United States)

2010-07-01

....515 Section 101.515 Navigation and Navigable Waters COAST GUARD, DEPARTMENT OF HOMELAND SECURITY MARITIME SECURITY MARITIME SECURITY: GENERAL Other Provisions § 101.515 TWIC/Personal Identification. (a... TWIC must allow his or her TWIC to be read by a reader and must submit his or her reference biometric...

9 CFR 113.101 - Leptospira Pomona Bacterin.

Science.gov (United States)

2010-01-01

... 9 Animals and Animal Products 1 2010-01-01 2010-01-01 false Leptospira Pomona Bacterin. 113.101... Inactivated Bacterial Products § 113.101 Leptospira Pomona Bacterin. Leptospira Pomona Bacterin shall be produced from a culture of Leptospira pomona which has been inactivated and is nontoxic. Each serial of...

45 CFR 205.101 - Organization for administration.

Science.gov (United States)

2010-10-01

... 45 Public Welfare 2 2010-10-01 2010-10-01 false Organization for administration. 205.101 Section... ADMINISTRATION-PUBLIC ASSISTANCE PROGRAMS § 205.101 Organization for administration. (a) A State plan for... description of the organization and functions of the single State agency and an organizational chart of the...

41 CFR 101-39.201 - Services available.

Science.gov (United States)

2010-07-01

...-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.2-GSA Interagency Fleet Management System Services § 101-39.201 Services available. GSA Interagency Fleet Management System (IFMS) vehicles and services shall be used in... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Services available. 101...

7 CFR 58.101 - Meaning of words.

Science.gov (United States)

2010-01-01

... 7 Agriculture 3 2010-01-01 2010-01-01 false Meaning of words. 58.101 Section 58.101 Agriculture Regulations of the Department of Agriculture (Continued) AGRICULTURAL MARKETING SERVICE (Standards... of words. For the purpose of the regulations of this subpart, words in the singular form shall be...

21 CFR 101.10 - Nutrition labeling of restaurant foods.

Science.gov (United States)

2010-04-01

... 21 Food and Drugs 2 2010-04-01 2010-04-01 false Nutrition labeling of restaurant foods. 101.10... restaurant foods. Nutrition labeling in accordance with § 101.9 shall be provided upon request for any restaurant food or meal for which a nutrient content claim (as defined in § 101.13 or in subpart D of this...

34 CFR 101.3 - Use of gender and number.

Science.gov (United States)

2010-07-01

... 34 Education 1 2010-07-01 2010-07-01 false Use of gender and number. 101.3 Section 101.3 Education Regulations of the Offices of the Department of Education OFFICE FOR CIVIL RIGHTS, DEPARTMENT OF EDUCATION PRACTICE AND PROCEDURE FOR HEARINGS UNDER PART 100 OF THIS TITLE General Information § 101.3 Use of gender...

The GABAA receptor agonist THIP is neuroprotective in organotypic hippocampal slice cultures

DEFF Research Database (Denmark)

Kristensen, Bjarne Winther; Noraberg, Jens; Zimmer, Jens

2003-01-01

The potential neuroprotective effects of the GABA(A) receptor agonists THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) and muscimol, and the selective GluR5 kainate receptor agonist ATPA ((RS)-2-amino-3-(3-hydroxy-5-tert-butylisoxazol-4-yl)propanoic acid), which activates GABAergic interneu......The potential neuroprotective effects of the GABA(A) receptor agonists THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) and muscimol, and the selective GluR5 kainate receptor agonist ATPA ((RS)-2-amino-3-(3-hydroxy-5-tert-butylisoxazol-4-yl)propanoic acid), which activates GABAergic...... interneurons, were examined in hippocampal slice cultures exposed to N-methyl-D-aspartate (NMDA). The NMDA-induced excitotoxicity was quantified by densitometric measurements of propidium iodide (PI) uptake. THIP (100-1000 microM) was neuroprotective in slice cultures co-exposed to NMDA (10 microM) for 48 h......, while muscimol (100-1000 microM) and ATPA (1-3 microM) were without effect. The results demonstrate that direct GABA(A) agonism can mediate neuroprotection in the hippocampus in vitro as previously suggested in vivo....

24 CFR 941.101 - Purpose and scope.

Science.gov (United States)

2010-04-01

... housing residents over the long term and have the lowest possible life cycle costs, taking into account... 24 Housing and Urban Development 4 2010-04-01 2010-04-01 false Purpose and scope. 941.101 Section 941.101 Housing and Urban Development Regulations Relating to Housing and Urban Development (Continued...

41 CFR 101-5.303 - Guiding principles.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Guiding principles. 101-5... COMPLEXES 5.3-Federal Employee Health Services § 101-5.303 Guiding principles. The following principles will..., the compensation of the employees of the health unit, and other factors of medical economics prevalent...

27 CFR 21.101 - tert-Butyl alcohol.

Science.gov (United States)

2010-04-01

... 27 Alcohol, Tobacco Products and Firearms 1 2010-04-01 2010-04-01 false tert-Butyl alcohol. 21.101 Section 21.101 Alcohol, Tobacco Products and Firearms ALCOHOL AND TOBACCO TAX AND TRADE BUREAU, DEPARTMENT OF THE TREASURY LIQUORS FORMULAS FOR DENATURED ALCOHOL AND RUM Specifications for Denaturants § 21...

41 CFR 101-39.306 - Operator's packet.

Science.gov (United States)

2010-07-01

...-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.3-Use and Care of GSA Interagency Fleet Management System Vehicles § 101-39.306 Operator's packet. The GSA Interagency Fleet Management System (IFMS) will provide each... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Operator's packet. 101-39...

41 CFR 101-39.004 - Optional operations.

Science.gov (United States)

2010-07-01

...-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.0-General Provisions § 101-39.004 Optional operations. Nothing in this part shall preclude the establishment or operation of interagency fleet management systems by GSA or by... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Optional operations. 101...

48 CFR 15.101-1 - Tradeoff process.

Science.gov (United States)

2010-10-01

... 48 Federal Acquisition Regulations System 1 2010-10-01 2010-10-01 false Tradeoff process. 15.101-1... AND CONTRACT TYPES CONTRACTING BY NEGOTIATION Source Selection Processes and Techniques 15.101-1 Tradeoff process. (a) A tradeoff process is appropriate when it may be in the best interest of the...

41 CFR 101-4.525 - Fringe benefits.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Fringe benefits. 101-4... in Employment in Education Programs or Activities Prohibited § 101-4.525 Fringe benefits. (a) “Fringe benefits” defined. For purposes of these Title IX regulations, fringe benefits means: Any medical, hospital...

Primary root growth in Arabidopsis thaliana is inhibited by the miR159 mediated repression of MYB33, MYB65 and MYB101.

Science.gov (United States)

Xue, Tao; Liu, Zhenhua; Dai, Xuehuan; Xiang, Fengning

2017-09-01

Organ growth is a fundamental developmental process basing on cell proliferation and differentiation. The growth of the plant root is sustained by the activity of the root meristem, a process controlled in part by various transcription factors. Here, the miR159 has been identified as a post transcriptional repressor of root growth, on the basis that the mir159ab double mutant developed a larger meristem than did the wild type, and that it formed longer roots. In the mutant, the abundance of MYB33, MYB65 and MYB101 transcript was substantially increased. When MYB33, MYB65 and MYB101 were replaced by the miR159-resistant forms mMYB33, mMYB65 and mMYB101 respectively, the root meristem was similarly enlarged and the growth of the primary root enhanced. MYB65 activity promoted cell division in the root meristem by accelerating the cell cycle. The data suggest that miR159 acts as a key repressor of the primary root's growth, acting through its repression of MYB65 and consequent blocking of the cell cycle. Copyright © 2017 Elsevier B.V. All rights reserved.

Antineoplastic Effects of PPARγ Agonists, with a Special Focus on Thyroid Cancer.

Science.gov (United States)

Ferrari, Silvia Martina; Materazzi, Gabriele; Baldini, Enke; Ulisse, Salvatore; Miccoli, Paolo; Antonelli, Alessandro; Fallahi, Poupak

2016-01-01

Peroxisome Proliferator-Activated Receptor-γ (PPARγ) is a ligand-activated nuclear hormone receptor that functions as transcription factor and plays an important role in lipid metabolism and insulin sensitization. Recent studies have shown that PPARγ is overexpressed in many tumor types, including cancers of breast, lung, pancreas, colon, glioblastoma, prostate and thyroid differentiated/anaplastic cancers. These data suggest a role of PPARγ in tumor development and/or progression. PPARγ is emerging as a growth-limiting and differentiation-promoting factor, and it exerts a tumor suppressor role. Moreover, naturally-occurring and synthetic PPARγ agonists promote growth inhibition and apoptosis. Thiazolidinediones (TZDs) are synthetic agonists of PPARγ that were developed to treat type II diabetes. These compounds also display anticancer effects which appear mainly to be independent of their PPARγ agonist activity. Various preclinical and clinical studies strongly suggest a role for TZDs both alone and in combination with existing chemotherapeutic agents, for the treatment of cancer. Differentiation therapy involves the use of agents with the ability to induce differentiation in cells that have lost this ability, i.e. cancer cells, targeting pathways capable of re-activating blocked terminal differentiation programs. PPARγ agonists have been shown to induce differentiation in solid tumors such as thyroid differentiated/ anaplastic cancers and sarcomas. However, emerging data suggest that chronic use of TZDs is associated with increased risk of adverse cardiovascular events. The exploration of newer PPARγ agonists can help in unveiling the underlying mechanisms of these drugs, providing new molecules that are able to treat cancer, without increasing the cardiovascular risk of neoplastic patients.

PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR (PPAR) AGONISTS AS PROMISING NEW MEDICATIONS FOR DRUG ADDICTION: PRECLINICAL EVIDENCE

Science.gov (United States)

Foll, Bernard Le; Ciano, Patricia Di; Panlilio, Leigh V.; Goldberg, Steven R.; Ciccocioppo, Roberto

2013-01-01

This review examines the growing literature on the role of peroxisome proliferator-activated receptors (PPARs) in addiction. There are two subtypes of PPAR receptors that have been studied in addiction: PPAR-α and PPAR-γ. The role of each PPAR subtype in common models of addictive behavior, mainly pre-clinical models, is summarized. In particular, studies are reviewed that investigated the effects of PPAR-α agonists on relapse, sensitization, conditioned place preference, withdrawal and drug intake, and effects of PPAR-γ agonists on relapse, withdrawal and drug intake. Finally, studies that investigated the effects of PPAR agonists on neural pathways of addiction are reviewed. Taken together this preclinical data indicates that PPAR agonists are promising new medications for drug addiction treatment. PMID:23614675

Rapid internalization of the oncogenic K+ channel K(V10.1.

Directory of Open Access Journals (Sweden)

Tobias Kohl

Full Text Available K(V10.1 is a mammalian brain voltage-gated potassium channel whose ectopic expression outside of the brain has been proven relevant for tumor biology. Promotion of cancer cell proliferation by K(V10.1 depends largely on ion flow, but some oncogenic properties remain in the absence of ion permeation. Additionally, K(V10.1 surface populations are small compared to large intracellular pools. Control of protein turnover within cells is key to both cellular plasticity and homeostasis, and therefore we set out to analyze how endocytic trafficking participates in controlling K(V10.1 intracellular distribution and life cycle. To follow plasma membrane K(V10.1 selectively, we generated a modified channel of displaying an extracellular affinity tag for surface labeling by α-bungarotoxin. This modification only minimally affected K(V10.1 electrophysiological properties. Using a combination of microscopy and biochemistry techniques, we show that K(V10.1 is constitutively internalized involving at least two distinct pathways of endocytosis and mainly sorted to lysosomes. This occurs at a relatively fast rate. Simultaneously, recycling seems to contribute to maintain basal K(V10.1 surface levels. Brief K(V10.1 surface half-life and rapid lysosomal targeting is a relevant factor to be taken into account for potential drug delivery and targeting strategies directed against K(V10.1 on tumor cells.

Reports of pathological gambling, hypersexuality, and compulsive shopping associated with dopamine receptor agonist drugs.

Science.gov (United States)

Moore, Thomas J; Glenmullen, Joseph; Mattison, Donald R

2014-12-01

Severe impulse control disorders involving pathological gambling, hypersexuality, and compulsive shopping have been reported in association with the use of dopamine receptor agonist drugs in case series and retrospective patient surveys. These agents are used to treat Parkinson disease, restless leg syndrome, and hyperprolactinemia. To analyze serious adverse drug event reports about these impulse control disorders received by the US Food and Drug Administration (FDA) and to assess the relationship of these case reports with the 6 FDA-approved dopamine receptor agonist drugs. We conducted a retrospective disproportionality analysis based on the 2.7 million serious domestic and foreign adverse drug event reports from 2003 to 2012 extracted from the FDA Adverse Event Reporting System. Cases were selected if they contained any of 10 preferred terms in the Medical Dictionary for Regulatory Activities (MedDRA) that described the abnormal behaviors. We used the proportional reporting ratio (PRR) to compare the proportion of target events to all serious events for the study drugs with a similar proportion for all other drugs. We identified 1580 events indicating impulse control disorders from the United States and 21 other countries:710 fordopamine receptor agonist drugs and 870 for other drugs. The dopamine receptor agonist drugs had a strong signal associated with these impulse control disorders (n = 710; PRR = 277.6, P < .001). The association was strongest for the dopamine agonists pramipexole (n = 410; PRR = 455.9, P < .001) and ropinirole (n = 188; PRR = 152.5, P < .001), with preferential affinity for the dopamine D3 receptor. A signal was also seen for aripiprazole, an antipsychotic classified as a partial agonist of the D3 receptor (n = 37; PRR = 8.6, P < .001). Our findings confirm and extend the evidence that dopamine receptor agonist drugs are associated with these specific impulse control disorders. At present

Pharmacological characterization of 30 human melanocortin-4 receptor polymorphisms with the endogenous proopiomelanocortin-derived agonists, synthetic agonists, and the endogenous agouti-related protein antagonist.

Science.gov (United States)

Xiang, Zhimin; Proneth, Bettina; Dirain, Marvin L; Litherland, Sally A; Haskell-Luevano, Carrie

2010-06-08

The melanocortin-4 receptor (MC4R) is a G-protein-coupled receptor (GPCR) that is expressed in the central nervous system and has a role in regulating feeding behavior, obesity, energy homeostasis, male erectile response, and blood pressure. Since the report of the MC4R knockout mouse in 1997, the field has been searching for links between this genetic biomarker and human obesity and type 2 diabetes. More then 80 single nucleotide polymorphisms (SNPs) have been identified from human patients, both obese and nonobese controls. Many significant studies have been performed examining the pharmacological characteristics of these hMC4R SNPs in attempts to identify a molecular defects/insights that might link a genetic factor to the obese phenotype observed in patients possessing these mutations. Our laboratory has previously reported the pharmacological characterization of 40 of these polymorphic hMC4 receptors with multiple endogenous and synthetic ligands. The goal of the current study is to perform a similar comprehensive side-by-side characterization of 30 additional human hMC4R with single nucleotide polymorphisms using multiple endogenous agonists [alpha-, beta-, and gamma(2)-melanocyte stimulating hormones (MSH) and adrenocorticotropin (ACTH)], the antagonist agouti-related protein hAGRP(87-132), and synthetic agonists [NDP-MSH, MTII, and the tetrapeptide Ac-His-dPhe-Arg-Trp-NH(2) (JRH887-9)]. These in vitro data, in some cases, provide a putative molecular link between dysfunctional hMC4R's and human obesity. These 30 hMC4R SNPs include R7H, R18H, R18L, S36Y, P48S, V50M, F51L, E61K, I69T, D90N, S94R, G98R, I121T, A154D, Y157S, W174C, G181D, F202L, A219 V, I226T, G231S, G238D, N240S, C271R, S295P, P299L, E308K, I317V, L325F, and 750DelGA. All but the N240S hMC4R were identified in obese patients. Additionally, we have characterized a double I102T/V103I hMC4R. In addition to the pharmacological characterization, the hMC4R variants were evaluated for cell surface

Agonist-induced desensitization of human β3-adrenoceptors expressed in human embryonic kidney cells

NARCIS (Netherlands)

Michel-Reher, Martina B.; Michel, Martin C.

2013-01-01

β3-Adrenoceptors are resistant to agonist-induced desensitization in some cell types but susceptible in others including transfected human embryonic kidney (HEK) cells. Therefore, we have studied cellular and molecular changes involved in agonist-induced β3-adrenoceptor desensitization in HEK cells.

Development of specific dopamine D-1 agonists and antagonists

International Nuclear Information System (INIS)

Sakolchai, S.

1987-01-01

To develop potentially selective dopamine D-1 agonists and to investigate on the structural requirement for D-1 activity, the derivatives of dibenzocycloheptadiene are synthesized and pharmacologically evaluated. The target compounds are 5-aminomethyl-10,11-dihydro-1,2-dihydroxy-5H-dibenzo[a,d]cycloheptene hydrobromide 10 and 9,10-dihydroxy-1,2,3,7,8,12b-hexahydrobenzo[1,2]cyclohepta[3,4,5d,e]isoquinoline hydrobromide 11. In a dopamine-sensitive rat retinal adenylate cyclase assay, a model for D-1 activity, compound 10 is essentially inert for both agonist and antagonist activity. In contrast, compound 11 is approximately equipotent to dopamine in activation of the D-1 receptor. Based on radioligand and binding data, IC 50 of compound 11 for displacement of 3 H-SCH 23390, a D-1 ligand, is about 7 fold less than that for displacement of 3 H-spiperone, a D-2 ligand. These data indicate that compound 11 is a potent selective dopamine D-1 agonist. This study provides a new structural class of dopamine D-1 acting agent: dihydroxy-benzocycloheptadiene analog which can serve as a lead compound for further drug development and as a probe for investigation on the nature of dopamine D-1 receptor

Serotonin 2A receptor agonist binding in the human brain with [C]Cimbi-36

DEFF Research Database (Denmark)

Ettrup, A.; da Cunha-Bang, S.; McMahon, Barry P.

2014-01-01

[C]Cimbi-36 was recently developed as a selective serotonin 2A (5-HT) receptor agonist radioligand for positron emission tomography (PET) brain imaging. Such an agonist PET radioligand may provide a novel, and more functional, measure of the serotonergic system and agonist binding is more likely ....... Thus, we here describe [C]Cimbi-36 as the first agonist PET radioligand to successfully image and quantify 5-HT receptors in the human brain.Journal of Cerebral Blood Flow & Metabolism advance online publication, 30 April 2014; doi:10.1038/jcbfm.2014.68....... than antagonist binding to reflect 5-HT levels in vivo. Here, we show data from a first-in-human clinical trial with [C]Cimbi-36. In 29 healthy volunteers, we found high brain uptake and distribution according to 5-HT receptors with [C]Cimbi-36 PET. The two-tissue compartment model using arterial input...

Spinal Cord Injury 101

Medline Plus

Full Text Available ... Living with SCI Personal Experiences by Topic Resources Peer ... Adult Injuries Spinal Cord Injury 101 David Chen, MD Preventing Pressure Sores Mary Zeigler, MS Transition from Hospital to ...

Kv10.1 potassium channel: from the brain to the tumors.

Science.gov (United States)

Cázares-Ordoñez, V; Pardo, L A

2017-10-01

The KCNH1 gene encodes the Kv10.1 (Eag1) ion channel, a member of the EAG (ether-à-go-go) family of voltage-gated potassium channels. Recent studies have demonstrated that KCHN1 mutations are implicated in Temple-Baraitser and Zimmermann-Laband syndromes and other forms of developmental deficits that all present with mental retardation and epilepsy, suggesting that Kv10.1 might be important for cognitive development in humans. Although the Kv10.1 channel is mainly expressed in the mammalian brain, its ectopic expression occurs in 70% of human cancers. Cancer cells and tumors expressing Kv10.1 acquire selective advantages that favor cancer progression through molecular mechanisms that involve several cellular pathways, indicating that protein-protein interactions may be important for Kv10.1 influence in cell proliferation and tumorigenesis. Several studies on transcriptional and post-transcriptional regulation of Kv10.1 expression have shown interesting mechanistic insights about Kv10.1 role in oncogenesis, increasing the importance of identifying the cellular factors that regulate Kv10.1 expression in tumors.

47 CFR 101.503 - Digital Electronic Message Service Nodal Stations.

Science.gov (United States)

2010-10-01

... Service § 101.503 Digital Electronic Message Service Nodal Stations. 10.6 GHz DEMS Nodal Stations may be... 47 Telecommunication 5 2010-10-01 2010-10-01 false Digital Electronic Message Service Nodal Stations. 101.503 Section 101.503 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) SAFETY...

Solar 101 STAT Webinars | State, Local, and Tribal Governments | NREL

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101 STAT Webinars Solar 101 STAT Webinars The Solar 101 series represents the foundation of the Solar Technical Assistance Team (STAT) webinars, which are organized by the DOE Solar Office in coordination with the National Renewable Energy Laboratory (NREL). The following sessions are available: Solar

41 CFR 101-8.310 - New construction.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true New construction. 101-8... FINANCIAL ASSISTANCE 8.3-Discrimination Prohibited on the Basis of Handicap § 101-8.310 New construction. (a) Design and construction. Each facility or part of a facility constructed by, on behalf of, or for the use...

The effects of the dopamine agonist rotigotine on hemispatial neglect following stroke

OpenAIRE

Gorgoraptis, Nikos; Mah, Yee-Haur; Machner, Bjoern; Singh-Curry, Victoria; Malhotra, Paresh; Hadji-Michael, Maria; Cohen, David; Simister, Robert; Nair, Ajoy; Kulinskaya, Elena; Ward, Nick; Greenwood, Richard; Husain, Masud

2012-01-01

Hemispatial neglect following right-hemisphere stroke is a common and disabling disorder, for which there is currently no effective pharmacological treatment. Dopamine agonists have been shown to play a role in selective attention and working memory, two core cognitive components of neglect. Here, we investigated whether the dopamine agonist rotigotine would have a beneficial effect on hemispatial neglect in stroke patients. A double-blind, randomized, placebo-controlled ABA design was used, ...

Potential of beta-adrenergic agonists for increasing protein deposition in ruminants in developing countries

International Nuclear Information System (INIS)

Berschauer, F.

1989-01-01

Various substituted phenylethanolamines, acting on the sympathetic nervous system, have been shown to increase protein retention (via decreased proteolysis) and reduce fat deposition (via increased lipolysis and reduced lipogenesis) in ruminants and monogastrics. Research with finishing lambs in developed countries show various beta-adrenergic agonists to improve growth rate (by 18%), feed conversion (by 12%) and carcass quality (28% increase in area of longissimus dorsi and 33% reduction in subcutaneous fat). Similar effects of beta-agonists on carcass composition of well fed cattle have been reported. The effects of beta-agonists on livestock in developing countries of the tropics have not yet been investigated, but their effects in increasing metabolic rate suggest that treated ruminants would be more vulnerable to hot environments. Beta-agonists appear to improve nitrogen retention to a greater extent in breeds with a lower potential for muscle growth. In view of this, they might be particularly effective in improving nitrogen retention in tropical breeds which have a low growth potential. This aspect, together with the response of undernourished animals in the developing countries, needs investigation. Beta-adrenergic agonists are not yet registered for use in animal production, but product licenses for some of them are expected to be granted soon. (author). 31 refs, 1 fig., 12 tabs

Transcriptome analysis of endometrial tissues following GnRH agonist treatment in a mouse adenomyosis model

Directory of Open Access Journals (Sweden)

Guo S

2017-03-01

Full Text Available Song Guo,1,* Xiaowei Lu,1,* Ruihuan Gu,2 Di Zhang,3 Yijuan Sun,2 Yun Feng1 1Department of Obstetrics and Gynecology, Reproductive Medicine Center, Ruijin Hospital Affiliated to Shanghai Jiaotong University School of Medicine, Shanghai, People’s Republic of China; 2Gynecology, Shanghai Ji Ai Genetics & In Vitro Fertilization Institute, Obstetrics and Gynecology Hospital, Fudan University, Shanghai, People’s Republic of China; 3Department of Gynecology and Obstetrics, Jinan Military General Hospital, Jinan, People’s Republic of China *These authors contributed equally to this work Purpose: Adenomyosis is a common, benign gynecological condition of the female reproductive tract characterized by heavy menstrual bleeding and dysmenorrhea. Gonadotropin-releasing hormone (GnRH agonists are one of the medications used in adenomyosis treatment; however, their underlying mechanisms are poorly understood. Moreover, it is difficult to obtain endometrial samples from women undergoing such treatment. To overcome this, we generated an adenomyosis mouse model, which we treated with an GnRH agonist to determine its effect on pregnancy outcomes. We also analyzed endometrial gene expression following GnRH agonist treatment to determine the mechanisms that may affect pregnancy outcome in individuals with adenomyosis.Methods: Neonatal female mice were divided into a control group, an untreated adenomyosis group, and an adenomyosis group treated with a GnRH agonist (n=6 each. The pregnancy outcome was observed and compared among the groups. Then, three randomly chosen transcriptomes from endometrial tissues from day 4 of pregnancy were analyzed between the adenomyosis group and the GnRH agonist treatment group by RNA sequencing and quantitative reverse transcription polymerase chain reaction (PCR.Results: The litter size was significantly smaller in the adenomyosis group than in the control group (7±0.28 vs 11±0.26; P<0.05. However, the average live litter

Library 101: Why, How, and Lessons Learned

Science.gov (United States)

Porter, Michael; King, David Lee

2010-01-01

This article describes how and why the Library 101 Project was created and the lessons that the developers learned out of this project. The Library 101 is a project that challenges librarians to revise the paradigm of "basic" library services in order to remain relevant in this technology-driven world. It was developed by Michael Porter,…

Spinal Cord Injury 101

Medline Plus

Full Text Available ... How Peer Counseling Works Julie Gassaway, MS, RN Pediatric Injuries Pediatric Spinal Cord Injury 101 Lawrence Vogel, MD The Basics of Pediatric SCI Rehabilitation Sara Klaas, MSW Transitions for Children ...

Spinal Cord Injury 101

Medline Plus

Full Text Available ... Medical Experts People Living with SCI Personal Experiences by Topic Resources Peer ... Injuries Spinal Cord Injury 101 David Chen, MD Preventing Pressure Sores Mary Zeigler, MS Transition from Hospital to ...

Innate Immune Responses to TLR2 and TLR4 Agonists Differ between Baboons, Chimpanzees and Humans

Science.gov (United States)

Brinkworth, Jessica F.; Pechenkina, Ekaterina A.; Silver, Jack; Goyert, Sanna M.

2012-01-01

Background African catarrhine primates differ in bacterial disease susceptibility. Methods Human, chimpanzee, and baboon blood was stimulated with TLR-detected bacterial agonists and cytokine/chemokine induction assessed by real-time pcr. Results Humans and chimpanzees shared similar cytokine/chemokine responses, while baboon cytokine/chemokine induction differed. Generally, responses were agonist-independent. Conclusions These primates tend to generate species rather than agonist–specific responses to bacterial agonists. PMID:22978822

Food Allergy 101 | NIH MedlinePlus the Magazine

Science.gov (United States)

... issue contents Food Allergy 101 Follow us Food Allergy 101 What is a food allergy? In a person with a food allergy, the ... be life-threatening. What foods commonly cause an allergy? Foods that often cause allergic reactions in adults ...

48 CFR 1649.101-71 - FEHBP termination for convenience clause.

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2010-10-01

... 48 Federal Acquisition Regulations System 6 2010-10-01 2010-10-01 true FEHBP termination for convenience clause. 1649.101-71 Section 1649.101-71 Federal Acquisition Regulations System OFFICE OF PERSONNEL... CONTRACTS General Principles 1649.101-71 FEHBP termination for convenience clause. The clause set forth in...

Tank 241-AZ-101 tank characterization plan

International Nuclear Information System (INIS)

Schreiber, R.D.

1995-01-01

The Defense Nuclear Facilities Safety Board has advised the DOE to concentrate the near-term sampling and analysis activities on identification and resolution of safety issues. The Data Quality Objective (DQO) process was chosen as a tool to be used in the resolution of safety issues. As a result, A revision in the Federal Facilities Agreement and Consent Order (Tri-Party Agreement) milestone M-44 has been made, which states that ''A Tank Characterization Plan (TCP) will also be developed for each double-shell tank (DST) and single-shell tank (SST) using the DQO process. Development of TCPs by the DQO process is intended to allow users to ensure their needs will be met and that resources are devoted to gaining only necessary information''. This document satisfies that requirement for Tank 241-AZ-101 (AZ-101) sampling activities. Tank AZ-101 is currently a non-Watch List tank, so the only DQOs applicable to this tank are the safety screening DQO and the compatibility DQO, as described below. The contents of Tank AZ-101, as of October 31, 1994, consisted of 3,630 kL (960 kgal) of dilute non-complexed waste and aging waste from PUREX (NCAW, neutralized current acid waste). Tank AZ-101 is expected to have two primary layers. The bottom layer is composed of 132 kL of sludge, and the top layer is composed of 3,500 kL of supernatant, with a total tank waste depth of approximately 8.87 meters

Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists.

Science.gov (United States)

Maruyama, Tatsuya; Onda, Kenichi; Hayakawa, Masahiko; Matsui, Tetsuo; Takasu, Toshiyuki; Ohta, Mitsuaki

2009-06-01

In the search for potent and selective human beta3-adrenergic receptor (AR) agonists as potential drugs for the treatment of obesity and noninsulin-dependent (type II) diabetes, a novel series of acetanilide-based analogues were prepared and their biological activities were evaluated at the human beta3-, beta2-, and beta1-ARs. Among these compounds, 2-pyridylacetanilide (2f), pyrimidin-2-ylacetanilide (2u), and pyrazin-2-ylacetanilide (2v) derivatives exhibited potent agonistic activity at the beta3-AR with functional selectivity over the beta1- and beta2-ARs. In particular, compound 2u was found to be the most potent and selective beta3-AR agonist with an EC(50) value of 0.11 microM and no agonistic activity for either the beta1- or beta2-AR. In addition, 2f, 2u, and 2v showed significant hypoglycemic activity in a rodent diabetic model.

Inhibitory GTP binding protein G/sub i/ regulates β-adrenoceptor affinity towards β-agonists

International Nuclear Information System (INIS)

Marbach, I.; Levitzki, A.

1987-01-01

Treatment of S-49 lymphoma cell membranes with pertussis toxin (PT) causes a three-fold reduction of β-adrenoceptor (βAR) affinity towards isoproterenol. A similar treatment with cholera toxin (CT) does not cause such a modulation. The effects were studied by the detailed analysis of 125 I-cyanopindolol (CYP) binding curves in the absence and presence of increasing agonist concentrations. Thus, the authors were able to compare in detail the effects of G/sub s/ and G/sub i/ on the agonist-associated state of the βAR. In contrast to these findings, PT treatment does not have any effect on the displacement of 125 I-CYP by (-)isoproterenol. These results demonstrate that the inhibitory GTP protein G/sub i/ modulates the βAR affinity towards β-agonists. This might be due to the association of G/sub i/ with the agonist-bound βAR x G/sub s/ x C complex within the membrane. This hypothesis, as well as others, is under investigation

Activation of Cyclic AMP Synthesis by Full and Partial Beta-Adrenergic Receptor Agonists in Chicken Skeletal Muscle Cells

Science.gov (United States)

Young, R. B.; Bridge, K. Y.

2003-01-01

Several beta-adrenergic receptor (bAR) agonists are known to cause hypertrophy of skeletal muscle tissue. Accordingly, five bAR agonists encompassing a range in activity from strong to weak were evaluated for their ability to stimulate CAMP accumulation in embryonic chicken skeletal muscle cells in culture. Two strong agonists (epinephrine and isoproterenol), one moderate agonist (albuterol), and two weak agonists known to cause hypertrophy in animals (clenbuterol and cimaterol) were studied. Dose response curves were determined over six orders of magnitude in concentration for each agonist, and values were determined for their maximum stimulation of CAMP synthesis rate (Bmax) and the agonist concentration at which 50% stimulation of CAMP synthesis (EC50) occurred. Bmax values decreased in the following order: isoproterenol, epinephrine, albuterol, cimaterol, clenbuterol. Cimaterol and clenbuterol at their Bmax concentrations were approximately 15-fold weaker than isoproterenol in stimulating the rate of CAMP synthesis. When cimaterol and clenbuterol were added to culture media at concentrations known to cause significant muscle hypertrophy in animals, there was no detectable effect on stimulation of CAMP synthesis. Finally, these same levels of cimaterol and clenbuterol did not antagonize the stimulation of CAMP by either epinephrine or isoproterenol.

Muscarinic Receptor Agonists and Antagonists

Directory of Open Access Journals (Sweden)

David R. Kelly

2001-02-01

Full Text Available A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the treatment of Alzheimer’s disease are discussed. A selection of chemical routes are described, which illustrate contemporary methodology for the synthesis of chiral medicinal compounds (asymmetric synthesis, chiral pool, enzymes. Routes to bicyclic intrannular amines and intramolecular Diels-Alder reactions are highlighted.

Effects of cannabinoid and vanilloid receptor agonists and their interaction on learning and memory in rats.

Science.gov (United States)

Shiri, Mariam; Komaki, Alireza; Oryan, Shahrbanoo; Taheri, Masoumeh; Komaki, Hamidreza; Etaee, Farshid

2017-04-01

Despite previous findings on the effects of cannabinoid and vanilloid systems on learning and memory, the effects of the combined stimulation of these 2 systems on learning and memory have not been studied. Therefore, in this study, we tested the interactive effects of cannabinoid and vanilloid systems on learning and memory in rats by using passive avoidance learning (PAL) tests. Forty male Wistar rats were divided into the following 4 groups: (1) control (DMSO+saline), (2) WIN55,212-2, (3) capsaicin, and (4) WIN55,212-2 + capsaicin. On test day, capsaicin, a vanilloid receptor type 1 (TRPV1) agonist, or WIN55,212-2, a cannabinoid receptor (CB 1 /CB 2 ) agonist, or both substances were injected intraperitoneally. Compared to the control group, the group treated with capsaicin (TRPV1 agonist) had better scores in the PAL acquisition and retention test, whereas treatment with WIN55,212-2 (CB 1 /CB 2 agonist) decreased the test scores. Capsaicin partly reduced the effects of WIN55,212-2 on PAL and memory. We conclude that the acute administration of a TRPV1 agonist improves the rats' cognitive performance in PAL tasks and that a vanilloid-related mechanism may underlie the agonistic effect of WIN55,212-2 on learning and memory.

41 CFR 101-27.206 - Procurement of shelf-life materials.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Procurement of shelf-life materials. 101-27.206 Section 101-27.206 Public Contracts and Property Management Federal Property... MANAGEMENT 27.2-Management of Shelf-Life Materials § 101-27.206 Procurement of shelf-life materials. ...

41 CFR 101-27.506 - Determination of acceptability for credit.

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2010-07-01

...-INVENTORY MANAGEMENT 27.5-Return of GSA Stock Items § 101-27.506 Determination of acceptability for credit... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Determination of acceptability for credit. 101-27.506 Section 101-27.506 Public Contracts and Property Management Federal...

41 CFR 101-39.4901 - Obtaining standard and optional forms.

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2010-07-01

... VEHICLES 39-INTERAGENCY FLEET MANAGEMENT SYSTEMS 39.49-Forms § 101-39.4901 Obtaining standard and optional... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Obtaining standard and optional forms. 101-39.4901 Section 101-39.4901 Public Contracts and Property Management Federal Property...

Acceptance/operational test procedure 101-AW tank camera purge system and 101-AW video camera system

International Nuclear Information System (INIS)

Castleberry, J.L.

1994-01-01

This procedure will document the satisfactory operation of the 101-AW Tank Camera Purge System (CPS) and the 101-AW Video Camera System. The safety interlock which shuts down all the electronics inside the 101-AW vapor space, during loss of purge pressure, will be in place and tested to ensure reliable performance. This procedure is separated into four sections. Section 6.1 is performed in the 306 building prior to delivery to the 200 East Tank Farms and involves leak checking all fittings on the 101-AW Purge Panel for leakage using a Snoop solution and resolving the leakage. Section 7.1 verifies that PR-1, the regulator which maintains a positive pressure within the volume (cameras and pneumatic lines), is properly set. In addition the green light (PRESSURIZED) (located on the Purge Control Panel) is verified to turn on above 10 in. w.g. and after the time delay (TDR) has timed out. Section 7.2 verifies that the purge cycle functions properly, the red light (PURGE ON) comes on, and that the correct flowrate is obtained to meet the requirements of the National Fire Protection Association. Section 7.3 verifies that the pan and tilt, camera, associated controls and components operate correctly. This section also verifies that the safety interlock system operates correctly during loss of purge pressure. During the loss of purge operation the illumination of the amber light (PURGE FAILED) will be verified

Molecular interactions of agonist and inverse agonist ligands at serotonin 5-HT2C G protein-coupled receptors: computational ligand docking and molecular dynamics studies validated by experimental mutagenesis results

Science.gov (United States)

Córdova-Sintjago, Tania C.; Liu, Yue; Booth, Raymond G.

2015-02-01

To understand molecular determinants for ligand activation of the serotonin 5-HT2C G protein-coupled receptor (GPCR), a drug target for obesity and neuropsychiatric disorders, a 5-HT2C homology model was built according to an adrenergic β2 GPCR (β2AR) structure and validated using a 5-HT2B GPCR crystal structure. The models were equilibrated in a simulated phosphatidyl choline membrane for ligand docking and molecular dynamics studies. Ligands included (2S, 4R)-(-)-trans-4-(3'-bromo- and trifluoro-phenyl)-N,N-dimethyl-1,2,3,4-tetrahydronaphthalene-2-amine (3'-Br-PAT and 3'-CF3-PAT), a 5-HT2C agonist and inverse agonist, respectively. Distinct interactions of 3'-Br-PAT and 3'-CF3-PAT at the wild-type (WT) 5-HT2C receptor model were observed and experimental 5-HT2C receptor mutagenesis studies were undertaken to validate the modelling results. For example, the inverse agonist 3'-CF3-PAT docked deeper in the WT 5-HT2C binding pocket and altered the orientation of transmembrane helices (TM) 6 in comparison to the agonist 3'-Br-PAT, suggesting that changes in TM orientation that result from ligand binding impact function. For both PATs, mutation of 5-HT2C residues S3.36, T3.37, and F5.47 to alanine resulted in significantly decreased affinity, as predicted from modelling results. It was concluded that upon PAT binding, 5-HT2C residues T3.37 and F5.47 in TMs 3 and 5, respectively, engage in inter-helical interactions with TMs 4 and 6, respectively. The movement of TMs 5 and 6 upon agonist and inverse agonist ligand binding observed in the 5-HT2C receptor modelling studies was similar to movements reported for the activation and deactivation of the β2AR, suggesting common mechanisms among aminergic neurotransmitter GPCRs.

The emergence of devastating impulse control disorders during dopamine agonist therapy of the restless legs syndrome.

Science.gov (United States)

Dang, Dien; Cunnington, David; Swieca, John

2011-01-01

The Restless Legs Syndrome is a common sensorimotor disorder, typically amenable to treatment with dopamine agonist therapy. Dopamine agonists have been associated with emergent impulse control disorders (ICDs) when used in patients with Parkinson disease, and ICDs have now been reported in individuals with RLS on dopamine agonist therapy. Our aim was to characterize cases of emergent ICDs in Australian patients with focus on the dopamine agonists implicated and the social significance of ICDs. A series of RLS patients on dopamine agonist therapy were identified with ICDs over a 2-year period. Additional cases of ICDs were found using a mailout questionnaire designed to capture those with high impulsivity. These patients were assessed using the Barratt Impulsiveness Scale, Version 11, and a modified Minnesota Impulse Disorders Interview. Case records and medication schedules were evaluated. Twelve cases of patients with de novo ICDs were found with a range of impulsive behaviors including pathological gambling, kleptomania, compulsive shopping, and hypersexuality. Criminality, suicidality, and marital discord also were featured. These occurred over a wide range of latencies and l-dopa exposures. This group of Australian RLS patients with ICDs display high levels of impulsivity and is the first to use the BIS-11 questionnaire in this setting. Impulse control disorders can occur over a wide range of dopamine agonist therapy types and dose exposures. Impulse control disorder tendencies may persist, despite withdrawal of dopamine agonists. The emergence of ICDs needs careful consideration in light of their potentially devastating financial, social, and marital consequences.

41 CFR 101-27.500 - Scope and applicability of subpart.

Science.gov (United States)

2010-07-01

... MANAGEMENT 27.5-Return of GSA Stock Items § 101-27.500 Scope and applicability of subpart. This subpart sets... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Scope and applicability of subpart. 101-27.500 Section 101-27.500 Public Contracts and Property Management Federal Property...

Assembly of high-affinity insulin receptor agonists and antagonists from peptide building blocks

Science.gov (United States)

Schäffer, Lauge; Brissette, Renee E.; Spetzler, Jane C.; Pillutla, Renuka C.; Østergaard, Søren; Lennick, Michael; Brandt, Jakob; Fletcher, Paul W.; Danielsen, Gillian M.; Hsiao, Ku-Chuan; Andersen, Asser S.; Dedova, Olga; Ribel, Ulla; Hoeg-Jensen, Thomas; Hansen, Per Hertz; Blume, Arthur J.; Markussen, Jan; Goldstein, Neil I.

2003-01-01

Insulin is thought to elicit its effects by crosslinking the two extracellular α-subunits of its receptor, thereby inducing a conformational change in the receptor, which activates the intracellular tyrosine kinase signaling cascade. Previously we identified a series of peptides binding to two discrete hotspots on the insulin receptor. Here we show that covalent linkage of such peptides into homodimers or heterodimers results in insulin agonists or antagonists, depending on how the peptides are linked. An optimized agonist has been shown, both in vitro and in vivo, to have a potency close to that of insulin itself. The ability to construct such peptide derivatives may offer a path for developing agonists or antagonists for treatment of a wide variety of diseases. PMID:12684539

Gigantism: X-linked acrogigantism and GPR101 mutations.

Science.gov (United States)

Iacovazzo, Donato; Korbonits, Márta

X-linked acrogigantism (XLAG) is a recently identified condition of early-onset GH excess resulting from the germline or somatic duplication of the GPR101 gene on chromosome Xq26.3. Thirty patients have been formally reported so far. The disease affects mostly females, occurs usually sporadically, and is characterised by early onset and marked overgrowth. Most patients present with concomitant hyperprolactinaemia. Histopathology shows pituitary hyperplasia or pituitary adenoma with or without associated hyperplasia. XLAG-related pituitary adenomas present peculiar histopathological features that should contribute to raise the suspicion of this rare condition. Treatment is frequently challenging and multi-modal. While females present with germline mutations, the sporadic male patients reported so far were somatic mosaics with variable levels of mosaicism, although no differences in the clinical phenotype were observed between patients with germline or somatic duplication. The GPR101 gene encodes an orphan G protein-coupled receptor normally expressed in the central nervous system, and at particularly high levels in the hypothalamus. While the physiological function and the endogenous ligand of GPR101 are unknown, the high expression of GPR101 in the arcuate nucleus and the occurrence of increased circulating GHRH levels in some patients with XLAG, suggest that increased hypothalamic GHRH secretion could play a role in the pathogenesis of this condition. In this review, we summarise the published evidence on XLAG and GPR101 and discuss the results of recent studies that have investigated the potential role of GPR101 variants in the pathogenesis of pituitary adenomas. Copyright © 2016 Elsevier Ltd. All rights reserved.

Pharmacological Characterization of 30 Human Melanocortin-4 Receptor Polymorphisms with the Endogenous Proopiomelanocortin Derived Agonists, Synthetic Agonists, and the Endogenous Agouti-Related Protein (AGRP) Antagonist

Science.gov (United States)

Xiang, Zhimin; Proneth, Bettina; Dirain, Marvin L.; Litherland, Sally A.; Haskell-Luevano, Carrie

2010-01-01

The melanocortin-4 receptor (MC4R) is a G-protein coupled receptor (GPCR) that is expressed in the central nervous system and has a role in regulating feeding behavior, obesity, energy homeostasis, male erectile response, and blood pressure. Since the report of the MC4R knockout mouse in 1997, the field has been searching for links between this genetic bio marker and human obesity and type 2 diabetes. More then 80 single nucleotide polymorphisms (SNPs) have been identified from human patients, both obese and non-obese controls. Many significant studies have been performed examining the pharmacological characteristics of these hMC4R SNPs in attempts to identify a molecular defects/insights that might link a genetic factor to the obese phenotype observed in patients possessing these mutations. Our laboratory has previously reported the pharmacological characterization of 40 of these polymorphic hMC4 receptors with multiple endogenous and synthetic ligands. The goal of the current study is to perform a similar comprehensive side-by-side characterization of 30 additional human hMC4R with single nucleotide polymorphisms using multiple endogenous agonists [α-, β, γ2-melanocyte stimulating hormones (MSH) and adrenocorticotropin (ACTH)], the antagonist agouti-related protein hAGRP(87-132), and synthetic agonists [NDP-MSH, MTII, and the tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 (JRH887-9)]. These in vitro data, in some cases, provide a putative molecular link between dysfunctional hMC4R's and human obesity. These 30 hMC4R SNPs include R7H, R18H, R18L, S36Y, P48S, V50M, F51L, E61K, I69T, D90N, S94R, G98R, I121T, A154D, Y157S, W174C, G181D, F202L, A219V, I226T, G231S, G238D, N240S, C271R, S295P, P299L, E308K, I317V, L325F and 750DelGA. All but the N240S hMC4R were identified in obese patients. Additionally, we have characterized a double I102T/V103I hMC4R. In addition to the pharmacological characterization, the hMC4R variants were evaluated for cell surface expression by flow

Peroxisome proliferator-activated receptor-gamma agonists suppress tissue factor overexpression in rat balloon injury model with paclitaxel infusion.

Directory of Open Access Journals (Sweden)

Jun-Bean Park

Full Text Available The role and underlying mechanisms of rosiglitazone, a peroxisome proliferator-activated receptor-gamma (PPAR-γ agonist, on myocardial infarction are poorly understood. We investigated the effects of this PPAR-γ agonist on the expression of tissue factor (TF, a primary molecule for thrombosis, and elucidated its underlying mechanisms. The PPAR-γ agonist inhibited TF expression in response to TNF-α in human umbilical vein endothelial cells, human monocytic leukemia cell line, and human umbilical arterial smooth muscle cells. The overexpression of TF was mediated by increased phosphorylation of mitogen-activated protein kinase (MAPK, which was blocked by the PPAR-γ agonist. The effective MAPK differed depending on each cell type. Luciferase and ChIP assays showed that transcription factor, activator protein-1 (AP-1, was a pivotal target of the PPAR-γ agonist to lower TF transcription. Intriguingly, two main drugs for drug-eluting stent, paclitaxel or rapamycin, significantly exaggerated thrombin-induced TF expression, which was also effectively blocked by the PPAR-γ agonist in all cell types. This PPAR-γ agonist did not impair TF pathway inhibitor (TFPI in three cell types. In rat balloon injury model (Sprague-Dawley rats, n = 10/group with continuous paclitaxel infusion, the PPAR-γ agonist attenuated TF expression by 70±5% (n = 4; P<0.0001 in injured vasculature. Taken together, rosiglitazone reduced TF expression in three critical cell types involved in vascular thrombus formation via MAPK and AP-1 inhibitions. Also, this PPAR-γ agonist reversed the paclitaxel-induced aggravation of TF expression, which suggests a possibility that the benefits might outweigh its risks in a group of patients with paclitaxel-eluting stent implanted.

41 CFR 101-26.308 - Obtaining filing cabinets.

Science.gov (United States)

2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Obtaining filing cabinets. 101-26.308 Section 101-26.308 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND...

41 CFR 101-26.509 - Tabulating machine cards.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Tabulating machine cards. 101-26.509 Section 101-26.509 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND...

41 CFR 101-26.300 - Scope of subpart.

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2010-07-01

... 41 Public Contracts and Property Management 2 2010-07-01 2010-07-01 true Scope of subpart. 101-26.300 Section 101-26.300 Public Contracts and Property Management Federal Property Management Regulations System FEDERAL PROPERTY MANAGEMENT REGULATIONS SUPPLY AND PROCUREMENT 26-PROCUREMENT SOURCES AND...

AGONISTIC BEHAVIOR OF LABORATORY MICE

Directory of Open Access Journals (Sweden)

D. Cinghiţă

2005-01-01

Full Text Available In this work we study agonistic behavior of laboratory white mice when they are kept in captivity. For all this experimental work we used direct observation of mice, in small lists, because we need a reduced space to emphasize characteristics of agonistic behavior. Relations between members of the same species that live in organized groups are based in most cases on hierarchical structure. Relations between leader and subservient, decided by fighting, involve a thorough observation between individuals. Each member of a group has its own place on the ierarchical scale depending on resultes of fhights – it can be leader or it can be subsurvient, depending on if it wines or looses the fight. Once hierarchical scale made, every animal will adjust its behavior. After analyzing the obtained data we have enough reasons to believe that after fights the winner, usually, is the massive mouse, but it is also very important the sexual ripeness, so the immature male will be beaten. The leader male had a big exploring area and it checks up all territory.The females can be more aggressive, its fights are more brutal, than male fights are, when they fight for supremacy, but in this case fights are not as frequent as in the case of males. Always the superior female, on hierarchical scale, shows males its own statute, so the strongest genes will be perpetuated.