UK PubMed Central (United Kingdom)

Fatalities caused by parasitic infections often occur as a result of tissue injury that results from a form of host-cell death known as apoptosis. However, instead of being pathogenic, parasite-induced...Full Text Available

UK PubMed Central (United Kingdom)

Approximately 65% of PSI structures report some type of ligand(s) that is bound in the crystal structure. Here, a description is given of how such ligands are handled and analyzed at the JCSG and a...Full Text Available

British Library Electronic Table of Contents (United Kingdom)

DFNA5 was first identified as a gene causing autosomal dominant hearing loss (HL). Different mutations have been found, all exerting a highly specific gain-of-function effect, in which skipping of exon 8 causes the HL. Later reports revealed the involvement of the gene in different types of cancer. Epigenetic silencing of DFNA5 in a large percentage of gastric, colorectal and breast tumors and p53-dependent transcriptional activity have been reported, concluding that DFNA5 acts as a tumor suppressor gene in different frequent types of cancer. Despite these data, the molecular function of DFNA5 has not been investigated properly. Previous transfection studies with mutant DFNA5 in yeast and in mammalian cells showed a toxic effect of the mutant protein, which was not seen after transfection ...

British Library Electronic Table of Contents (United Kingdom)

Mammary glands are special tissue characterized by proliferation of the epithelium, during puberty and pregnancy and by programmed cell death, during involution. In this study, apoptosis was identified by TUNEL staining and then related to cell proliferation, as determined by Ki-67 staining. The apoptotic index was at its highest at 8 days of involution, whereas the proliferation index was at its highest during lactation. Caspase-3 was immunolocalised only in mast cells and along the basal membrane in the mammary tissue at -10 days from lambing, 150 days of lactation and at 8 days of involution. This finding could indicate that caspase-3 is not involved in sheep mammary gland apoptosis, but that other proteins - such as apoptosis inducing factor (AIF) - can trigger apoptosis, through the m...

UK PubMed Central (United Kingdom)

ABSTRACTPurpose: To describe previously reported locomotor muscle and whole-body composition factors related to mobility in older individuals.Methods:...Full Text Available

International Nuclear Information System (INIS)

Morusin is a pure compound isolated from root bark of Morusaustralis (Moraceae). In this study, we demonstrated that morusin significantly inhibited the growth and clonogenicity of human colorectal cancer HT-29 cells. Apoptosis induced by morusin was characterized by accumulation of cells at the sub-G_1 phase, fragmentation of DNA, and condensation of chromatin. Morusin also inhibited the phosphorylation of IKK-#alpha#, IKK-#beta# and I#kappa#B-#alpha#, increased expression of I#kappa#B-#alpha#, and suppressed nuclear translocation of NF-#kappa#B and its DNA binding activity. Dephosphorylation of NF-#kappa#B upstream regulators PI3K, Akt and PDK1 was also displayed. In addition, activation of caspase-8, change of mitochondrial membrane potential, release of cytochrome c and Smac/DIABLO, and activation of caspase-9 and -3 were observed at the early time point. Downregulation in the expression of Ku70 and XIAP was exhibited afterward. Caspase-8 ...

Energy Technology Data Exchange (ETDEWEB)

No abstract prepared.

British Library Electronic Table of Contents (United Kingdom)

An aliphatic thiol ligand of CuInS2/ZnS core/shell quantum dots is replaced with a hydroxyl-terminated thiol ligand by utilizing `on-off state' of ligands during growth stage of the quantum dots. After the ligand-exchange, negligible differences were observed on both photoluminescence spectrum and luminescent quantum efficiency. The reason for the high retention of luminescent efficiency comes from no local agglomeration and no surface deterioration of QDs. It is also observed that 70% of initial ligands are exchanged by the replacing ligand, determined by FT-IR and 1H NMR. The proposed method provides the quantum dots with an excellent dispersibility in polar solvents, supported by identical luminescence decay characteristics of the QDs.

UK PubMed Central (United Kingdom)

OBJECTIVEThis randomized, four-arm, placebo-controlled, dose-ranging phase 2 trial was conducted to determine whether repeated subcutaneous injections of the altered peptide ligand,...Full Text Available

UK PubMed Central (United Kingdom)

Ligand exchange of hydrated metal complexes is common in chemical and biological systems. Using the ultrafast T-jump, we examined this process, specifically the transformation of aqua cobalt (II) complexes...Full Text Available

Science.gov (United States)

The thermodynamics of protonation and europium(III) complex formation with substituted methane diphosphonic acids have been reported recently. These ligands form strong complexes with europium in moderately acidic solutions ((H{sup +}) {ge} 0.1 M), conditions not conducive to complexation by most carboxylate and aminopolycarboxylate ligands. A correlation of log {beta} vs pK{sub a} values for phosphonate and carboxylate ligands is used to explore the effect of ligand structure on complex stability. 5 refs., 1 fig.

International Nuclear Information System (INIS)

Short communication.

Energy Technology Data Exchange (ETDEWEB)

Peroxisome proliferator activated receptor-{gamma} (PPAR{gamma}) regulates metabolic homeostasis and adipocyte differentiation, and it is activated by oxidized and nitrated fatty acids. Here we report the crystal structure of the PPAR{gamma} ligand binding domain bound to nitrated linoleic acid, a potent endogenous ligand of PPAR{gamma}. Structural and functional studies of receptor-ligand interactions reveal the molecular basis of PPAR{gamma} discrimination of various naturally occurring fatty acid derivatives.

International Nuclear Information System (INIS)

Scandium reacts with 4-(2-pyridylazo)resorcinol in the presence of monocarboxylic acids (X) to form mixed-ligand complexes with a Sc:PAR:x ratio of 1:2:2. The chemical nature of this interaction has been established, and the extraction of these mixed-ligand complexes has also been investigated; stability constants and molar extinction coefficients have been calculated. The values of the latter decrease in the order CH_3COOH > CH_2ClCOOH > CCl_3COOH. The formation and extraction of mixed-ligand complexes in Sc-PAR-HX systems make it possible to increase the sensitivity and selectivity of scandium determination in comparison with the use of the Sc-PAR mono-ligand complex.

UK PubMed Central (United Kingdom)

Little is known about how sociodemographic factors relate to children’s chronic pain. This paper describes the pain, health, and sociodemographic characteristics of a cohort of children...Full Text Available

UK PubMed Central (United Kingdom)

The objectives of this study were to examine the association between dietary factors and underweight and overweight adult Vietnamese living in the rural areas of Vietnam. A cross-sectional study of...Full Text Available

International Nuclear Information System (INIS)

The present study was designed to assess the radioprotective effects of amifostine on ovarian follicles. Three week-old female mice with or without pretreatment of amifostine were irradiated with 6.42 Gy of #gamma# -ray. Ovaries were collected 0 and 6h after irradiation. DNA fragmentation pattern and expression of genes and activity of proteins related with apoptosis were investigated by means of RT-PCR and Western blot. Proliferation of granulosa cells was reduced and incidence rate of follicular atresia was increased in ovarian follicles in #gamma# -ray irradiated mice compared to those in control or amifostine-treated group. DNA fragmentation was increased in time-dependent manner in granulosa cells of all irradiated groups. However, no difference between amifostine pre-treated group and irradiated groups was found and the expression of p53 as tumor suppressor gene and Bax as one of pro-apoptotic Bcl-2 family was increased in irradiated mice ovaries. PARP as DNA damage sensor was ...

Energy Technology Data Exchange (ETDEWEB)

'The objective of this project is to provide a means to optimize ligand architecture for f-block metal recognition. The authors strategy builds on an innovative and successful molecular modeling approach in developing polyether ligand design criteria for the alkali and alkaline earth cations. The hypothesis underlying this proposal is that differences in metal ion binding with multidentate ligands bearing the same number and type of donor groups are primarily attributable to intramolecular steric factors. They propose quantifying these steric factors through the application of molecular mechanics models. The research involves close integration of theoretical and experimental chemistry. The experimental work entails synthesizing novel ligands and experimentally determining structures and binding constants for metal ion complexation by series of ligands in which architecture ...

International Nuclear Information System (INIS)

In order to increase the sensitivity of photometric determination of tungsten and to find forms with high molar extinction coefficients, mixed-ligand complexes of tungsten with antipyrine and trihydroxyfluorone have been studied. The molar extinction coefficients have been determined for chloride associates of mixed-ligand complexes containing different trioxyfluorones: phenylfluorone, salicylflourone, p-bromphenylfluorone, anthrafluorone, dioxyfluorescein, and dioxyfluoroscein ethylate (DOFE). An associate formed by DOFE has the maximum molar extinction coefficient. It has been used for photometric determination of microgram amounts of tungsten impurity in vanadyl sulphate.

International Nuclear Information System (INIS)

Reaction of At(I) with triphenylphosphine, triethylphosphite and tri-n-octylphosphine oxide was investigated in ethanolic solution by means of electromigration. A cationic complex with triphenylphosphine was identified being stable at pH = 1,9 in the concentration range of the ligand between c = 10"-"5 to 10"-"3 M. At a higher ligand concentration and at pH>2, the reduction effect of phosphine is superimposed on the complex formation. Complex formation is confirmed by ligand exchange reactions with Br"- and I"-. A comparatively weak complex is formed by triethylphosphite and At(I). No compound is formed by tri-n-octylphosphine oxide and At(I). (orig.).

International Nuclear Information System (INIS)

Bisaminoethanethiol (BAT) ligands with various gem-dimethyl and amide groups were prepared, and the corresponding neutral Tc-99m complexes were prepared and evaluated for their relative stabilities by ligand-exchange reactions. It was demonstrated that technetium complexes containing gem-dimethyl substituents have higher lipophilicities, whereas those with an amide group possess greater stability, which enhances ligand-exchange reaction. The most interesting observation was that the brain uptake in rats is not determined only by lipophilicity. Apparently, Tc-99m complexes with an amide functional group display lower brain uptakes in rats compared to those without an amide group. The brain uptake was strongly influenced by substituents on the BAT ligand. These factors are critically important and should be taken into consideration when designing Tc-99m-labeled agents for CNS receptor imaging.

UK PubMed Central (United Kingdom)

Orphan G protein-coupled receptors (GPCRs) are receptors lacking endogenous ligands. Found by molecular biological analyses, they became the roots of reverse pharmacology, in which receptors are attempted...Full Text Available

International Nuclear Information System (INIS)

Published in summary form only.

UK PubMed Central (United Kingdom)

Many microbial pathogens recognize oligosaccharides displayed on the surface of host cells as receptors for toxins and adhesins. These ligand-receptor interactions are critical for disease pathogenesis,...Full Text Available

International Nuclear Information System (INIS)

Consideration is given to results of investigation into thorium complexing with morin (H_2Mor) in extraction systems containing different carboxylic acids as well as different salt background. The obtained data enabled to suggest the method of photometric determination of thorium in the form of Th(HMor)_2Benz_2 different-ligand complex (where Benz-anion of benzilic acid) with 0.25 #mu#g/ml detection limit.

International Nuclear Information System (INIS)

Using the PMR method the interaction of zirconium and hafnium tetrachlorides with tri.tet.butylphenyl ester of 1,2- naphthoquinonediazide (2)-5-sulfonic acid is studied. The formation of MCl_4xNQD complexes is established, the equilibrium constants and thermodynamic parameters of complexing reaction are determined. The presence of rapid ligand exchange, proceeding according to associative mechanism, is detected. The rate constants and activation energies of the exchange reaction are calculated.

Energy Technology Data Exchange (ETDEWEB)

Occupational and environmental exposure to organic ligands, solvents, fuel hydrocarbons, and polychlorinated biphenyls are linked with increased risk of hematologic malignancies. DOE facilities and waste sites in the U.S. are contaminated with mixtures of potentially hazardous chemicals such as metals, organic ligands, solvents, fuel hydrocarbons, polychlorinated biphenyls and radioactive isotopes. A major goal of this project was to establish linkage between chemical/radiation exposure and induction of genomic damage in target populations with the capability to undergo transformation.

International Nuclear Information System (INIS)

One approach in the design of neutral oxotechnetium complexes is based on the simultaneous substitution of a tridentate dianionic ligand and a monodentate monoanionic coligand on a [Tc(V)O]"+"3 precursor. Following this ''mixed ligand'' concept, a novel "9"9"mTc complex with N,N-bis(2-mercaptoethyl)-N'N'-diethylethylenediamine as ligand and 1-octanethiol as coligand is prepared and evaluated as potential brain radiopharmaceutical. Preparation of the complex at tracer level was accomplished by using "9"9"mTc-glucoheptonate as precursor. The substitution was optimized and a coligand/ligand ratio of 5 was selected. Under this conditions the labeling yield was over 80% and a major product (with radiochemical purity > 80%) was isolated by HPLC methods and used for biological evaluation. Chemical characterization at carrier level was developed using the corresponding rhenium complex as structural model. ...

Energy Technology Data Exchange (ETDEWEB)

Asialoorosomucoid (ASOR) is internalized and degraded by HepG2 cells after binding to the asialoglycoprotein (ASGP) receptor, internalization through the coated pit/coated vesicle pathway, and trafficking to lysosomes. Primaquine, an 8-aminoquinoline antimalarial compound, inhibits ASOR degradation at concentrations greater than 0.2 mM by neutralizing intracellular acid compartments. This leads to alterations in surface receptor number, receptor-ligand dissociation, and receptor recycling. We have investigated the effects of primaquine on 125I-ASOR uptake and degradation as a function of primaquine concentration and duration of exposure. Concentrations below those required for neutralization of acidic compartments block 125I-ASOR degradation in HepG2 cells and lead to intracellular ligand accumulation. This effect is maximal at 80 microM primaquine. The intracellular 125I-ASOR is undegraded, dissociated from the ASGP receptor, and contained ...

UK PubMed Central (United Kingdom)

BackgroundSouth Africa has a high tuberculosis (TB)-human immunodeficiency virus (HIV) coinfection rate of 73%, yet only 46% of TB patients are tested for HIV. To date, relatively...Full Text Available

International Nuclear Information System (INIS)

Eu"3"+ and Tb"3"+ complexes with novel branched calix[4]arene ligands incorporating 2,2' -bipyridine subunits functionalized in the 6- or 5,5'-positions have been synthesized and their photophysical properties investigated. High luminescence intensity was obtained for the Eu"3"+ complex of the calix[4]arene ligand carrying four 5,5' -substituted- 2,2' -bipyridines, which has high molar extinction coefficients (#epsilon#_m_a_x 39 600 M"-"1 cm"-"1) and a high luminescence quantum yield (15%). (authors). 12 refs., 2 figs., 1 tab.

UK PubMed Central (United Kingdom)

Subcellular-fractionation techniques were used to characterize the endocytic pathway followed by ricin in rat liver in vivo and tentatively identify the site(s) at which the ricin interchain disulphide...Full Text Available

UK PubMed Central (United Kingdom)

BackgroundThe aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that mediates the toxicity and biological activity of dioxins and related chemicals. The...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

The synthesis, characterization, and emission properties of a series of Pt(L{sub 2})(S-S) complexes are reported. The (L{sub 2}) ligands include 4,7-diphenyl-1,10-phenanthroline (Ph{sub 2}phen), 4,4{prime}-dimethyl-2,2{prime}-bipyridine (Me{sub 2}bpy), 1,5-cyclo-octadiene (COD), trimethyl phosphite (P(OMe){sub 3}), and the {alpha}-C-deprotonated form of 2-phenylpyridine (2-phpy). The (S-S) ligands include 1-(tert-butoxycarbonyl)-1-cyanoethylene-2,2-dithiolate (tbcda), 1-(diethoxyphosphinyl)-1-cyanoethylene-2,2-dithiolate (cpdt), cis-1,2-dicarbomethoxyethylene-1,2-dithiolate (met), and N,N-diethyldithio-carbamate (Et{sub 2}dtc). The complexes are readily synthesized by the addition of the dithiolate or thiolate ligand to Pt(L{sub 2})Cl{sub 2} except for Pt(P(OMe){sub 3}){sub 2}(met), which is prepared by the addition of 2 equiv of trimethyl phosphite to Pt(COD)(met).

British Library Electronic Table of Contents (United Kingdom)

Potassium dichlorido(l-prolinato)platinate(II), K[PtCl"2(l-pro"?"H)] (1), and chlorido(dimethyl sulfoxide)(l-prolinato)platinum(II), [PtCl(l-pro"?"H)(dmso)] (2), were synthesized by ligand substitution reactions. Both complexes were characterized by ^1H, ^1^3C, and ^1^9^5Pt NMR spectroscopy, elemental analysis, and HR-ESI-MS. The molecular structures of 1 and 2 were determined by single crystal X-ray diffraction, proving bidentate coordinated l-prolinato ligand and SP-4-4 configuration of 2a. With the help of DFT calculations stability of possible isomers of 1 and 2 was studied. A considerable difference in the in vitro cytotoxicity of 1 versus 2a (exchange of one chlorido ligand by dmso) against four human cancer cell lines was found.

UK PubMed Central (United Kingdom)

The effects of selected ligands on the structure of the truncated heavy-chain chemomechanical motor domains of Drosophila ncd and human kinesin were compared using the technique of transient electric...Full Text Available

UK PubMed Central (United Kingdom)

Receptor activator of NF-kB ligand (RANKL) and osteoprotegerin (OPG) play key roles in the pathogenesis of glucocorticoid-induced osteoporosis (GIO). The aim of our study was to determine whether the...Full Text Available

UK PubMed Central (United Kingdom)

Genetic algorithms (GA) were used to develop specific copper metal-ligand force field parameters for the MM3 force field, from a combination of crystallographic structures and ab initio...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

No abstract prepared.

International Nuclear Information System (INIS)

The aim of this study was to assess the utility of a radioimmunoconjugate containing a lead radionuclide for therapy and scintigraphy applications. The radioimmunoconjugate evaluated consisted of a bifunctional DOTA ligand and monoclonal antibody (MAb) B72.3 using athymic mice bearing LS-174T tumors, human colon carcinoma xenografts. In the studies reported here, the lead-203-DOTA complex itself was first demonstrated to have in vivo stability. MAb B72.3 was then conjugated with the DOTA ligand and labeled with "2"0"3Pb, and the immunoreactivity of B72.3 was maintained. The localization of the radioimmunoconjugate to tumor tissue and other select organs paralleled that of DOTA-"1"2"5I-B72.3, suggesting a similar metabolic pattern of the two radioimmunoconjugates. Thus, the DOTA-metal complex does not alter the behavior of the radioimmunoconjugate. Tumor localization of the "2"0"3Pb-DOTA-B72.3 conjugate was demonstrated with biodistribution ...

UK PubMed Central (United Kingdom)

The programming of cellular networks to achieve new biological functions depends on the development of genetic tools that link the presence of a molecular signal to gene-regulatory activity. Recently,...Full Text Available

UK PubMed Central (United Kingdom)

BackgroundOne virulence property of Borrelia burgdorferi is its resistance to innate immunity, in particular to complement-mediated killing. Serum-resistant B....Full Text Available

Science.gov (United States)

Chiral auxiliaries are promising emerging tools for the asymmetric synthesis of octahedral metal complexes. We recently introduced chiral salicyloxazolines as coordinating bidentate chiral ligands which provide excellent control over the metal-centered configuration in the course of ligand substitution reactions and can be removed afterward in an acid-induced fashion under complete retention of configuration (J. Am. Chem. Soc. 2009, 131, 9602-9603). Here reported is our detailed investigation of this sequence of reactions, affording virtually enantiopure ruthenium polypyridyl complexes. The control of the metal-centered chirality by the coordinated chiral salicyloxazolinate ligand was evaluated as a function of reaction conditions, the employed bidentate 2,2'-bipyridine and 1,10-phenanthroline ligands, and the substituent at the asymmetric 5-position of the oxazoline heterocycle. Most striking was the ...

UK PubMed Central (United Kingdom)

Cd36 is a small-molecular-weight integral membrane protein expressed in a diverse, but select, range of cell types. It has an equally diverse range of ligands and physiological functions, which has...Full Text Available

UK PubMed Central (United Kingdom)

Bacterial pathogens use virulence strategies to invade epithelial barriers, but active processes of epithelial cells may also contribute to the endocytosis of microbial particles. To focus on the latter,...Full Text Available

UK PubMed Central (United Kingdom)

We investigated the ability of N-benzyl-N-ethyl-2-(7,8-dihydro-7-methyl-8-oxo-2-phenyl-9H-purin-9-yl)acetamide...Full Text Available

UK PubMed Central (United Kingdom)

Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors belonging to the nuclear hormone receptor superfamily. Their discovery in the 1990s provided insights...Full Text Available

International Nuclear Information System (INIS)

Six kinds of diamino-dithiol compounds are labelled with "9"9Tc"m by ligands exchange reaction. Their ligands exchange percentage is over 95%. The biodistribution of one of these compounds in mice shows 0.88% brain uptake after two minutes and 0.28% after 15 minutes respectively. Although the brain uptake is lower for this compound, it has longer retention in brain. So, the experiment results are valuable to the design of new brain imaging agent in the future.

International Nuclear Information System (INIS)

Of the radionuclides with physical properties most suited for use with monoclonal antibody for tumor imaging or therapy, few are more available or desirable than Pb-203, 212 and Bi-212. Yet no clinical studies have as yet been possible solely due to the lability in vivo of known complexes. We now report that bismuth complexes of the ligands p-SCN-Bz-DOTA and p-SCN-Bz-trans-cyclohexylDTPA are effective at protecting Bi-206 from release when linked to immunoproteins. Practicable, efficient ligand syntheses will be reported. Initial studies reveal that antibody is labeled efficiently with radiolead DOTA complexes. Preliminary studies indicate stability in vivo.

British Library Electronic Table of Contents (United Kingdom)

Metalloid cluster compounds of group 14 of the general formulae EnRm with n > m (E = Si, Ge, Sn, Pb; R = ligand), where naked as well as ligand bound tetrel atoms are present, represent a novel class of cluster compounds in group 14 chemistry and can be seen as intermediates on the way to the elemental state. Therefore, interesting properties are expected for these compounds, which might complement results from nanotechnology. In this article, first results for germanium are discussed, together with novel build-up reactions on the way to novel materials based on metalloid cluster compounds. GRAPHICAL ABSTRACT[image omitted

International Nuclear Information System (INIS)

The mechanistic aspects of electrochemical reductions of U"V"IO_2(acac)_2dmso(acac=acetylacetonate, dmso=dimethyl sulfoxide) complex with bidentate ligand(acac) in DMSO were investigated by using cyclic voltammetry, normal pulse voltammetry, and spectrophotometer equipped with an optical transparent thin layer electrode cell. It is concluded that the uranyl complexes with bidentate ligands at the equatorial plane form stable U(V) complexes by the electrochemical reduction and that their molar extinction coefficients in the visible region are very small. (J.P.N.).

International Nuclear Information System (INIS)

A study was made on complex formation of thiosemicarbazide diacetic acid (H_2L) with neodymium (3), holmium (3) and erbium (3) in solutions and formation of complexes of metal: ligand=4:1 composition was revealed. Synthesis conditions were developed and products of LnLClxnH_2O, LnLOHxnH_2O, Na[LnL_2]xnH_2O composition were separated in crystalline state. It was shown, that H_2L behaves in these compounds as tripod ligand with O, O, N, N donor atoms.

Energy Technology Data Exchange (ETDEWEB)

A new series of heteroleptic cyclometalated platinum(II) complexes Pt-1a-f was synthesized, employing 2-arylpyridine (or 1-arylisoquinoline) (HC{sup L}AMDAN-1) and 1,3-bis(3,4-dibutoxyphenyl)propane-1,3-dione (HO{sup L}AMDAO-1) for cyclometalation and as ancillary ligands, respectively, and photoluminescent properties were investigated. Focusing on red-shifted phosphorescence, C{sup L}AMDAN ligands containing pi-extended aromatics and electron-rich heterocycles were examined. All obtained complexes exhibited photoluminescence at ambient temperature, and the emission maxima ranged from green (lambda{sub PL}=518 nm) to far red (lambda{sub PL}=708 nm). The large Stokes shifts of more than 100 nm and sub-microsecond or microsecond emission lifetimes revealed that these complexes are phosphorescent emissive. The quantum yield of Pt-1 ranged from 0.02 to 0.59 at ambient temperature and decreased as the emission maximum was red-shifted. In comparison ...

Science.gov (United States)

This instructional unit is one of 10 developed by students on various energy-related areas that deals specifically with fireplaces and fuels. Its objective is for the student to be able to discuss the structural design, operation, and efficiency of fireplaces and characteristics of different fireplace fuels. Some topics covered are fuels, elements of the fire triangle, factors relating to high efficiency of masonry fireplaces, uses of grates and chimney, heat recovery, and prefabricated and free standing fireplaces. Materials in each unit may include some or all of the following: terminal and specific objectives, list of references, information sheet with terms and definitions, informative materials, transparency masters, assignment sheet(s), and unit test with answers. (YLB)

International Nuclear Information System (INIS)

The p75 neurotrophin receptor (p75"N"T"R) is a death receptor which belongs to the tumor necrosis factor receptor super-family of membrane proteins. This study shows that p75"N"T"R retarded cell cycle progression by induced accumulation of cells in G0/G1 and a reduction in the S phase of the cell cycle. The rescue of tumor cells from cell cycle progression by a death domain deleted (#DELTA#DD) dominant-negative antagonist of p75"N"T"R showed that the death domain transduced anti-proliferative activity in a ligand-independent manner. Conversely, addition of NGF ligand rescued retardation of cell cycle progression with commensurate changes in components of the cyclin/cdk holoenzyme complex. In the absence of ligand, p75"N"T"R-dependent cell cycle arrest facilitated an increase in apoptotic nuclear fragmentation of the prostate cancer cells. Apoptosis of p75"N"T"R expressing cells occurred via the intrinsic mitochondrial ...

Energy Technology Data Exchange (ETDEWEB)

During the past year, further studies on mAChR were conducted. These studies included verification of the difference in pituitary distribution based on ligand charge. The pituitary localization of TRB. A neutral mAChR ligand, was verified. The lack of QNB blockade of TRB uptake was tested by blockage with scopolamine, another mAChR antagonist and by testing the effect in a different strain of rat. Neither scopolamine or change of rat strain had any effect. We concluded that TRB uptake in pituitary is not a receptor-mediated process. Further studies were conducted with an additional quaternized mAChR ligand: MQNB. Pituitary localization of MQNB, like MTRB, could be blocked by pretreatment with QNB. We have tentatively concluded that permanent charge on a mAChR antagonist changes the mechanism of uptake in the pituitary. Time course studies and the effects of DES on myocardial uptake are reported. A brief report on ...

Science.gov (United States)

The thermostable Thermus aquaticus DNA polymerase (Taq Pol) has been the key factor in transforming the initial PCR method into one with huge impact in molecular biology and biotechnology. Therefore, the development of effective affinity adsorbents for the purification of Taq Pol, as well as other DNA polymerases, attracts the attention of the enzyme manufacturers and the research laboratories. In this report we describe a simple protocol for the purification of Taq Pol from E. coli lysates, leading to enzymes of high specific activity and purity. The protocol is based on a single affinity chromatography step, featuring an immobilized ligand selected from a structure-biased combinatorial library of dNTP-mimetic synthetic ligands. The ligand library was screened for its ability to bind and purify Taq Pol from E. coli lysates. One immobilized ligand (mABSGu) of the general formula X-Trz-Y, bearing ...

International Nuclear Information System (INIS)

New five complexes of the type of [RuL sub(3-x)(dmby) sub(x)]X sub(2)(x = 1,2,3, L = 2,2'-bipyridyl or 1,10-phenanthroline, dmby = 3,3'-dimethy1-2,2'-bipyridyl, X = halide ion) have been synthesized in order to investigate the effects of two methyl groups of dmby on the absorption and emission spectra, luminescence quantum yields, and lifetimes. Values of the radiative and nonradiative rate constants have been calculated from these data at 77K. Although the absorption and emission maxima and the lifetimes are not much affected by the dmby ligand substitution, the molar extinction coefficients and emission quantum yields are decreased compared with trischelated complexes of the parent bipyridyl or phenanthroline ligands. At 25"0C the emission yields of the complexes containing dmby decrease by 3 - 4 orders of magnitude than at 77K. Possible causes of the decrease in the quantum yields are discussed. (author).

British Library Electronic Table of Contents (United Kingdom)

Platinum(II) complexes (1-4) with bidentate N,Nprime-ligands, O,Oprime-dialkyl esters (alkyl = ethyl, n-propyl, n-butyl and n-pentyl), of (S,S)-ethylenediamine-N,Nprime-di-2-(4-methyl)pentanoic acid were synthesized and characterized by IR, 1H NMR and 13C NMR spectroscopy and elemental analysis. DFT calculations were performed for the complexes and it was found that only one diastereoisomer could be formed. Cytotoxic activity of complexes 1-4 was determined against chronic lymphocytic leukemia cells (CLL) and compared to the activity of ligand precursors L12HCl-L42HCl and corresponding palladium(II) complexes, [PdCl2L] (L = L1-L4). The complexes were found to exhibit significantly higher antitumor activities than cisplatin on CLL cells. Cytotoxic effect of platinum(II) complexes on CLL cel...

International Nuclear Information System (INIS)

The thiazolidinedione (TZD) or glitazone class of peroxisome proliferator-activated-#gamma# (PPAR-#gamma#) ligands not only induce adipocyte differentiation and increase insulin sensitivity, but also exert growth inhibitory effects on several carcinoma cell lines in vitro as well as in vivo. In the current study the in vitro effect of four PPAR-#gamma# agonists (ciglitazone, pioglitazone, troglitazone, rosiglitazone) on the cell growth of seven human neuroblastoma cell lines (Kelly, LAN-1, LAN-5, LS, IMR-32, SK-N-SH, SH-SY5Y) was investigated. Growth rates were assessed by a colorimetric XTT-based assay kit. Expression of PPAR-#gamma# protein was examined by immunohistochemistry and Western blot analysis. All glitazones inhibited in vitro growth and viability of the human neuroblastoma cell lines in a dose-dependent manner showing considerable effects only at high concentrations (10 #mu#M and 100 #mu#M). Effectiveness of the glitazones on neuroblastoma cell growth ...

International Nuclear Information System (INIS)

The exchange charge model of crystal field theory has been used to analyze systematically the ground state absorption spectra of octahedrally coordinated Ni"2"+ ion in isostructural nickel halide crystals NiCl_2, NiBr_2, and NiI_2. The parameters of the crystal field acting on the Ni"2"+ ion are calculated from the available crystal structure data. The obtained energy level schemes are compared with experimental absorption spectra; a good agreement with experimental data is demonstrated. Dependencies of the crystal field invariants and covalence effects on the type of ligands are considered. It is shown numerically that the overlap effects between Ni"2"+ ion and ligands increase with an increase of the ligands' atomic number resulting in the following order of the degree of covalence: NiI_2>NiBr_2>NiCl_2.

International Nuclear Information System (INIS)

The future use of single-molecule magnets in applications will require the ability to control and manipulate the spin state and magnetization of the magnets by external means. There are different approaches to this control, one being the modification of the magnets by adsorption of small ligand molecules. In this paper we use iron phthalocyanine supported by an Au(111) surface as a model compound and demonstrate, using x-ray photoelectron spectroscopy and density functional theory, that the spin state of the molecule can be tuned to different values (S #approx# 0, 1/2, 1) by adsorption of ammonia, pyridine, carbon monoxide or nitric oxide on the iron ion. The interaction also leads to electronic decoupling of the iron phthalocyanine from the Au(111) support. (fast track communication)

International Nuclear Information System (INIS)

The extraction-spectrophotometric method has been used to study lanthanoid ion complexing (Pr, Nd, Ho and Er) with antipyrine (Ant) and salicylic acid (Sal). The component relationship in different-ligand compounds Ln:Aut:Sal=2:3:6 and solvate number equal to 5 are determined; molar extinction coefficients of binary and different-ligand compounds are calculated. Oscillator strengths of absorption bands corresponding to supersensitive transitions of neodymium, holmium, erbium and some most intensive praseodymium bands are calculated. The study of IR spectra of investigated compounds allows to conclude on formation of coordination bonds of the central atom with the antipyrine molecule through the oxygen of the carbonyl group as well as on carboxyl group hydrogen substitution for metal and formation of coordination bond with OH group in salicylic acid molecules.

Energy Technology Data Exchange (ETDEWEB)

This paper describes the search for new potential chemotherapeutic agents based on transition metal complexes with planar ligands. In this study, palladium polypyridyl complexes were synthesized and characterized by elemental analysis, NMR, UV-VIS and IR spectroscopies. The interaction of the complexes with DNA was also investigated by spectroscopic methods. All metal-to-ligand charge transfer (MLCT) bands of the palladium polypyridyl complexes exhibited hypochromism and red shift in the presence of DNA. The binding constant and viscosity data suggested that the complexes [PdCl{sub 2}(phen)] and [PdCl{sub 2}(phendiamine)] interact with DNA by electrostatic forces. Additionally, these complexes induced an important leishmanistatic effect on L. (L.) mexicana promastigotes at the final concentration of 10 {mu}mol L{sup -1} in 48 h. (author)

International Nuclear Information System (INIS)

Pulse radiolysis was used to examine the nature of the silver species obtained when an aqueous solution containing sequestered Ag"+ ions was reduced by hydrated electrons in the presence of a surfactant macrocyclic crown ether, labeled L, and/or a maltoside surfactant. The initially formed product is the Ag"0(L) species which rapidly loses its ligand (half-life #<=#5 #mu#s) and reacts with another Ag"+(L) ion to form Ag_2"+(L). The latter species decays by a bimolecular process to form the Ag_4"2"+(L)_n species at a faster rate than its ligand free analogue. Ultimately, colloidal metallic silver, (Ag)_n, forms which is stabilized by the surfactant moieties. No long-term stability to the reduced monomolecular species could be obtained.

Energy Technology Data Exchange (ETDEWEB)

A detailed comparison of the softness of gold and silver has been reported in the light of hard soft acid base (HSAB) principle. Gold and silver nanoparticles in organic media (i.e., organosol) have been exploited individually to establish the principle. Sulfur and nitrogen were employed as soft and borderline donating atoms to examine the metal-ligand interactions. In this regard, thiols and amines have been considered as interacting ligands with sulfur and nitrogen donor atoms respectively. The stronger affinity of gold towards softer sulfur donor as compared to nitrogen and conversely a reasonable interaction of silver nanoparticles with both the atoms authenticate the softer nature of gold nanoparticle as compared to silver one.

British Library Electronic Table of Contents (United Kingdom)

A new bimetallic complex [HNEt3][Cuq2IEu(hfac)3] (q^- = 8-hydroxyquinolinato, hfac^- = hexafluoroacetylacetonate) was prepared simply with only one step and characterized. Upon excitation of the organic ligand q^-, the sensitized europium luminescence was achieved.

British Library Electronic Table of Contents (United Kingdom)

Varying coordination modes of the Schiff base ligand H"2L [5-methyl-1-H-pyrazole-3-carboxylic acid (1-pyridin-2-yl-ethylidene)-hydrazide] towards different metal centers are reported with the syntheses and characterization of four mononuclear Mn(II), Co(II), Cd(II) and Zn(II) complexes, [Mn(H"2L)(H"2O)"2](ClO"4)"2(MeOH) (1), [Co(H"2L)(NCS)"2] (2), [Cd(H"2L)(H"2O)"2](ClO"4)"2 (3) and [Zn(H"2L)(H"2O)"2](ClO"4)"2 (4), and a binuclear Cu(II) complex, [Cu"2(L)"2](ClO"4)"2 (5). In the complexes 1-4 the neutral ligand serves as a 3N,2O donor where the pyridine ring N, two azomethine N and two carbohydrazine oxygen atoms are coordinatively active, leaving the pyrazole-N atoms inactive. In the case of complex 5, each ligand molecule behaves as a 4N,O donor utilizing the pyridine N, one azomethine N...

Energy Technology Data Exchange (ETDEWEB)

No abstract prepared.

International Nuclear Information System (INIS)

The symmetrical complexes ["9"9"mTc][TcN(R_2PS_2)_2] [R = CH_3, CH_2CH_3, CH_2CH_2CH_3, CH_2(CH_3)_2], and the unsymmetrical complex ["9"9"mTc][TcN(Me_2PS_2)(Et_2PS_2)] have been prepared, at tracer level, through a two-step procedure involving the preliminary formation of a prereduced technetium nitrido intermediate followed by substitution reaction onto this species by the appropriate dithiophosphinate ligand [R_2PS_2]Na. The chemical identity of the resulting complexes have been established by comparison with the corresponding "9"9Tc-analogs prepared, at macroscopic level, by reacting the complex ["9"9TcNCl_4] [n-Bu_4N] (n-Bu = n-butyl) with an excess of ligand in methanol, and characterized by elemental analyses and spectroscopic techniques. The complexes are neutral and lipophilic, and possess a square pyramidal geometry, with an apical Tc N group and two dithiophosphinate ligands spanning the four positions on the ...

Energy Technology Data Exchange (ETDEWEB)

Stability constants for uranium-tetracycline complexes were determined by the method of average number of ligands, the method of limiting values, the method of two parameters and the method of weighted least squares. Solvent extraction technique was used to obtain experimental data. (author). 10 refs.; 5 figs.

International Nuclear Information System (INIS)

The synthesis, characterization of M"vO([CH_3CH_2N(CH_2CH_2S)_2](p-S-Ph-COOCH_2-CH_3)) (M:"9"9"mTc: I, Re: II) is presented in this work, where a pendant ester function is attached to the monothiolate ligand. Chemical structure of I is established after chromatographic comparison with II, synthesized in macroscopic amounts. Complex II is fully characterized by classical methods of analysis showing that the compound adopts a distorted trigonal bipyramidal configuration around the metal. The two sulfur atoms of the tridentate ligand and the oxo group form the basal plane, while the remaining nitrogen atom of the tridentate ligand and the sulfur atom of the monothiolate ligand occupy the apices of the bipyramid. In vitro challenge experiments with glutathione (GSH) in neutral aqueous medium demonstrate, that I suffers nucleophilic attack by GSH and thereby transformation to a more hydrophilic daughter ...

UK PubMed Central (United Kingdom)

The retinoic acid receptor-related orphan receptors α and γ (RORα (NR1F1) and RORγ (NR1F3)) are orphan nuclear receptors and perform critical roles in regulation of development,...Full Text Available

UK PubMed Central (United Kingdom)

Translocator protein (TSPO) is upregulated in activated microglia and thus can serve as a marker of neuroinflammation. Recently, a novel radioligand, ¹¹C-N,N-diethyl-2-[2-(4-methoxyphenyl)-5,7-dimethyl-pyrazolo[1,5-a]pyrimidin-3-yl]-acetamide...Full Text Available

UK PubMed Central (United Kingdom)

The immunolocalization of the low density lipoprotein receptor-related protein 1 (LRP1) and its ligand alpha 2-Macroglobulin (α₂M) was examined in tissues from human donor...Full Text Available

UK PubMed Central (United Kingdom)

PlGF, one of the ligands for VEGFR-1, has been implicated in tumor angiogenesis. However, more recent studies indicate that genetic or pharmacological inhibition of PlGF signaling does not result in...Full Text Available

International Nuclear Information System (INIS)

An improved labeling procedure for peptides attached to organometallic 99mTc(III) '4+1' mixed-ligand complexes in which the radiometal is coordinated by a tripodal tetradentate chelator 2,2',2''-nitrilotriethanethiol (NS3) and a monodentate isocyanide ligand is presented. The labeling procedure was evaluated by the synthesis of [99mTc(NS3)(L2-RGD)]. The containing radiopharmaceutically interesting RGD-peptide cyclo[Arg-Gly-Asp-D-Tyr-Lys] was modified with 4-isocyanobutanoic acid (L2) as linker conjugated to N6-Lys to get the monodentate ligand L2-RGD. The structural identity of the 99mTc-conjugate was confirmed by comparison to a Re reference compound. The Tc- and Re-conjugates had matching retention times under identical HPLC conditions. The 99mTc-labeling was performed in a novel one-step procedure using the eluate of a 99Mo/99mTc generator, NS3, the isocyanide modified peptide, SnCl2, Na2EDTA, mannitol and ascorbic acid ...

International Nuclear Information System (INIS)

The purpose was to develop a simplified and reliable method of separating free from antibody-bound ligand using a precipitating antibody linked to a cellulose derivative. Dose-response curves and control sera were set up in parallel for various pituitary and placental polypeptides, steroid hormones, insulin, glucagon, triiodothyronine, thyroxine, angiotensin I, calcitonin, gastrin, cyclic AMP, and digoxin. After first-antibody reactions had reached equilibrium, free and bound ligand were separated using a double-antibody solid-phase system in parallel with conventional methods, including dextran-coated charcoal, double-antibody precipitation, single-antibody solid phase, organic solvents, salt precipitation, and anion-exchange resins. The effect of variations in temperature, incubation time, protein content, pH, and amount of separating material added were studied. The results showed that separation was complete within 1 hr for small ...

UK PubMed Central (United Kingdom)

The p90 ribosomal S6 kinases (RSKs) also known as MAPKAP-Ks are serine/threonine protein kinases that are activated by ERK or PDK1 and act as downstream effectors of mitogen-activated protein kinase...Full Text Available

UK PubMed Central (United Kingdom)

The DNA-binding properties of Ru(bpy)₂(eilatin)²⁺ have been investigated to determine if the sterically expansive eilatin ligand confers specificity for destabilized single-base...Full Text Available

Science.gov (United States)

Amphiphilic pincer palladium complexes bearing hydrophilic and hydrophobic side chains on the planar NCN palladium pincer backbone were designed and prepared via the ligand introduction route. The complexes self-assembled under aqueous conditions to form vesicles with bilayer membranes containing palladium species. The catalytic activity of the vesicles in the Miyaura-Michael reaction in water was investigated. PMID:21837316

British Library Electronic Table of Contents (United Kingdom)

Climate change and limited primary energy resources require indigenous renewable electricity generation options to change the current coal-dominated power source matrix in China. The wind power is such a solution for the above challenges, and it still has large space for improvement in China. In this paper several critical factors related to Chinese wind power were studied in details, including the wind resources, the wind turbine industry and the policies from the Chinese government. Based on the study, the perspective of wind power in China was discussed. With outstanding advantages, the offshore wind power has a bright future in China, so its main characteristics are discussed. Based on the discussions, suggestions were given to improve the development of Chinese wind power, and the gov...

British Library Electronic Table of Contents (United Kingdom)

A large body of evidence indicates clear relationships between number and space processing in healthy and brain-damaged adults, as well as in children. The present paper addressed this issue regarding atypical math development. Adults with a diagnosis of dyscalculia (DYS) during childhood were compared to adults with average or high abilities in mathematics across two bisection tasks. Participants were presented with Arabic number triplets and had to judge either the number magnitude or the spatial location of the middle number relative to the two outer numbers. For the numerical judgment, adults with DYS were slower than both groups of control peers. They were also more strongly affected by the factors related to number magnitude such as the range of the triplets or the distance between t...

British Library Electronic Table of Contents (United Kingdom)

Purpose - This article aims to examine approaches by academic libraries in demonstrating return on investment (RoI). Design/methodology/approach - As a participant in a recent international RoI study, the author reviews the various difficulties in developing a suitable methodology. Findings - Using grant income as the basis for demonstrating RoI, it was found that wide differences in results may be attributable to a number of factors related to the parent organisation, the availability of grant funding and the country of the study. Research limitations/implications - Further work is necessary to arrive at a suitable methodology for a diverse range of academic libraries. Practical implications - Library managers are alerted to issues and problems surrounding the development of return on inv...

Science.gov (United States)

Ternary copper(II) complexes [Cu(L1)B](ClO4) (1, 2) and [Cu(L2)B](ClO4) (3, 4), where HL1 and HL2 are tridentate NSO- and ONO-donor Schiff bases and B is a heterocyclic base, viz. dipyrido[3,2-d:2',3'-f]quinoxaline (dpq, 1 and 3) or dipyrido[3,2-a:2',3'-c]phenazine (dppz, 2 and 4), were prepared and their DNA binding and photoinduced DNA cleavage activity studied. Complex 1, structurally characterized by single-crystal X-ray crystallography, shows an axially elongated square-pyramidal (4 + 1) coordination geometry in which the monoanionic L1 binds at the equatorial plane. The NN-donor dpq ligand exhibits an axial-equatorial binding mode. The complexes display good binding propensity to calf thymus DNA, giving a relative order 2 (NSO-dppz) > 4 (ONO-dppz) > 1 (NSO-dpq) > 3 (ONO-dpq). They cleave supercoiled pUC19 DNA to its nicked circular form when treated with 3-mercaptopropionic acid (MPA) by formation of hydroxyl radicals as the cleavage active species ...

International Nuclear Information System (INIS)

The authors have been involved for the last few years in developing high affinity sigma-receptor-specific radiopharmaceuticals for use in nuclear medicine. They recently demonstrated that sigma-1 receptors are expressed in human melanoma cells and that sigma receptors could be used as external markers for non-invasive imaging. In order to determine the presence of sigma receptors in other human tumors they have screened numerous non-small cell lung carcinoma, melanoma and breast cancer cell lines. All of these cell lines expressed high sigma receptor densities using commercially available ["3H]-(+)-pentazocine or ["3H]DTG tritiated sigma ligands. Therefore, a sigma ligand with high affinity in both sigma-1 and sigma-2 subtype pharmacological assays could be potentially useful for imaging a variety of primary and metastatic sites of various origins. The authors describe recent efforts to develop high affinity sigma radiopharmaceuticals and ...

British Library Electronic Table of Contents (United Kingdom)

Reaction between [V^I^VO(acac)2] and the ONN donor Schiff base Hpydx-aepy (I) (Hpydx-aepy=Schiff base obtained by the condensation of pyridoxal and 2-aminoethylpyridine) resulted in the formation of a complex [V^I^VO(acac)(pydx-aepy)] (1). Addition of aqueous 30% H2O2 to 1 yields the poor stable oxidoperoxidovanadium(V) complex [V^VO(O2)(pydx-aepy)] (2). Its formation has also been demonstrated in solution by treating 1 with H2O2 in methanol. Reaction of vanadium exchanged zeolite-Y with I in methanol followed by aerial oxidation gave zeolite-Y encapsulated dioxidovanadium(V) complex, abbreviated as [V^VO2(pydx-aepy)]-Y (4). The crystal and molecular structure of 1 has been determined, confirming the ONN binding mode of the ligand. The encapsulated complex [V^VO2(pydx-aepy)]-Y (4) catalyse...

British Library Electronic Table of Contents (United Kingdom)

A general approach has been designed to synthesize some mononuclear and binuclear cyclometalated platinum(II) complexes, containing aromatic N-donor ligands with the presence of one Cl- trans to carbon. In this way, cyclometalated platinum(II) complex [Pt(C^N)Cl(dmso)], 1, C^N = N(1),C(2prime)-chelated, deprotonated 2-phenylpyridine and dmso = dimethylsulfoxide, was used as a precursor to react with imidazole derivatives (1-methylimidazole, 2a, imidazole, 2b,), monodentate pyridine derivatives (4-methylpyridine, 2c, pyridine, 2d,) and bidentate pyridine derivative (4,4prime-bipyridine, 3 and 4,). Synthesized complexes were fully characterized by using multinuclear NMR spectroscopy (1H, 13C{1H} and 195Pt), correlation NMR spectroscopy (1H-1H COSY, 13C{1H}-1H Heteronuclear Multiple Quantum C...

Energy Technology Data Exchange (ETDEWEB)

Ultraviolet (UV) photoirradiation of Ag(I) compounds in the presence of an aqueous Triton X-100 solution has been exploited for the first time to prepare reproducible yellow silver hydrosol. The evolution of nanosized silver particles has been examined critically under the influence of different anions/ligands. Hence, time dependent evolution of silver hydrosol from different silver compounds in micelle via photochemical reduction is observed. Anions/ligands of precursor salts have been found to show profound influence (due to electron scavenging property, solubility, stability etc.) on the evolution route and efficiency of photochemical reduction of Ag(I) to Ag(O) in micelle and thereby classification of silver compounds becomes possible. Kinetic results reveal that the formation of silver particles proceeds via autocatalytic growth mechanism. The observed variation in rate constant values for the evolution of nanoparticles from different ...

International Nuclear Information System (INIS)

New dioxouranium (VI) complexes of Schiff bases derived from orthaminophenol and salicylaldehyde, 5,6-benzosalicyladehyde, orthohydroxyacetophenone, orthohydroxybenzophenone, acetoacetanilide and benzoylacetanilide have been prepared and characterized by elemental analysis, conductance, molecular weight, infrared, electronic spectra and magnetic susceptibility measurements. The schiff bases behave as ONO donor tridentate dibasic ligands. Two types of complexes, viz. UO_2L.CH_3OH and UO_2L_2 (where LH_2 schiff base) have been synthesized. The comlexes are monomers, nonelectrolytes and diamagnetic. The #nu#(C=N), #nu#(C-O) (phenolic), #nu#(C-O)(CH_3OH) and the ligands. The #nu#sub(as)(O = U =0) occurs in the range 885-940 cm"-"1 and U-O bond length lies in the 1.72-1.74 A range. The 1:1 complexes are six-cordinated and 1:2 complexes are eight coordinated. (author).

Energy Technology Data Exchange (ETDEWEB)

Targeted studies completed include the evaluation of tritiated N-0437, evaluation of /sup 35/S-cysteamine, evaluation of /sup 18/F-FDG and initiation of synthetic efforts towards the synthesis of iodinated N-0437 and pergolide analogs. The direction of the project has been changed due to several factors which include the decided lack of favorable experimental results, the excellence of results using muscarinic receptor ligands in pituitary, brain and heart and the contention of the DOE review panel that the original grant proposal was based on flawed assumptions together with their perceived lack of importance to pituitary imaging. In the final year of this grant, three studies will be completed. The first study is the continuation of synthetic efforts to prepare iodinated N-0437 and pergolide analogs for possible use as brain imaging agents. The second study is directed towards completion of biochemical evaluation of various muscarinic receptor analogs for heart, ...

International Nuclear Information System (INIS)

Several dioxomolybdenum(VI) complexes of the schiff bases derived from salicylaldehyde, 2-hydroxy-1-naphthaldehyde, o-hydroxyacetophenone or pyridoxal and o-aminobenzylalcohol, o-aminophenol, o-hydroxybenzylamine, o-hydroxy(methylbenzyl)amine or 3-amino-2-naphthoic acid have been synthesized and characterized by elemental analysis, electrical conductance, molecular weight, IR and electronic spectral and magnetic susceptibility measurements. The schiff bases behave as dibasic, tridentate ligands and coordinate through ONO donor system forming complexes of the type MoO_2L.X (where LH_2=schiff base, X=H_2O or Ch_3OH). The compounds MoO_2L.Ch_3OH react with 2,2'-dipyridyl to form heterochelates of the type MoO_2L.dipyridyl. The complexes are non-electrolytes, monomers, diamagnetic and possess a cis-MoO_2 structure. The complexes exhibit a ligand-to-metal charge-transfer transition around 25000 cm"-"1. The complexes MoO_2L.X and MoO_2L.dipyridyl are ...

Science.gov (United States)

The visible absorption spectra of 1,4-(dihydroxy)-9,10-anthraquinone and of Co(II), Ni(II), Cu(II) and Zn(II) chelates have been studied in different organic solvents. This system provides a model for the anthracycline antibiotics and their metal chelates. The band structure of the spectrum has been determined using the second and fourth derivatives of the spectrum. The visible absorption band of the parent molecule can be assigned to a single electronic state with a reduced dipole moment in the excited state; structure in this band is ascribed to two overlapping vibrational progressions. In contrast, the dianion (hydroxy protons removed) shows a single electronic state with an increased dipole moment in the excited state; structure in this band can be assigned to a single vibrational progression. All of the metal chelates show spectra which are similar in appearance to that of the dianion although the identity of the metal determines the bathochromic shift of the absorption band. ...

International Nuclear Information System (INIS)

Human complement protein C9 is shown to be a metalloprotein that binds 1 mol of Ca"2"+/mol of C9 with a dissociation constant of 3 #mu#m as measured by equilibrium dialysis. Incubation with EDTA removes the bound calcium, resulting in a apoprotein with decreased thermal stability. This loss in stability leads to aggregation and, therefore, to loss of hemolytic activity upon heating to a few degrees above the physiological temperature. Heat-induced aggregation of apoC9 can be prevented by salts that stabilize proteins according to the Hofmeister series of lyotropic ions, suggesting that the ion in native C9 may ligand with more than one structural element of domain of the protein. Ligand blotting indicates that the calcium binding site is located in the amino-terminal half of the protein. Removal of calcium by inclusion of EDTA in assay mixtures has no effect on the hemolytic activity of C9, and its capacity to bind to C8 in solution, or to ...

British Library Electronic Table of Contents (United Kingdom)

In the MnIII complex of the title compound, [MnIII(C18H12N4O2)(H2O)2]ClO4, the MnIII atom is coordinated by four N atoms from the bpb2- [1,2-bis(pyridine-2-carboxamido)benzene] ligand located in the equatorial plane and two O atoms of water molecules at axial positions, yielding a distorted MnN4O2 octahedral coordination geometry. The bpb2- ligand is nearly planar, with a maximum deviation of 0.2311 (3) A from the mean plane. The MnIII complex cation and the perchlorate anion, both of which are located on twofold rotation axes, are connected by O-H...O and C-H...O hydrogen bonds into a three-dimensional supramolecular network structure.

British Library Electronic Table of Contents (United Kingdom)

The 1H NMR, electronic absorption, and luminescence spectra, as well as voltammograms of the reduction and oxidation of the complexes [Pd(C?N)(N?N)]ClO4 and [Pd(C?N)(?-OOCCH3)]2 [where (C?N)? is deprotonated 2-phenyl-4,5-dihydro-1,3-oxazole, and N?N is ethylenediamine or 2,2?-bipyridine (bpy)] were compared. Magnetic nonequivalence of protons in the dihydrooxazole ring and upfield shift of the corresponding signals were observed as a result of anisotropic effect of the ring current in palladated phenyl substituents in the [Pd(C?N)(?-OOCCH3)]2 complex having a C 2 symmetry. One-electron reduction wave of [Pd(C?N)bpy]+ was assigned to ligand-centered electron transfer to the ?* orbital of 2,2?-bipyridine, and two oxidation waves of [Pd(C?N)(?-OOCCH3)]2 were attributed to successive one-elect...

International Nuclear Information System (INIS)

Chelating tendencies of several biologically important compounds viz. glycocyamine (GCN: N-amidino-aminoethanoic acid) taurine (TRN: 2-aminoethanesulphonic acid) and pyridoxal [PDL: 3-hydroxy-5-(hydroxymethyl)-2-methyl-pyridine-4-carbaldehyde] have been examined by pH-metric titration technique in their binary complex formation with copper(II) and uranyl(VI) ions. The work has further been extended to investigating the ternary complex formation involving 2.2'-bipyridine. 1,10-phenanthroline or nitrilotriacetic acid as a primary and TRN and PDL as secondary ligands. All the experiments were carried out at 25"0C and at an ionic strength of 0.1M (NaCl0_4) in aqueous or 50% (v/v) aqueous-ethanol medium according to the suitability of the experimental conditions. Stabilities of ternary complexes as compared to those of the corresponding binary complexes of the secondary ligands have also been discussed. (author).

International Nuclear Information System (INIS)

"2"1"1At is one of the most promising radionuclides in #alpha#-radioimmunotherapy (#alpha#-RIT). Unfortunately, biomolecules labeled by direct electrophilic astatination are unstable due to the rapid loss of "2"1"1At under both in vitro and in vivo conditions. The present paper describes the results of our studies on attaching At"- to the rhodium(III) complex with thioether ligand: 1,5,9,13-etrathiacyclohexadecane-3,11-diol (16-S4-diol). Rh"3"+ was chosen as a moderately soft metal cation which should form very strong bonds with soft At"- anions, but first of all because of the kinetic inertness of low spin rhodium(III) d"6 complexes. The 16-S4-diol ligand was selected due to formation of stable complexes with Rh"3"+. The experiments related to optimization of the reaction conditions were performed with the "1"3"1I, basing on a chemical similarity of I"- to At"-. The experiments with "2"1"1At were then carried out under the conditions found ...

International Nuclear Information System (INIS)

A few metal complexes of isatin-isonicotinoylhydrazone with Ni(II), Cr(III), Co(II), Cu(II), Zn(II) and Cd(II) have been prepared and characterized on the basis of elemental analyses, infrared and electronic spectra as well as "1H NMR spectra, conductivity and magnetic measurements. In view of the results obtained, it has been found that two molecules of isatin-isonicotinoylhydrazone are chelated to the central metal ion as bis-uninegative ONO tridentate ligand forming non-electrolytic octahedral metal complexes. (author)

British Library Electronic Table of Contents (United Kingdom)

Three novel inosine-based dinuclear platinum complexes have been synthesized via a solid-phase strategy. In these compounds, the metal is linked both to the N-7 of the purine nucleus and to the terminal amine group of a hexylamine side chain installed on N-1. Cis- or trans- diamine as well as ethylenediamine ligands are coordinated to platinum along with a chloride. The synthesised complexes were tested against four different human tumor cell lines. One of these complexes proved to be more cytotoxic than cisplatin against the MCF7 cancer cell line in a short-term exposure assay.

International Nuclear Information System (INIS)

Several new complexes of isomeric schiff bases derived from salicylaldehyde and o-hydroxybenzylamine/o-aminobenzyl-alcohol with Pr(III), Nd(III), Sm(III), Gd(III), Tb(III), and Dy(III) have been synthesized and characterized by elemental analysis, molar conductance, IR, electronic spectra and magnetic susceptibility measurements. The schiff bases behave as monobasic tridentate ONO donor and dibasic tridentate ONO donor ligands and form complexes of the type Ln(LH)L. (author). 12 refs.

Energy Technology Data Exchange (ETDEWEB)

Radioisotopes of Pb(II) have been of some interest in radioimmunotherapy and radioimmunoimaging (RII). However, the absence of a kinetically stable bifunctional chelating agent for Pb(II) has hampered its use for these applications. {sup 203}Pb (T{sub 1/2}=52.02 h) has application potential in RII, with a {gamma}-emission that is ideal for single photon emission computerized tomography, whereas {sup 212}Pb (T{sub 1/2}=10 h) is a source of highly cytotoxic {alpha}-particles via its decay to its {sup 212}Bi (T{sub 1/2}=60 min) daughter. The synthesis of the novel bifunctional chelating agent 2-(4-isothiocyanotobenzyl)-1,4,7,10-tetraaza-1,4,7,10-tetra-(2-carbamoyl methyl)-cyclododecane (4-NCS-Bz-TCMC) is reported herein. The Pb[TCMC]{sup 2+} complex was less labile to metal ion release than Pb[DOTA]{sup 2-} at pH 3.5 and below in isotopic exchange experiments. In addition to increased stability to Pb{sup 2+} ion release at low pH, the bifunctional TCMC ligand was ...

Science.gov (United States)

Silanization of the silica gel surface in the synthesis of silica gel polyamine composites uses (chloropropyl)-trichlorosilane (CPTCS). It is possible to substitute a molar fraction of reagent CPTCS with methyltrichlorosilane (MTCS), creating a mixed silane surface layer. Two types of silica gels were modified with a series of MTCS:CPTCS molar ratios. Solid-state CP/MAS 29Si and 13C NMR spectroscopies were used to evaluate the surface silane composition. Surface silane coverage was markedly improved for the resulting gels. When polyamines were grafted to the resultant MTCS:CPTCS silane layers, it was shown that the decrease in the number of propyl attachments to the polyamine resulted in increased quantities of ''free amines''. Optimum MTCS:CPTCS ratios were determined for three polyamines grafted onto one silica gel. A substantial free amine increase was observed for poly(allylamine) (PAA). Metal uptake studies show increases in Cu(II) capacity ...

Energy Technology Data Exchange (ETDEWEB)

Amino acids other than those that serve as ligands have been found to influence the chemical properties of transferrin iron. The catalytic ability of pyrophosphate to mediate transferrin iron release to a terminal acceptor is largely quenched by modification non-liganded histine groups on the protein. The first order rate constants of iron release for several partially histidine modified protein samples were measured. A statistical method was employed to establish that one non-liganded histidine per metal binding domain was responsible for the reduction in rate constant. These results imply that the iron mediated chelator, pyrophosphate, binds directly to a histidine residue on the protein during the iron release process. EPR spectroscopic results are consistent with this interpretation. Kinetic and amino acid sequence studies of ovotransferrin and lactoferrin, in addition to human serum transferrin, have allowed the ...

International Nuclear Information System (INIS)

A series of crown ethers carrying a pyrene group with nitrogen-sulfur donor atoms, that differ in having three, four and five sulfur atoms in the macrocycle was designed and synthesized by the reaction of the corresponding macrocyclic compound and 1-bromomethylpyrene. The influence of metal cations such as Mn2+, Fe2+, Fe3+, Co2+, Ni2+, Cu2+, Zn2+, Cd2+, Hg2+, Pb2+ and Al3+ on the spectroscopic properties of the ligands was investigated in acetonitrile-dichloromethane (1:1) by means of absorption and emission spectrometry. Absorption spectra show isosbestic points in the spectrophotometric titration of Fe2+, Zn2+, Cu2+, Pb2+ and Hg2+. The results of spectrophotometric titration experiments disclosed the complexation compositions and complex stability constants of the novel ligands with Fe2+, Zn2+, Cu2+, Pb2+ and Hg2+ cations. The monoazatetrathia crown ether showed good sensitivity for Cu2+ with linearity in the range 5.0x10-7-2.5x10-6 M and ...

Energy Technology Data Exchange (ETDEWEB)

Novel ligands cis-2,6-bis[N,N-bis(carboxymethyl)aminomethyl]-1-piperidineacetic acid (PIP-DTPA), cis-[(1R,11S)-6,9,15-Tris-carboxymethyl-3,6,9,15-tetraazabicyclo[9.3.1] pentadec-3-yl]-acetic acid (PIP-DOTA), cis-{l_brace}2,7-bis-[bis-carboxymethyl-amino)-methyl]-azepan-1-yl{r_brace}-acetic acid (AZEP-DTPA), [2-(4,7-bis-carboxymethyl-[1,4,7]triazacyclononan-1-yl-ethyl] -2-carbonylmethyl-amino]-tetraacetic acid (NETA) and [{l_brace}4-carboxymethyl-7-[2-(carboxymethylamino)-ethyl]-perhydro-1,4,7-triazonin-1-yl{r_brace}-acetic acid (NPTA) are investigated as potential chelators of {sup 177}Lu, {sup 9}Y, {sup 212}Pb and {sup 213}Bi for radioimmunotherapy (RIT). The new ligands are radiolabeled with {sup 177}Lu, {sup 86/88/9}Y, {sup 203}Pb and {sup 205/6}Bi, and in vitro stability and in vivo stability of the radiolabeled complexes are assessed in human serum and athymic mice, respectively. In vitro studies indicate that all radiolabeled complexes ...

British Library Electronic Table of Contents (United Kingdom)

Many advances have been carried out on the estrogens, GnRH and endocannabinoid system that have impact in the reproductive field. Indeed, estrogens, the generally accepted female hormones, have performed an unsuspected role in male sexual functions thanks to studies on non-mammalian vertebrates. Similarly, these animal models have provided important contributions to the identification of several GnRH ligand and receptor variants and their possible involvement in sexual behavior and gonadal function regulation. Moreover, the use of non-mammalian animal models has contributed to a better comprehension about the endocannabinoid system action in several mammalian reproductive events. We wish to highlight here how non-mammalian vertebrate animal model research contributes to advancements with i...

British Library Electronic Table of Contents (United Kingdom)

A promising drug target currently under investigation to improve cognitive deficits in neuropsychiatric and neurological disorders is the neuronal nicotinic alpha7 acetylcholine receptor (a7nAChR). Improving cognitive impairments in diseases such as Alzheimer's (AD) and schizophrenia remains a large unmet medical need, and the a7nAChR has many properties that make it an attractive therapeutic target. The a7nAChR is a ligand gated ion channel that has particularly high permeability to Ca^2^+ and is expressed in key brain regions involved in cognitive processes (e.g., hippocampus). The a7nAChRs are localized both pre-synaptically, where they can regulate neurotransmitter release, and post-synaptically where they can activate intracellular signaling cascades and influence downstream processes...

International Nuclear Information System (INIS)

Two peptide ligands conjugated adenine, [9-N-(tritylmercapto acetyl diglycyl aminoethyl) adenine, Tr-MAG_2-Ade] and [9-N-(tritylmercapto acetyl triglycyl aminoethyl) adenine, Tr-MAG3-Ade], are synthesized and labeled with "9"9"mTc by directly labeling method. The stability of "9"9"mTc-MAG_2- adenine and "9"9"mTc-MAG_3-adenine in vitro is measured. The uptake radios of tumor to muscle at 3h post-injection are 5.70 and 4.92, respectively. The biodistribution and scintigraphic imaging studies show that the two complexes have high localization in tumor and high contrasted tumor images can be obtained, which suggest their potential utility as tumor imaging agents. But the high radioactivity of abdomen could prevent the tumor imaging in this area. (author)

British Library Electronic Table of Contents (United Kingdom)

Fgf receptor 2c (Fgfr2c) was expressed in mature adipocytes of mouse white adipose tissue (WAT). To examine the role of Fgfr2c in mature adipocytes, we generated adipocyte-specific Fgfr2 knockout (Fgfr2 CKO) mice. The hypertrophy impairment of adipocytes in the mesenteric WAT but not in the subcutaneous WAT and decreased plasma free fatty acid (FFA) levels were observed in Fgfr2 CKO mice. Although the expression of genes involved in adipocyte differentiation and lipid metabolism in the mesenteric WAT was essentially unchanged, the expression of uncoupling protein 2 potentially involved in energy dissipation was significantly increased. Among potential Fgf ligands for Fgfr2c, Fgf9 was preferentially expressed in the mesenteric WAT. The present findings indicate that Fgfr2c potentially activ...

British Library Electronic Table of Contents (United Kingdom)

An hydrazone derivative, 1,2-cyclohexanedione bis-benzoyl-hydrazone (1,2-CHBBH), has been used as a selective reagent for an advanced environmental application consisting of separating the different species of nickel in natural waters by solvent extraction. The effects of pH and reagent concentration on the extraction process were studied, as well as the influence of both organic (humic acids) and inorganic ligands (Cl-). Under natural conditions, organic and inorganic nickel species presented different extraction behaviors, and the variations in extraction yields could be correlated with the concentrations of organic complexes in the samples, allowing the separation of labile and non-labile nickel species in both fresh and marine waters.

British Library Electronic Table of Contents (United Kingdom)

Studies addressed to a deep understanding of the structure/property relationship on the near infrared (NIR)-emissive erbium-quinolinolate complexes, which are of interest for low-cost photonic systems, are reviewed. The role of the 8-quinolinolate ligand (Q), which studies also as sensitizer to overcome the weak absorptivity of lanthanide ion, is discussed. Synthetic and structural aspects are reported to revise the old assumption that these complexes are analogous in structure to AlQ3 and to point out the specificity of the lanthanide coordination chemistry. In fact depending on reaction conditions, species with high coordination numbers and differing for nuclearity and stoichiometry have been isolated and fully characterized. In some instances it has been shown that coordinated water mol...

Energy Technology Data Exchange (ETDEWEB)

Colloidal nanocrystals attract significant interest due to their potential applications in electronic, magnetic, and optical devices. Nanocrystal supercrystals (NCSCs) are particularly appealing for their well ordered structure and homogeneity. The interactions between organic ligands that passivate the inorganic nanocrystal cores critically influence their self-organization into supercrystals, By investigating the mechanical properties of supercrystals, we can directly characterize the particle-particle interactions in a well-defined geometry, and gain insight into both the self-assembly process and the potential applications of nanocrystal supercrystals. Here we report nanoindentation studies of well ordered lead-sulfide (Pbs) nanocrystal supercrystals. Their modulus and hardness were found to be similar to soft polymers at 1.7 GPa and 70 MPa respectively and the fractures toughness was 39 KPa/m1/2, revealing the extremely brittle nature of these materials.

Energy Technology Data Exchange (ETDEWEB)

One of the research challenges in oncology is to develop new biochemical methods for noninvasive tumor therapy evaluation to determine whether the chemotherapeutics is effective. Vascular endothelial growth factor (VEGF) was labeled with radioiodine and evaluated in vitro as well as in vivo, using A2058, a melanoma cell line overexpressing VEGFR-1 and -2. Saturation binding analysis with [{sup 125}I]-VEGF resulted in a K {sub d} of 0.1 nM. Internalization assays indicate the preserved ligand induced internalization and metabolization of the tracer. Biodistribution studies with [{sup 123}I]-VEGF in wild type and A2058 tumor-bearing athymic mice showed low background activity and a tumor to reference tissue ratio of maximum 6.12. These results suggest that [{sup 123}I]-VEGF is a potentially suitable tracer for tumor therapy evaluation.

Energy Technology Data Exchange (ETDEWEB)

The proposed active sites on the catalyst surface in heterogeneous propylene ammoxidation have been successfully modelled by structurally characterized pinacolato W(VI) tert-butylimido complexes. These compounds exist as an equilibrating mixture of amine-bis(imido) and imido-bis(amido) complexes, the position of this equilibrium is dependent on the electronic nature of the glycolate ligand. Both of the C-N bond-forming reactions proposed in recent studies by Grasselli et al. (1) have been reproduced using discrete Group VI d{sup 0} organoimido complexes under mild conditions suitable for detailed mechanistic studies. These reactions are: (1) oxidative trapping of radicals at molybdenum imido sites, and (2) migration of the allyl group from oxygen to an imido nitrogen atom.

International Nuclear Information System (INIS)

New Schiff base chelating ligands were synthesized by reacting equimolar quantities of 2,3-dimethyl-4-formyl-1-phenyl-3-pyrazoline-5-one and o-anisidine, p-anisidine, m-anisidine, o-toluidine, p-toluidine, m-toluidine, 2,6-xylidine or 2,4-xylidine in ethanol medium. Their subsequent reaction with gadolinium (III) nitrate hexahydrate in 2:1 molar ratio gave complexes that were characterized by elemental analyses, molar conductances, magnetic measurements, electronic and I.R. spectral studies. All the chelates were found to be non-electrolytic in nature. (author). 15 refs., 1 fig., 1 tab.

International Nuclear Information System (INIS)

The absorption and magnetic circular dichroism spectra of [N(n-Bu)_4]"+[(MeCp)_3PrCl]"- dissolved in 2-MeTHF were measured at room and at low temperatures. On the basis of these spectra the crystal field splitting pattern could be derived. The parameters of an empirical Hamiltonian were fitted to the energies of 42 levels to give an r.m.s. deviation of 23 cm"-"1. From the crystal field parameters obtained the crystal field strength of the ligand collective was estimated. Compared with neutral Cp_3Pr circle B complexes the crystal field strength of the anionic [(MeCp)_3PrCl]"- moiety is unusually low. (orig.)

Energy Technology Data Exchange (ETDEWEB)

The present work focuses on investigations of a highly selective ligand for Am(III)/Ln(III) separation: bis-triazinyl-pyridine (BTP). By means of nano-electro-spray mass spectrometry, complex formation of BTP with selected elements of the lanthanide series is investigated. We show that the diluent drastically influences complex speciation. Measurements obtained in the extraction-relevant diluent 1-octanol show the occurrence of Ln(BTP){sub i} (i 1-3) species in different relative abundances, depending on the lanthanide used. Here, the relative abundances of the Ln(BTP){sub 3} complexes correlate with the distribution ratios for extraction to the organic phase of the respective lanthanide. (authors)

Science.gov (United States)

Platinum and ruthenium in carbon supported Pt and Pt-Ru catalysts were determined by direct and derivative spectrophotometric methods. Complexes of platinum and ruthenium with SnCl(3)(-) ligands (tin(II) chloride in HCl) were used to determine both metals in solutions obtained after digestion of the samples of the catalysts. Platinum in the Pt/C catalyst can be determined in solutions obtained by digestion of the samples in aqua regia. Derivative spectrophotometry was used to determine both metals in the presence of each other in solutions obtained after digestion of samples of the Pt-Ru/C catalyst in the mixture of HCl+HNO(3) (6:1). The first derivative at 377 nm (;zero-crossing' point of ruthenium) and the second-derivative values at 495 nm (;zero-crossing' point of platinum) were used to estimate the concentration of platinum and ruthenium, respectively. PMID:18967441

Energy Technology Data Exchange (ETDEWEB)

Carbohydrate and nucleotide structural determination using modern spectroscopic techniques is dependent on our ability to label oligonucleotides and oligosaccharides with stable isotopes. Uniform Carbon 13 and Nitrogen 15 labeling of oligonucleotides is important to present-day efforts, which are focused on determining the structure of relatively small oligosaccharides and oligonucleotides, which form the elements of larger structures. Because of the relatively recent interest in three-dimensional structure, the development of techniques used to label them has lagged behind parallel techniques used to label peptides and proteins. Therefore, this group`s discussion focused primarily on problems faced today in obtaining oligonucleotides labeled uniformly with carbon 13 and nitrogen 15.

British Library Electronic Table of Contents (United Kingdom)

Apelin is a peptide known as the ligand of the G-protein-coupled receptor APJ. Several active apelin forms exist such as apelin-36, apelin-17, apelin-13, and the pyroglutamated form of apelin-13. Apelin and APJ are expressed in the central nervous system, particularly in the hypothalamus and in many peripheral tissues. Apelin has been shown to be involved in the regulation of cardiovascular and fluid homeostasis, food intake, cell proliferation, and angiogenesis. In addition to be an ubiquitous peptide, apelin is also produced and secreted by adipocytes and thus considered as an adipokine. This has opened a new field of investigation establishing a link between apelin and metabolic disorders (obesity, type 2 diabetes, etc.) which is the focus of the present review. Several studies, but not...

British Library Electronic Table of Contents (United Kingdom)

A new procedure for preparing an 211At-labeled radiopharmaceutical is suggested. The 211At? anion forms a strong bond with the Rh3+ cation incorporated in the complex with a thiother ligand, 1,5,9,13-tetrathiacyclohexadecane-3,11-diol (16-S4-diol). The reaction conditions are optimized with 131I as astatine analog. The complexes are studied by paper electrophoresis, ion exchange, and thin-layer chromatography. The kinetics of the addition of the 131I? anion to Rh(16-S4-diol) and the dependence of the yield of the forming complex 131I-Rh(16-S4-diol) on the temperature, solution acidity, and reactant concentrations are examined. Taking into account the results obtained, the complex 211At-Rh(16-S4-diol) is prepared by adding astatide (211 At?) to equivalent amounts of RhCl3 and the tetrathioe...

Energy Technology Data Exchange (ETDEWEB)

The murine 3T3-L1 fibroblast under appropriate incubation conditions differentiates into an adipocyte phenotype. This 3T3-L1 adipocyte exhibits many of the morphologic, biochemical, and insulin-responsive features of the normal rodent adipocyte. Using quantitative electron microscopic (EM) autoradiography we find that, when /sup 125/I-insulin is incubated with 3T3-L1 adipocytes, the ligand at early times of incubation localizes to the plasma membrane of the cell preferentially to microvilli and coated pits. When the incubation is continued at 37 degrees C, /sup 125/I-insulin is internalized by the cells and preferential binding to the villous surface is lost. With the internalization of the ligand, two intracellular structures become labeled, as determined by the method of hypothetical grain analysis. These include large clear, presumably endocytotic, vesicles and multivesicular bodies. Over the first hour of incubation the labeling of these ...

International Nuclear Information System (INIS)

Three regio-isomers of N-(N-benzylpiperidin-4-yl)-4-iodobenzamide, IBP, were prepared and evaluated for their sigma affinities. All three isomers (2, 3, and 4-substituted) showed high affinities for sigma-1 receptors in guinea pig brain membranes (Ki - 1.64 nM, 3.02 nM, 1.70 nM respectively) against ["3H]-(+)-pentazocine, a sigma-1 selective ligand. 2-IBP and 4-IBP showed modest affinities for sigma-2 sites in rat liver (Ki = 29.6 nM. 25.2 nM respectively) against ["3H]DTG in the presence of dextrallorphan to mask sigma-1 sites. The homologous competition binding studies of 4-["1"2"5I]BP in MCF-7 human breast tumor cells showed high affinity dose-dependent binding. Competition binding studies with haloperidol and DTG also showed a high affinity binding (Ki = 4.6 nM, 60 nM respectively), demonstrating the sigma specificity. The saturation binding (Scatchard analysis) of ["3H]DTG with MCF-7 cell membrane preparations gave Kd of 24.54 nM and a Bmax of 2071 fmol/mg ...

International Nuclear Information System (INIS)

A single round of Edman degradation was employed to remove the NH_2-terminal valine from isolated #alpha# chains of human hemoglobin. Reconstitution of normal #beta# chains with truncated or substituted #alpha# chains was used to form truncated (des-Val"1-#alpha#1) and substituted ([[1-"1"3C]Gly"1]#alpha#1) tetrameric hemoglobin analogs. Structural homology of the analogs with untreated native hemoglobin was established by using several spectroscopic and physical methods. Functional studies indicate that the reconstituted tetrameric protein containing des-Val"1-#alpha# chains has a higher affinity for oxygen, is less influenced by chloride ions or 2,3-biphosphoglycerate, and shows lower cooperativity than native hemoglobin. These results confirm the key functional role of the #alpha#-chain NH_2 terminus in mediating cooperative oxygen binding across the dimer interface. The NH_2-terminal pK/sub 1/2/ value was determined for the ["1"3C]glycine-substituted analog to be 7.46 +/- 0.09 at ...

Science.gov (United States)

The natriuretic peptides are considered to be cardioprotective; however, their receptors have not been identified in human myocardium using radiolabeled analogs. Dendroaspis natriuretic peptide (DNP) has been recently identified as a new member of this peptide family and is thought to be less susceptible to enzymatic degradation. Therefore, we have developed the novel radiolabeled analog [125I]-DNP and used this to localize high-affinity (K(D)=0.2 nmol/L), saturable, specific binding sites in adult human heart (n=6) and coronary artery (n=8). In competition binding experiments, atrial natriuretic peptide and brain type natriuretic peptide had greater affinity for [125I]-DNP binding sites than C-type natriuretic peptide and the natriuretic peptide receptor (NPR)-C ligand, cANF. This rank order of potency suggested binding of [125I]-DNP was specific to NPR-A. Messenger RNA encoding NPR-A was identified in left ventricle and coronary artery smooth muscle, and ...

International Nuclear Information System (INIS)

Introduction: Development of agonist positron emission tomography (PET) radioligands for the 5-HT neurotransmitter system is an important target to enable the understanding of human 5-HT function in vivo. ["1"1C]CUMI-101, proposed as the first 5-HT_1_A receptor agonist PET ligand, has been reported to behave as a potent 5-HT_1_A agonist in a cellular system stably expressing human recombinant 5-HT_1_A receptors. In this study, we investigate the agonist properties of CUMI-101 in rat brain tissue. Methods: ["3"5S]-GTP#gamma#S binding studies were used to determine receptor function in HEK (human embryonic kidney) 293 cells transfected with human recombinant 5-HT_1_A receptors and in rat cortex and rat hippocampal tissue, following administration of CUMI-101 and standard 5-HT1A antagonists (5-HT, 5-CT and 8-OH-DPAT). Results: CUMI-101 behaved as an agonist at human recombinant 5-HT_1_A receptors (pEC_5_0 9.2). However, CUMI-101 did not show agonist activity in either ...

International Nuclear Information System (INIS)

A burgeoning interest in technetium coordination chemistry has been spurred by its widespread use in nuclear medicine. Recent focus has been on the design and preparation of new technetium complexes, the lipophilicity, polarity, and overall charge of which can be readily altered by simple substitutions in the molecular framework of the ligand in order to optimize the biodistribution and target specific organs. Examples are cationic (Cardiolite) and neutral (Ceretec) technetium complexes, used as myocardial and brain imaging agents, respectively. The authors have been pursuing a continuing study of tris(3-hydroxy-4-pyridinonato)gallium and -indium complexes that are water soluble, are hydrolytically stable, and are of varying lipophilicity and neutral charge. Studies of in vivo in rabbits and mice have revealed that several of these cationic complexes may be useful as morphologic kidney imaging agents, with ["9"9"mTc(pap)_3]"+ showing elevated levels in the kidneys ...

International Nuclear Information System (INIS)

New RNAA determinations of Ba, Sr, Zr, U, Re, Pd, Ag, Zn and Se and INAA measurements of Lu are added to published data for 21 other elements in the same suite of ten samples. On the average, 21 refractory elements are not significantly fractionated from one another. The mean of their enrichment factors relative to C1 chondrites is 17.5 +- 0.4, indicating that the high-temperature condensate inclusions represent 5.7 wt% of the total condensable matter. Os, Ir, Ru, Re and most of the W condensed in one or more refractory siderophile element alloys along with small fractions of the Pd, Co, Au and Ag. The bulk of the Eu and Sr condensed in solid solution in melilite. Sc, Zr, Hf, Ta, U and the remaining REE condensed in a phase whose abundance in the inclusions in negatively correlated with that of melilite, either diopside or one or more minor or trace phases, including perovskite. Ba condensed in a different phase, separately from all these ...

Science.gov (United States)

The optimal concentrations of nutrient medium components, aeration conditions, and pH providing for maximum biomass yields, as well as fumarase and L-aspartase activities, during submerged cultivation of Erwinia sp. were determined. The data showed that different concentrations of carbon source (molasses) and pH of the nutrient medium were required to reach the maximum fumarase and L-aspartase activities. Calculations performed by application of the additive lattice model suggested that the combination of these optimized factors would result in 3.2-, 3.4-, and 3.8-fold increases as compared to the experimental means in Erwinia sp. biomass, and L-aspartase and fumarase activities, respectively. The conditions of the fumaric acid biotransformations into L-malic and L-aspartic acids were optimized on the basis of intact Erwinia sp. cells, a fumarase and L-aspartase producer. In the cases of fumarate transformation into L-malic acid and of fumarate transformation into L-aspartic acids, ...

Science.gov (United States)

The global spread of HIV and AIDS has presented a major threat to development, affecting the health of the poor and many aspects of social and economic development. The greatest impact of the epidemic has been felt in sub-Saharan Africa, and Zambia ranks among the worst hit countries. The Free Basic Education Policy in Zambia upholds the right of all children to a universal basic education. This study explored staff and student perceptions of the impact of the epidemic on access to, and the quality of, basic education for AIDS-affected children, orphans and other vulnerable children (OVCs) in the Copperbelt Province of Zambia, where the HIV/AIDS prevalence rate ranges from 34 to 40%, and life expectancy has dropped to 33 years. Data were collected from education personnel in six districts of the Copperbelt with the highest prevalence of HIV and AIDS and from staff and students in six schools. The data indicated a range of factors that adversely affect the access to, and quality of, ...

Energy Technology Data Exchange (ETDEWEB)

Rhenium is technetium`s third row congener and exhibits many of the chemical properties that technetium displays. Theoretically, a Re-PhAT complex will be isostructural with the {sup 99m}Tc PhAT complexes that have been prepared for use as brain imaging agents. A series of neutral rhenium(V) oxo complexes was synthesized by the reaction of ReOBr{sub 4}{sup {minus}} with diamino-thiol-thioether ligands of the type (RSC(CH{sub 3}){sub 2})CH{sub 2}NH(o-C{sub 6}H{sub 4})NHCH{sub 2}C(CH{sub 3}){sub 2}SH. The complexes were characterized by IR, UV/visible, and {sup 1}H and {sup 13}C NMR spectroscopy and by fast-atom-bombardment mass spectroscopy. The single-crystal X-ray structure determination on two of the complexes, where R = CH{sub 2}CH{double_bond}CH{sub 2} and CH{sub 2}CH{sub 2}-CH{sub 3}, showed them to consist of a square pyramidal Re{sup V}ON{sub 2}S{sub 2} core. ReO[CH{sub 2}{double_bond}CHCH{sub 2}SC(CH{sub 3}){sub 2}CH{sub 2}N(o-C{sub 6}H{sub 4})NCH{sub ...

Science.gov (United States)

Escherichia coli spheroplast protein y (EcSpy) is a small periplasmic protein that is homologous with CpxP, an inhibitor of the extracytoplasmic stress response. Stress conditions such as spheroplast formation induce the expression of Spy via the Cpx or the Bae two-component systems in E. coli, though the function of Spy is unknown. Here, we report the crystal structure of EcSpy, which reveals a long kinked hairpin-like structure of four ?-helices that form an antiparallel dimer. The dimer contains a curved oval shape with a highly positively charged concave surface that may function as a ligand binding site. Sequence analysis reveals that Spy is highly conserved over the Enterobacteriaceae family. Notably, three conserved regions that contain identical residues and two LTxxQ motifs are placed at the horizontal end of the dimer structure, stabilizing the overall fold. CpxP also contains the conserved sequence motifs and has a predicted secondary structure similar ...

International Nuclear Information System (INIS)

Thallium-201 diethyldithiocarbamate (DDC) behaves like a chemical microsphere and is trapped by spontaneous decomposition in the brain in proportion to regional perfusion. They have shown that the technetium-99m analog, Tc-99m DDC (1), is unsuitable for cerebral perfusion imaging because it does not decompose rapidly enough to be trapped in the brain. With the goal of turning this greater stability of 1 into an advantage, a series of dithiocarbamates with lipophilic or amine groups designed to enhance cerebral uptake and retention was prepared from the following amines by reaction with carbon disulfide and sodium hydroxide: pyrrolidine (2), piperazine (3), 4-benzylpiperazine (4), and 4-(1-piperidino)piperidine (5). These ligands (5 mg) were labelled with Tc-99m in > 95% efficiency (ITLC-SG, saline) by reduction of pertechnetate at room temperature with formamidine sulfinic acid at alkaline pH. In preliminary studies, 4 and 5 show a trend of increasing oil/buffer ...

Energy Technology Data Exchange (ETDEWEB)

A series of (diamine)isopropylidenmalonatoplatinum(II) complexes and the oxidation products, (diamine)Pt(OOC){sub 2}C=C(CH{sub 3}){sub 2}(X){sub 2}, (diamine=ethylenediamine(en), 1,2-diaminopropan(dap), N-methylethylenediamine(men); X=OH, OCOCH{sub 3}, OCOCF{sub 3}), have been prepared, and their interaction with guanosine-5'-monophosphate (5'-GMP) have been examined by means of {sup 1}H NMR spectroscopy. The present platinum(II) complexes have shown to interact with 5'-GMP through N7 coordination in two consecutive steps in a similar way as with cisplatin, but no interaction between the present platinum(IV) complexes and 5'-GMP was observed. However, in the presence of ascorbic acid, the platinum(IV) complexes have been found to interest with 5'-GMP with the reation rate depending on their reduction rate.

Energy Technology Data Exchange (ETDEWEB)

NMR and CD studies indicate that Mg/sup 2 +/ and Ca/sup 2 +/ are able to change the conformation of tetracycline in DMSO solution. This may affect the in vivo effect of tetracycline. Using /sup 23/Na NMR, the formation constant of NaLAS (LAS represents the anion of lasalocid A) was found to be 80 M/sup -1/ which is much smaller than that in less polar solvents. Spin-lattice relaxation measurements were made to study the binding sites of Gd/sup 3 +/ on Las in ChCl/sub 3/-DMF mixed solvent system. No intermediate conformation (between cyclic and open-chain) was found. LAS was found to be a good second-sphere ligand to inert transition-metal amines. NMR studies suggest that LAS is in cyclic conformation when bound to these metal amines. A new method for the synthesis of spin-labeled anticancer Pt(II) complexes was developed. It is very simple and gives high yield of pure spin-labeled Pt(II) complexes.

Science.gov (United States)

Erectile dysfunction following radical prostatectomy remains a frequent problem despite the development of nerve-sparing techniques. This erectile dysfunction is believed to be neurogenic, enhanced by hypoxia-induced structural changes which result in additional veno-occlusive dysfunction. Recently, daily use of intracavernous vasoactive substances and oral use of PDE5-inhibitors have been clinically studied for treatment of postprostatectomy erectile dysfunction. Since these studies showed benefits of "penile rehabilitation therapy," these effects have been studied in a preclinical setting. We reviewed experimental literature on erectile tissue preserving and neuroregenerative treatment strategies, and found that preservation of the erectile tissue by the use of intracavernous nitric oxide donors or vasoactive substances, oral PDE5-inhibitors, and hyperbaric oxygen therapy improved erectile function by antifibrotic effects and preservation of smooth muscle. Furthermore, ...

Science.gov (United States)

CD-NP is a novel chimeric natriuretic peptide (NP) consisting of the 22-amino-acid (AA) human C-type natriuretic peptide (CNP), a venodilating peptide with limited renal actions and minimal effects on blood pressure, and the 15-AA C-terminus of Dendroaspis NP (DNP). The rationale for the design of CD-NP was to enhance the renal actions of CNP, the ligand for natriuretic peptide receptor-B, but without inducing excessive hypotension. Here we report the first-in-human studies for CD-NP, which represent the first successful clinical testing of a chimeric NP demonstrating in normal human volunteers that CD-NP possesses cyclic guanosine monophosphate-activating, natriuretic, and aldosterone-suppressing properties without inducing excessive hypotension, laying the foundation for additional studies on this first-in-class new cardiovascular therapeutic in human heart failure, which are now underway worldwide. PMID:19395584

Science.gov (United States)

There is an increased emphasis on hyphenated techniques such as immunoaffinity LC/MS/MS (IA-LC/MS/MS) or IA-LC/MRM. These techniques offer competitive advantages with respect to sensitivity and selectivity over traditional LC/MS and are complementary to ligand binding assays (LBA) or ELISA's. However, these techniques are not entirely straightforward and there are several tips and tricks to routine sample analysis. We describe here our methods and procedures for how to perform online IA-LC/MS/MS including a detailed protocol for the preparation of antibody (Ab) enrichment columns. We have included sample trapping and Ab methods. Furthermore, we highlight tips, tricks, minimal and optimal approaches. This technology has been shown to be viable for several applications, species and fluids from small molecules to proteins and biomarkers to PK assays. PMID:21872661

Energy Technology Data Exchange (ETDEWEB)

In developing new Tc-99m brain perfusion imaging agents for SPECT, a series of BAT (bis-aminoethanethiol) derivatives was prepared. These N/sub 2/S/sub 2/ ligands formed stable and neutral complexes with reduced Tc-99m, either by Sn(II)-PPi or sodium borohydride reduction. The purity of the Tc-99m complexes was >95% (HPLC reverse-phase column, acetonitrile: pH 7.0 buffer, 85:15). The biodistribution in rats was evaluated using I-125 iodoantipyrine (IAP), a free diffusible tracer, as the internal reference. Compounds with a free hydroxyl group (I and IV) showed lower brain uptake, inspite of high P.C.; this may be related to in vivo instability of the complexes. High initial brain uptake was observed for three compounds (II, III and V), however, only compound V (P.C.=384) showed significant brain retention. Planar imaging with compound V in a monkey demonstrated that the compound localized in brain and the retention time was T/sub 1/2/=35 min. Compounds of this ...

Energy Technology Data Exchange (ETDEWEB)

S-Adenosylmethionine decarboxylase (AdoMetDC) is a critical enzyme in the polyamine biosynthetic pathway and depends on a pyruvoyl group for the decarboxylation process. The crystal structures of the enzyme with various inhibitors at the active site have shown that the adenine base of the ligands adopts an unusual syn conformation when bound to the enzyme. To determine whether compounds that favor the syn conformation in solution would be more potent AdoMetDC inhibitors, several series of AdoMet substrate analogues with a variety of substituents at the 8-position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. The biochemical analysis indicated that an 8-methyl substituent resulted in more potent inhibitors, yet most other 8-substitutions provided no benefit over the parent compound. To understand these results, we used computational modeling and X-ray crystallography to study C{sup 8}-substituted adenine analogues bound in the ...

International Nuclear Information System (INIS)

New oxomolybdenum(V) complexes MoOClL (where LH_2 = Schiff base) derived from ethanolamine and salicylaldehyde, 5-chlorosalicylaldehyde, 5-bromosalicylaldehyde, 5-nitrosalicylaldehyde, 3-ethoxysalicylaldehyde and 2-hydroxy-1-naphthaldehyde have been synthesized and characterised by elemental analyses, conductance, molecular weight, i.r. and electronic spectra and magnetic measurements. The Schiff bases behave as dibasic tridentate ONO donor ligands. The complexes are non-electrolytes and dimers. The complexes exhibit subnormal magnetic moments and are involved in antiferromagnetic exchange with S = 0 ground state. The complexes exhibit electronic spectral bands at ca. 13000 and ca. 17000 cm"-"1 due to the transitions dsub(xy)->dsub(xz,yz) ("2B_2->"2E) and dsub(xy)->dsub(x2-y2) ("2B_2->"2B_1), respectively. The #nu#(Mo=O) frequency of the complexes is observed in the 900-970 cm"-"1 region. On the basis of the magnetic susceptibility, i.r. and molecular ...

British Library Electronic Table of Contents (United Kingdom)

Objective: To study the effects of minocycline hydrochloride (MINO) on the formation of tartrate-resistant acid phosphatase (TRAP) staining-positive multinucleated osteoclast-like cells in mouse bone marrow cells (BMCs) treated with 1@a,25(OH)"2D"3 or soluble receptor activator of nuclear factor-@kB ligand (s-RANKL). Materials and methods: Mouse BMCs were cultured in alpha-modified minimum essential medium containing foetal calf serum (10%) and tetracyclines (2.5, 5 and 10@mM), such as MINO, tetracycline hydrochloride (TC), oxytetracycline hydrochloride (OXT) or doxycycline (DOXY) in the presence of 1@a,25(OH)"2D"3 (10nM) or s-RANKL (20ng/ml) for 7 days, and the number of TRAP staining-positive osteoclast-like cells was counted. In RNA isolated from BMCs treated with 1@a,25(OH)"2D"3 or s-R...

Energy Technology Data Exchange (ETDEWEB)

The e.s.r. spectra of (AsPh/sub 4/)(TcNCl/sub 4/), Cs/sub 2/(TcNCl/sub 5/), (AsPh/sub 4/)(TcNBr/sub 4/), and Cs/sub 2/(TcNBr/sub 5/) have been studied in non-aqueous and concentrated aqueous acid solutions. None of the spectra shows evidence for the co-ordination of a fifth halide ligand in the trans position, even under circumstances such as a 2 000-fold excess of halide ion, which would be expected to favour the formation of the pentahalogenonitridotechnetate ion. The predominant species in solution is the tetrahalogenonitridotechnetate ion, where the trans position may be vacant or occupied by a solvent molecule in the case of the non-aqeuous solvents and by a water molecule in the case of HCl and HBr solutions. This conclusion may be contrasted with the behaviour of a number of tetra- and penta-halogeno-oxometal complexes, where the equilibrium (MOX/sub 4/)sup(n-) + X/sup -/< - - > (MOX/sub 5/)sup(n + 1)/sup -/ is clearly established.

International Nuclear Information System (INIS)

The heavy chains of Acanthamoeba myosins, IA, IB and II, turkey gizzard myosin, and rabbit skeletal muscle myosin subfragment-1 were specifically labeled by radioactive ATP, ADP, and UTP, each of which is a substrate or product of myosin ATPase activity, when irradiated with uv light at 0"0C. With UTP, as much as 0.45 mol/mol of Acanthamoeba myosin IA heavy chain and 1 mol/mol of turkey gizzard myosin heavy chain was incorporated. Evidence that the ligands were associated with the catalytic site included the observations that reaction occurred only with nucleotides that are substrates or products of the ATPase activity; that the reaction was blocked by pyrophosphate which is an inhibitor of the ATPase activity; that ATP was bound as ADP; and that label was probably restricted to a single peptide following limited subtilisin proteolysis of labeled Acanthamoeba myosin IA heavy chain and extensive cleavage with CNBr and trypsin of labeled turkey gizzard myosin heavy ...

Science.gov (United States)

In the course of observing by means of Auger spectroscopy graphite gasification reactions catalyzed by metals, it has been found that in the presence of hydrogen, nickel appears to diffuse from the surface into the bulk of the graphite. When potassium is deposited on graphite, it is volatilized above 400/sup 0/C. Surprisingly the production of methane and carbon dioxide from the reaction of graphite and steam was catalyzed by potassium at as low a temperature as 250/sup 0/C. It has been shown that literature on the alkylation of benzene with synthesis gas is erroneous and that the products reported are due to Lewis acid catalyzed cracking of benzene. A novel cobalt mediated, reversible cleavage of a vinyl-hydrogen bond has been discovered. All products from the thermal decomposition of tetralin have been identified. The stereochemistry of cis-1, 2 dihydrotetralin was determined. In the utilization of the water gas shift reaction as a reducing agent for model coal compounds it has been ...

Energy Technology Data Exchange (ETDEWEB)

Polynuclear aromatic sulphur heterocycles (PASHs) were isolated from a coal extract by two-step separation method using silica gel column chromatography and ligand exchanges thin layer chromatography (PdCl{sub 2}/SiO{sub 2}). The subfraction was examined by capillary column gas chromatography with flame ionization detector and flame photometric detector and gas chromatography - mass spectrometry. Identification was accomplished by comparison of chromatographic retention indices and mass spectra of compounds with those reported in the literature. It was found that the principal structures of the sulphur-containing fraction of Guiding coal extract have 3-4 aromatic rings. Dibenzothiophene, C{sub 1} - C{sub 3} alkylated dibenzothiophenes, benzonaphthothiophene and its alkylated derivatives were the main compounds. Only a few other polynuclear sulfur heterocycles were detected. No benzothiophene and its derivatives were presented. 8 refs., 2 figs., 3 tabs.

Science.gov (United States)

Besides the multifunctionality, another equally important aspect of nanoparticles is their engineerability to control the geometrical and chemical properties during fabrication. In this work, we exploited this aspect to define asymmetric surface chemistry of an iron oxide nanosphere by controlling the topology of ligand expression on its surface resulting in a particle with two faces, one displaying only amines and the other only thiols. Specifically, amine-functionalized iron oxide nanospheres were attached on a solid support via a crosslinker containing a disulfide bridge. Liberation of the nanosphere using thiolytic cleavage created thiols on the portion of the particle's surface that interacted with the solid support. Employing a solid-phase strategy and a step-by-step addition of particles, the two unique faces on the same nanosphere served as fittings to assemble them into linear nano-chains. Assembly of chains with various lengths and aspect ratios was ...

Energy Technology Data Exchange (ETDEWEB)

In the search for new brain imaging agents for use with single photon emission computed tomography (SPECT), quantitative structure activity relationship (QSAR) analysis of the correlations between initial brain uptake and physicochemical parameters like lipophilicity, log P, molecular weight, log MW and log U/D (undissociated/dissociated), of the {sup 99m}Tc-DADT (diaminedithiol) complexes and {sup 99m}Tc-PAO (propyleneaminoxime) complexes have been analyzed. High correlations are found for both the {sup 99m}Tc-DADT complexes (r = 0.94) and for the {sup 99m}Tc-PAO complexes (r = 0.83) which are significant at 99.9 and 99.5 percentile level, respectively. These results will help the further design of better ligands for {sup 99m}Tc in brain imaging. (author).

Energy Technology Data Exchange (ETDEWEB)

A correlation investigation was carried out on the series of atomic coordinates (MPV) and temperature factor (T {sub f}), respectively for human hemoglobin and HIV-1 protease protein main chains. The MPV series revealed resemblances to the corresponding T {sub f} series. Each minor or major peak in a series had a corresponding peak in the related series. This brings a qualitative evidence for the connection of the two parameters. The series were further subjected to spectral and detrended fluctuation analysis which all revealed long-range correlation properties. This combined analysis revealed that the data were controlled both by the correlation of stationary fluctuation and trends or non-stationary contribution to correlation. The correlation of all MPV series was found to be much less sensitive to ligand binding than the corresponding T {sub f} series. Thus the long-range correlation properties of the protein main chain structure and mobility revealed two ...

International Nuclear Information System (INIS)

Paper describes a new procedure to synthesize a pharmaceutical containing "2"1"1At. "2"1"1At"- anion was found to bind strongly with Rh"3"+ cation complexing with a thio-ether ligand - 1,5,9,13-tetratiacyclohexadecane-3,11-diol (16-S4-diol). One made use of "1"3"1I isotope to seek for the optimal conditions of the reaction. The derived complexes were studied by means of the paper electrophoresis, the ion exchange, the surface chromatography. One studied the kinetics of "1"3"1I"- anion binding with Rh(16-S4-diol), the dependence of the yield of "1"3"1I-Rh(16-S4-diol) forming complex on the temperature. the acidity of the reaction mixture and the concentration of the reagents. On the basis of the determined conditions of the synthesis one prepared "2"1"1At-Rh(16-S4-diol) complex by more astatide ("2"1"1At"-) to the equivalent amounts of RhCl_3 and tetra-thio-ether (16-S4-diol). One studied its behaviour

International Nuclear Information System (INIS)

Serotonin is one of the neurotransmitters found in the brain and mediates brain functions. It is very well known that serotonin related brain abnormalities are exerted mainly via serotonin receptors in a similar manner to other neurotransmitters found in the brain. Recently, it has also been found that serotonin is involved in Alzheimer's disease either directly or indirectly by its actions on serotonergic neurons. To understand and treat the diseases caused by abnormalities in the serotonergic system in the brain, it is certain that its mechanism of function has to be well investigated. So far several 5-HT receptors and receptor subtypes have been well characterized. Moreover, serotonin agonists and antagonists acting on specific receptors are chemically synthesized and are now available for the prevention or treatment of serotonergic related diseases. In recent years, a great demand for developing neuroimaging agents has emerged for the diagnosis of abnormal brain functions in the ...

Science.gov (United States)

One-electron reduction of the square-planar nickel precursor (PNP)NiCl ( 1) (PNP (-) = N[2-P(CHMe 2) 2-4-methylphenyl] 2) with KC 8 effects ligand reorganization of the pincer ligand to assemble a Ni(I) dimer, [Ni(mu 2-PNP)] 2 ( 2), containing a Ni 2N 2 core structure, as inferred by its solid-state X-ray structure. Solution magnetization measurements are consistent with a paramagnetic Ni(I) system likely undergoing a monomer dimer equilibrium. The room-temperature and 4 K solid-state X-band electron paramagnetic resonance (EPR) spectra display anisotropic signals. Low-temperature solid-state X-band EPR data at 4 K reveal rhombic values g z = 1.980(4), g x = 2. 380(4), and g y = 2.225(4), as well as a forbidden signal at g = 4.24 for the Delta M S = 2 half field transition, in accord with 2 having two weakly interacting metal centers. Utilizing an S = 1 model, full spin Hamiltonian simulation of the low-temperature EPR spectrum on the solid ...

Energy Technology Data Exchange (ETDEWEB)

A series of dinuclear platinum(II) complexes, [(dien)Pt(NH{sub 2}(CH{sub 2}){sub n}NH{sub 2})Pt(dien)]Cl{sub 4} (dien = diethylenetriamine, n = 8, 9, 10, and 12) and their corresponding [2]rotaxanes with {alpha}-cyclodextrin ({alpha}-CD), [(dien)Pt{l_brace}NH{sub 2}(CH{sub 2}){sub n}NH{sub 2}{center_dot}{alpha}-CD{r_brace}Pt(dien)]Cl{sub 4}, have been synthesized and characterized by {sup 1}H, {sup 13}C, and {sup 195}Pt NMR spectroscopy and electrospray mass spectrometry. The rotaxanes were prepared by reacting the {l_brace}NH{sub 2}(CH{sub 2}){sub n}NH{sub 2}{center_dot}{alpha}-CD{r_brace} pseudorotaxanes with [Pt(dien)]Cl, to stopper the included linear {alpha},{omega}-diaminoalkane chains with the inert Pt(II) end groups. The kinetics of the self-assembly and dissociation of the {beta}-CD rotaxane, [(dien)Pt{l_brace}NH{sub 2}(CH{sub 2}){sub 10}NH{sub 2}{center_dot}{beta}-CD{r_brace}Pt(dien)]{sup 4+}, were investigated by using {sup 1}H NMR and are indicative of a slippage mechanism, ...

Energy Technology Data Exchange (ETDEWEB)

The palladium(II) and platinum(II)complexes(where, (M(L){sub 2}X{sub 2}), M=Pd(II), Pt(II); L=isoxazole (isox), 3, 5-dimethylisoxazole(3, 5-diMeisox), 3-methyl, 5-phenylisoxazole(3-Me, 5-Ph-isox), and 4-amino-3, 5-di-methylisoxazole (4-ADI); X=Cl, Br) with isoxazole and its derivatives were investigated on antitumor activity by MM2 and EHMO calculation. Because for all the complexes the {sigma}MO energy level (E{sub {sigma}}{sub (M-X)} between d{sub x}{sup 2}{sub -y}{sup 2} orbital of central metal and p{sub x} orbital of halogen atom is less than {sigma}MO energy level E{sub {sigma}}{sub (M-N)} between d{sub x}{sup 2}{sub -y}{sup 2} orbital of central metal and p{sub x} orbital of N atom, without exception. And judging, from the lower E{sub {sigma}}{sub (M-X)} value in trans, the bonding strength was found to be weaker in trans isomer than in cis. For the Pd(II) and Pt(II) complexes which have planar ligands, it was shown that for all the complexes dissociation of ...

International Nuclear Information System (INIS)

The effect of in vitro and in vivo administration of ethanol on the binding of "3"5S-t-butyl-bicyclophosphorothionate ("3"5S-TBPS) to cortical brain membranes of C57B1 mice was investigated using KCl (100 mM) containing assay media. The in vitro addition of ethanol produced a dose-dependent inhibition of basal "3"5S-TBPS binding. In the presence of chloride ions, GABA and pentobarbital had a biphasic action (stimulation followed by inhibition) on "3"5S-TBPS binding, whereas diazepam only stimulated the binding. Ethanol reduced the stimulatory effects of GABA and pentobarbital in a dose-dependent manner, but had no effect on the enhancement of "3"5S-TBPS binding produced by diazepam. "3"5S-TBPS binding to cortical brain membranes was inhibited by the putative Cl"- channel blocking agent DIDS. This inhibitory action of DIDS was significantly, and dose-dependently reduced by ethanol (#<=# 100 mM ethanol). Chronic ethanol ingestion in vivo, which produced tolerance to and physical ...

Energy Technology Data Exchange (ETDEWEB)

The functional interaction between the peroxisome proliferator-activated receptor {gamma} (PPAR{gamma}) and its coactivator PGC-1{alpha} is crucial for the normal physiology of PPAR{gamma} and its pharmacological response to antidiabetic treatment with rosiglitazone. Here we report the crystal structure of the PPAR{gamma} ligand-binding domain bound to rosiglitazone and to a large PGC-1{alpha} fragment that contains two LXXLL-related motifs. The structure reveals critical contacts mediated through the first LXXLL motif of PGC-1{alpha} and the PPAR{gamma} coactivator binding site. Through a combination of biochemical and structural studies, we demonstrate that the first LXXLL motif is the most potent among all nuclear receptor coactivator motifs tested, and only this motif of the two LXXLL-related motifs in PGC-1{alpha} is capable of binding to PPAR{gamma}. Our studies reveal that the strong interaction of PGC-1{alpha} and PPAR{gamma} is mediated through both ...

International Nuclear Information System (INIS)

Full text: In case of lanthanide (Ln) compounds the bis(trimethylsilyl)amido (btmsa) ligand is considered as a steric and electronic equivalent of the bis(trimethylsilyl)methanido (btmsm) group . Because of their extreme air and moisture sensitivity the chemistry of Ln(btmsm)_3 is very poor, whereas that of comparatively stable Ln(btmsa)_3 is much more developed. As we wish to extend the chemistry of Ln(btmsm)_3 and plan to derive and to parameterize the crystal field (CF) splitting patterns of the target molecules, it is recommended to study in advance the electronic structures of the corresponding compounds derived from Ln(btmsa)_3 . Beside (btmsa)_3 Nd(m-Cl)Li(THF)_3 a number of mono base adducts [(btmsa)_3 Ln.B] with sterically less demanding bases such as OPPh_3 , NCtBu or CNtBu have been described and were partly structurally characterized. Considering only the immediately coordinating atoms, the effective CF is of C_3_v symmetry. According to recent ...

International Nuclear Information System (INIS)

The utility of recording Raman spectroscopy under liquid nitrogen, a technique we call Raman Under Nitrogen (RUN), is demonstrated for ferrocene, uranocene and thorocene. Using RUN, low temperature (liquid nitrogen cooled) Raman spectra for these compounds exhibit higher resolution than previous studies and new vibrational features are reported. The first Raman spectra of crystalline uranocene at 77 K are reported using excitation from argon (5145 ) and krypton (6764 ) ion lasers. The spectra obtained showed bands corresponding to vibrational transitions at 212, 236, 259, 379, 753, 897, 1500, and 3042 cm-1 , assigned to ring-metal-ring stretching, ring-metal tilting, out-of-plane CCC bending, in-plane CCC bending, ring-breathing, C-H bending, CC stretching and CH stretching, respectively. The assigned vibrational bands are compared to those of uranocene in THF and thorocene. All vibrational frequencies of the ligands, except the 259 cm-1 out-of-plane CCC bending ...

Energy Technology Data Exchange (ETDEWEB)

We labelled Lipiodol with yttrium-90 and analysed the biodistribution in rats after intrahepatic arterial injection. An RP-18 column was used to separate {sup 90}Y from strontium-90. {sup 90}Y was retained on the column, which had been pretreated with yttrium-selective extraction reagent, di(2-ethylhexyl) phosphate, while {sup 90}Sr was washed out. A hexadentate nitrogen-donor chelating ligand N,N,N`,N`-tetrakis(2-benzymidazolylmethyl)-1,2-ethanediamine (EDTB) was synthesized by condensation of 1,2-benzenediamine and ethylene diamine tetra-acetic acid (EDTA). Lipiodol was covalently conjugated with EDTB. The final product was obtained by eluting the retained {sup 90}Y from the RP-18 column with EDTB-Lipiodol. Sixteen male rats (Sprague-Dawley) were sacrificed at 1 h, 24 h, 48 h and 72 h (four rats at each time) after injection of approximately 0.1 mCi {sup 90}Y-Lipiodol via the hepatic artery. Samples of liver, spleen, muscle, lung, kidney, bone, whole blood and ...

Science.gov (United States)

Synthetic atrial natriuretic peptide (carperitide) and B-type natriuretic peptide (BNP; nesiritide) are used to treat congestive heart failure. However, despite beneficial cardiac unloading properties, reductions in renal perfusion pressures limit their clinical effectiveness. Recently, CD-NP, a chimeric peptide composed of C-type natriuretic peptide (CNP) fused to the C-terminal tail of Dendroaspis natriuretic peptide (DNP), was shown to be more glomerular filtration rate-enhancing than BNP in dogs. However, the molecular basis for the increased responsiveness was not determined. Here, we show that the DNP tail has a striking effect on CNP, converting it from a non-agonist to a partial agonist of natriuretic peptide receptor (NPR)-A while maintaining the ability to activate NPR-B. This effect is specific for human receptors because CD-NP was only a slightly better activator of rat NPR-A due to the promiscuous nature of CNP in this species. Interesting, the DNP tail alone had no effect ...

Energy Technology Data Exchange (ETDEWEB)

Positron Emission Tomography (PET) was used to analyze in vivo antagonist binding to human myocardial muscarinic cholinergic receptor. The methiodide salt of the muscarinic antagonist, quinuclidinyl benzilate (MQNB), was labeled with the positron emitter, Carbon-11, and injected intravenously to 8 normal subjects. /sup 11/C-MQNB concentration was determined in vivo in the ventricular septum from 40 cross-sectional images acquired at the same transverse level over a period of 70 minutes. In 4 subjects, various amounts of unlabeled atropine were rapidly injected at 20 minutes to study whether atropine competitively inhibited MQNB. The kinetics of binding of /sup 11/C-MQNB were not the same in vivo and in vitro. The apparent dissociation rate of /sup 11/C-MQNB in vivo was much slower (by 1 to 2 orders of magnitude) than that observed in vitro with /sup 3/H-QNB. After atropine injection, /sup 11/C-MQNB dissociated from its binding sites at a rate that apparently depended on the amount of ...

International Nuclear Information System (INIS)

Three major monomeric hemoglobins have been isolated from the erythrocytes of Glycera dibranchiata. Their importance to structure-function studies of heme proteins lies in the fact that they have been shown to possess an exceptional amino acid substitution. In these proteins, the E-7 position is occupied by leucine rather than the more common distal histidine. This substitution alters the polarity of the heme ligand binding environment compared to myoglobin. Due to this, the G. dibranchiata monomer hemoglobins are attracting much attention. However, until now no purity criterion has been developed. Here the authors demonstrate that, for all of the Glycera momomer hemoglobins, multiple line patterns are shown on high-voltage isoelectric focusing (IEF) gels. Most of these lines are shown to be a consequence of heme-related phenomena and can be understood on the basis of changes in oxidation and ligation state of the heme iron. The multiple line pattern does not ...

International Nuclear Information System (INIS)

The PbII binding characteristics of the previously reported PbII binding proteins of rat kidney cytosol were investigated further. Saturation and Scatchard analysis of "2"0"3Pb binding in whole cytosol and in 40% saturated ammonium sulfate precipitated fractions disclosed a class of relatively high-affinity sites with an apparent Kd of approximately 50 nM and binding capacities of approximately 41 and 9 pmol/mg of protein, respectively. Two "2"0"3Pb binding proteins with approximate molecular masses of 63K and 11.5K daltons and a high molecular weight component (greater than 200K) were isolated by Sepharose-6B column chromatography. The time course of association of "2"0"3Pb with cytosol and the 63K protein showed maximum binding at 18 hr which was stable up to 25 hr at 4 degrees C. The approximate half-time dissociation rate (T 1/2) of specifically bound "2"0"3Pb to the 63K protein was 100 min at 4 degrees C whereas the 11.5K protein showed little dissociation of specifically bound ...

Energy Technology Data Exchange (ETDEWEB)

The kinetics of the oxidative addition of CH/sub 3/I to platinum(II) complexes in aqueous solutions of K/sub 2/PtCl/sub 4/ and KPtCl/sub 3/(C/sub 2/H/sub 4/) have been studied by PMR and GLC. The second-order rate constants for the PtCl/sub 3/(H/sub 2/O)/sup -/ and PtCl/sub 4//sup 2 -/ particles are equal to 400 exp(-2.7 x 10/sup 3//T) and 3.18 x 10/sup 10/ exp(-9.2 x 10/sup 3//T) mole/sup -1/ x liter x sec/sup -1/, respectively. The introduction of a ..pi..-acceptor ligand, viz. ethylene, into the coordination sphere of platinum(II) results in a sharp drop in the rate, probably due to a decrease in the electron density on the platinum atom. According to the PMR data, the product of the oxidative addition of CH/sub 3/I to Zeise's salt is a methyl complex of platinum(IV), is identical to the complex obtained by reacting methyl iodide with K/sub 2/PtCL/sub 4/, and does not contain an olefin.

International Nuclear Information System (INIS)

In-vitro experiments using "2"0"3Pb were performed to identify the lead binding components in human peripheral blood. The distribution of lead in plasma, in the red cell membrane, and within the red cell was also investigated. Studies of the distribution of "2"0"3Pb in the whole blood showed that at a lead concentration of 2.45 #mu#mol/l (50 #mu#g/100 ml) about 94% of lead had been incorporated by the erythrocytes and 6% remained in the plasma. After extraction of lipid by a methanol/chloroform mixture, about 75% of the lead was found to be associated with the protein fraction. The lipid contained about 21% of the "2"0"3Pb, the remainder being in the aqueous plasma. SDS polyacrylamide gel electrophoresis of blood plasma showed that almost 90% of the "2"0"3Pb was present in the albumin fraction; the remainder was likely to be associated with high molecular weight globulins. Several binding sites were identified on the erythrocyte membrane. The high molecular weight component, about 130 ...

Science.gov (United States)

We describe the synthesis of metal-chelating polymers (MCPs) with four different pendant polyaminocarboxylate ligands (EDTA, DTPA, TTHA, DOTA) and an orthogonal end-group, either a fluorescein molecule or a bismaleimide linker for antibody attachment. Polymer characterization by a combination of (1)H NMR, UV/vis absorption measurements, and thermal gravimetric analysis (TGA) indicated that each chain of the fluorescein-terminated polymers contained one dye molecule. These polymer samples were loaded with three different types of lanthanide ions as well as palladium and platinum ions. The numbers of metal atoms per chain were determined by a combination of UV/vis and conventional ICP-MS measurements. The experiments with lanthanide ions demonstrated that a net anionic charge on the polymer is important for water solubility. These experiments also showed that at least one type of lanthanide ion (La(3+)) is capable of forming a bimetallic complex with pendant DTPA ...

International Nuclear Information System (INIS)

Aminophenpyramine, a derivative of mepyramine (pyrilamine), a typical antagonists of histamine at its H_1 receptor was synthesized and converted into ["1"2"5I]iodoazidophenpyramine, a potential photoaffinity probe for the H_1 receptor. In the dark, reversible binding of this probe to cerebellar membranes occurred with a K/sub d/ of 1.2 x 10"-"1"1 M and a B/sub max/ of 240 fmol/mg of protein and was inhibited by various H_1-receptor antagonists with the expected potencies. These features establish the compound as one of the most potent H_1-receptor antagonists known so far. Upon IV irradiation, 5% of the bound radioactivity was covalently incorporated into cerebellar membrane polypeptides as shown by standard NaDodSO_4/PAGE. Two bands of 47 and 56 kDa were consistently labeled, labeling being prevented by various H_1-receptor antagonists with the expected potencies and stereoselectivity. In the presence of protease inhibitors, labeling of the 56-kDa peptide increased at the expense of ...

International Nuclear Information System (INIS)

High-resolution "1H and "3"1P nuclear magnetic resonance spectroscopy has been used to investigate the binding of 2,3-diphosphoglycerate to human normal adult hemoglobin and the molecular interactions involved in the allosteric effect of the 2,3-diphosphoglycerate molecule on hemoglobin. Individual hydrogen ion NMR titration curves have been obtained for 22-26 histidyl residues of hemoglobin and for each phosphate group of 2,3-diphosphoglycerate with hemoglobin in both the deoxy and carbonmonoxy forms. The results indicate that 2,3-diphosphoglycerate binds to deoxyhemoglobin at the central cavity between the two #beta# chains and the binding involves the #beta#2-histidyl residues. Moreover, the results suggest that the binding site of 2,3-diphosphoglycerate to carbonmonoxyhemoglobin contains the same (or at least some of the same) amino acid residues responsible for binding in the deoxy form. As a result of the specific interactions with 2,3-diphosphoglycerate, the #beta#2-histidyl ...

Energy Technology Data Exchange (ETDEWEB)

Single crystals of RbBaTaS{sub 4} (1) and K{sub 2}BaTa{sub 2}S{sub 11} (2) were obtained from the reactions of Ta, with in situ formed fluxes of A{sub 2}S{sub 3} (A = K, Rb), BaS, and S at 500 C. Compound 1 crystallizes in the orthorhombic space group Pnma with a = 9.3286(5), b = 7.0391(4), c = 12.4365(7) A, V = 816.6(1) A{sup 3}, Z = 4. Compound 2 crystallizes in the monoclinic space group P2{sub 1}/c with a = 14.5280(10), b = 12.6347(7), c = 17.5148(12) A, {beta} = 94.744(8) , V = 3203.9(4) A{sup 3}, Z = 4. The structure of RbBaTaS{sub 4} (1) consists of isolated tetrahedral [TaS{sub 4}]{sup 3-} anions and Rb{sup +} and Ba{sup 2+} cations. The Ba{sup 2+} cations are surrounded by nine sulfur atoms forming distorted tricapped trigonal prisms, whereas the Rb{sup +} cations are in an irregular environment of ten sulfur atoms. The structure of K{sub 2}BaTa{sub 2}S{sub 11} (2) consists of two different dinuclear [Ta{sub 2}S{sub 11}] units which are separated by Ba{sup 2+} and K{sup +} ...

Energy Technology Data Exchange (ETDEWEB)

Background: Cu-diacetyl-bis(N{sup 4}-methylthiosemicarbazone) [Cu-ATSM], although excellent for oncology applications, may not be suitable for delineating cardiovascular or neurological hypoxia. For this reason, new Cu hypoxia positron emission tomography (PET) imaging agents are being examined to search for a higher selectivity for hypoxic or ischemic tissue at higher oxygen concentrations found in these tissues. Two approaches are to increase alkylation or to replace the sulfur atoms with selenium, resulting in the formation of selenosemicarbazones. Methods: Three {sup 64}Cu-labeled selenosemicarbazone complexes were synthesized and one was screened for hypoxia selectivity in vitro using EMT-6 mouse mammary carcinoma cells. Rodent biodistribution and small animal PET images were obtained from BALB/c mice implanted with EMT-6 tumors. One alkylated thiosemicarbazone was synthesized and examined. Results: Of the three bis(selenosemicarbazone) ligands synthesized and ...

International Nuclear Information System (INIS)

The aim of this work is to understand the reasons for the selectivity shown in the complexation by unsaturated heteropolyanions (HPA) of actinides (An) which are oxidized to the number +IV. Different studies have been carried out, both in solution and in solid state, on P_2W_1_7O_6_1"1"0"- and its complexes with Zn"2"+, UO_2"2"+, Ce"4"+, Th"4"+ and U"4"+ to characterize the nature of the complexation site offered to the cation. Among the actinides(IV), the U"4"+ ion has been selected due to its singular spectroscopic and magnetic properties. An initial series of studies, in solution, using NMR"3"1P has thus enabled us to characterize these complexes and to compare them to those formed with the complexing agent PW_1_1O_3_9"8"-. This body of data allows to identify an identical complexation site for both ligands. An analysis of the NMR"3"1P spectrum of U(P_2W_1_7O_6_1)_2"1"6"- has shown a plane of symmetry passing through the actinide and enables us to confirm the ...

Science.gov (United States)

Several examples of agonist-directed trafficking of receptor signalling at 5-HT2A and 5-HT2C receptors have been reported that involve independent downstream transduction pathways. We now report the functional selectivity of a series of chemically diverse agonists at human (h)5-HT2A, h5-HT2B and h5-HT2C-VSV by examining two related responses, the upstream activation of Gq/11 proteins in comparison with its associated cascade of calcium mobilisation. At the h5-HT2A receptor, d-lysergic acid diethylamide (LSD) and the antiparkinsonian agents lisuride, bromocriptine and pergolide exhibit a higher potency for Gq/11 activation than calcium release in contrast with all the other tested ligands such as 5-HT, mCPP and BW723C86, that show an opposite preference of signalling pathway. Comparable observations are made at h5-HT2B and h5-HT2C-VSV receptors, suggesting a similar mechanism of functional selectivity for the three serotonin receptors. Interestingly, the ...