WorldWideScience
1

Human placental transport of cimetidine.  

UK PubMed Central (United Kingdom)

This study addresses the mechanism of transport of the H2-receptor antagonist, cimetidine, by the human placenta. A 4-h recycling perfusion of a single placental cotyledon of normal, term, human placenta...Full Text Available

1987-11-01

2

Selective estrogen receptor modulator (SERM) for the treatment of osteoporosis in postmenopausal women: focus on lasofoxifene  

UK PubMed Central (United Kingdom)

Selective estrogen receptor modulators (SERMs) represent a class with a growing number of compounds that act as either estrogen receptor agonists or antagonists in a tissue-specific manner. This article...Full Text Available

2010-01-01

3

Construction of a novel bifunctional biogenic amine receptor by two point mutations of the H2-histamine receptor.  

UK PubMed Central (United Kingdom)

BACKGROUND: H2-histamine receptors mediate a wide range of physiological functions extending from stimulation of gastric acid secretion to induction of human promyelocyte differentiation. We have previously...Full Text Available

1995-03-01

4

Reduction of IgG in nonhuman primates by a peptide antagonist of the neonatal Fc receptor FcRn  

UK PubMed Central (United Kingdom)

The neonatal Fc receptor FcRn provides IgG molecules with their characteristically long half-lives in vivo by protecting them from intracellular catabolism and then returning them to...Full Text Available

2008-02-19

5

Novel Analogs and Stereoisomers of the Marine Toxin Neodysiherbaine with Specificity for Kainate Receptors  

UK PubMed Central (United Kingdom)

Antagonists for kainate receptors (KARs), a family of glutamate-gated ion channels, are efficacious in a number of animal models of neuropathologies, including epilepsy, migraine pain, and anxiety....Full Text Available

2008-02-01

6

Antidepressant-Like Effects of ?-Opioid Receptor Antagonists in Wistar Kyoto Rats  

UK PubMed Central (United Kingdom)

The Wistar Kyoto (WKY) rat strain is a putative genetic model of comorbid depression and anxiety. Previous research showing increased κ-opioid receptor (KOR)...Full Text Available

2010-02-01

7

Role of intrathecal tachykinins for micturition in unanaesthetized rats with and without bladder outlet obstruction.  

UK PubMed Central (United Kingdom)

1. The effects on micturition of RP 67,580, a selective NK1 receptor antagonist, and SR 48,968, a highly, potent antagonist at NK2 receptor sites, given intrathecally (i.t.) or intra-arterially (i.a.)...Full Text Available

1994-09-01

8

Design of a new serotonin receptor 5-HT_1_A imaging agent based on "9"9"mTc  

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 ...

2004-07-01

9

Characterization of a Novel Small Molecule Subtype Specific Estrogen-Related Receptor ? Antagonist in MCF-7 Breast Cancer Cells  

UK PubMed Central (United Kingdom)

BackgroundThe orphan nuclear receptor estrogen-related receptor α (ERRα) is a member of the nuclear receptor superfamily. It was identified through a search for genes...Full Text Available

10

Synthesis, structural activity-relationships, and biological evaluation of novel amide-based allosteric binding site antagonists in NR1A/NR2B N-methyl-d-aspartate receptors  

British Library Electronic Table of Contents (United Kingdom)

The synthesis and structure-activity relationship analysis of a novel class of amide-based biaryl NR2B-selective NMDA receptor antagonists are presented. Some of the studied compounds are potent, selective, non-competitive, and voltage-independent antagonists of NR2B-containing NMDA receptors. Like the founding member of this class of antagonists (ifenprodil), several interesting compounds of the series bind to the amino terminal domain of the NR2B subunit to inhibit function. Analogue potency is modulated by linker length, flexibility, and hydrogen bonding opportunities. However, unlike previously described classes of NR2B-selective NMDA antagonists that exhibit off-target activity at a variety of monoamine receptors, the compounds described herein show much diminished effects against the...

2009-01-01

11

Effects of the cannabinoid antagonist SR141716 (rimonabant) and d-amphetamine on palatable food and food pellet intake in non-human primates  

UK PubMed Central (United Kingdom)

The purpose of this study was to determine if a cannabinoid CB1 receptor antagonist would selectively decrease consumption of highly palatable food in non-human primates. The CB1...Full Text Available

2007-04-01

12

Dopamine D3 and D2 Receptor Mechanisms in the Abuse-Related Behavioral Effects of Cocaine: Studies with Preferential Antagonists in Squirrel Monkeys  

UK PubMed Central (United Kingdom)

Dopamine (DA) D3 and D2 receptor mechanisms are implicated in cocaine's abuse-related behavioral effects, but the relative contribution of the two receptor subtypes is only partially characterized....Full Text Available

2010-08-01

13

The stereospecificity of LY253352 for alpha 1-adrenoceptor binding sites in the brain and prostate.  

UK PubMed Central (United Kingdom)

1. The stereospecificity of the enantiomers of LY253352, a potent and selective alpha 1-adrenoceptor antagonist, were studied in the human prostate and canine brain using radioligand receptor binding...Full Text Available

1988-09-01

14

RU486 did not exacerbate cytokine release in mice challenged with LPS nor in db/db mice  

UK PubMed Central (United Kingdom)

BackgroundGlucocorticoids down-regulate cytokine synthesis and suppress inflammatory responses. The glucocorticoid receptor (GR) antagonist RU486 may exacerbate the inflammatory...Full Text Available

15

Pharmacokinetics and tolerability of zibotentan (ZD4054) in subjects with hepatic or renal impairment: two open-label comparative studies  

UK PubMed Central (United Kingdom)

BackgroundZibotentan (ZD4054) is a specific endothelin A (ETA) receptor antagonist being investigated for the treatment of prostate cancer. As zibotentan is eliminated...Full Text Available

16

Kinetic manifestation of cooperative interaction between quinuclidinyl benzilate and rat brain muscarine cholinoreceptors  

Energy Technology Data Exchange (ETDEWEB)

A study was made of the kinetics of L-(/sup 3/H)quinuclidinyl benzilate binding with membrane-bound muscarine cholinoreceptors from the rat brain. Determination was made of the rate constants of this process, and constants as a function of ligand concentration was investigated, indicating that there is a complex mechanism of interaction of antagonists with muscarine receptor. With up to 3.5 nM concentrations of L-(/sup 3/H)quinuclidinyl benzilate, the binding reaction occurs in two stages: rapid equilibrated binding is followed by a slow process of conformational isomerization of the receptor-ligand complex. At higher ligand concentrations, there is additional drastic increase in constant of rate of ligand binding a new plateau is reached. Such dependence of rate constant on ligand concentration is indicative of the cooperative nature of interaction between antagonists and muscarine ...

1985-01-01

17

Reinforcing Effects of ?-Receptor Agonists in Rats Trained to Self-Administer Cocaine  

UK PubMed Central (United Kingdom)

σ-Receptor (σR) antagonists have been reported to block certain effects of psychostimulant drugs. The present study examined the effects of σR ligands in rats trained to self-administer...Full Text Available

2010-02-01

18

Characterization of histamine H_1-receptor binding peptides in guinea pig brain using ["1"2"5I]iodoazidophenpyramine, an irreversible specific photoaffinity probe  

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 ...

19

In vitro assessment of the agonist properties of the novel 5-HT_1_A receptor ligand, CUMI-101 (MMP), in rat brain tissue  

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 ...

2011-02-01

20

Effects of the cannabinoid antagonist SR141716 (rimonabant) and d-amphetamine on palatable food and food pellet intake in non-human primates  

British Library Electronic Table of Contents (United Kingdom)

The purpose of this study was to determine if a cannabinoid CB1 receptor antagonist would selectively decrease consumption of highly palatable food in non-human primates. The CB1 receptor antagonist SR141716 (rimonabant; 0.12?1.0?mg/kg, i.m.) and the stimulant anorectic drug d-amphetamine (0.12?1.0?mg/kg, i.m.) were administered to non-food deprived baboons for the purpose of measuring the effect of each drug on consumption of the normal diet, and a large single meal of a high-carbohydrate candy. Four male and four female baboons had access to food 24?h each day, but they had to complete a two phase operant procedure in order to eat. Responding on one lever during a 30-min appetitive phase was required before animals could start a consumption phase, where responding on another lever led to...

2007-01-01

21

Blockade of catecholamine-induced growth by adrenergic and dopaminergic receptor antagonists in Escherichia coli O157:H7, Salmonella enterica and Yersinia enterocolitica  

UK PubMed Central (United Kingdom)

BackgroundThe ability of catecholamines to stimulate bacterial growth was first demonstrated just over a decade ago. Little is still known however, concerning the nature of the putative...Full Text Available

22

Developments of PET radioligands for NMDA receptors  

International Nuclear Information System (INIS)

Aim: There has been a great demand for developments of the radioligands to visualize the N-methyl-D-aspartate (NMDA) receptors by PET/SPECT. We have recently synthesized two C-11 labeled antagonists for the glycine-binding site on NMDA receptors. The aim of this work is to examine for their in vitro and in vivo binding characteristics, and to evaluate their potentials as PET radioligands for the NMDA receptors. Materials and methods: Two C-11 labeled 4-hydroxy-2-quinolones (1 and 2) were synthesized by conventional methylation of the corresponding phenols with ["1"1C]methyl iodide. In vitro and ex vivo quantitative autoradiographs with imaging plate, as well as animal PET, were employed in order to evaluate their in vitro and in vivo binding to the NMDA receptors. Results: The compound 1 showed the specific binding to rat brain slices with higher localization in the hippocampus and ...

2002-09-01

23

Characterization of the xanthine-binding site on R/sub a/ and R/sub i/ subtypes of the adenosine receptor  

Energy Technology Data Exchange (ETDEWEB)

Methylxanthines and their derivatives are antagonists at cell surface adenosine receptors. They report here a systematic study of xanthine structure-activity relationships which compares potency at two adenosine receptor subtypes, R/sub a/ and R/sub i/. Adenylate cyclase stimulation (R/sub a/ in platelet membranes) and inhibition (R/sub i/ in adipocyte membranes) were used as models of receptor activation. K/sub i/ values were obtained by Schild analysis. The orders of potency of the xanthines to attenuate the effects of adenosine analogues were similar to those previously reported. Earlier work utilizing radioligand binding (R/sub i/ and (/sup 3/H) cAMP formation (R/sub a/) claimed that IIX and PACPX are at least 10 and 400 fold, respectively, more potent at R/sub i/ than at R/sub a/. However, in their assays which utilize modulation of receptor-coupled adenylate cyclase, the ...

1986-05-01

24

The (--)(/sup 3/H)dihydroalprenolol binding to rat adipocyte membranes: an explanation of curvilinear Scatchard plots and implications for quantitation of beta-adrenergic sites  

Energy Technology Data Exchange (ETDEWEB)

In rat adipocyte membranes, both beta-adrenergic agonists and beta-adrenergic antagonists competed with (--)(/sup 3/H)dihydroalprenolol for high affinity (KD 2-4 nM) and low capacity binding sites. The antagonists but not the agonists competed with (--)(/sup 3/H)dihydroalprenolol for lower affinity and higher capacity sites. The present studies were performed in order to characterize the adipocyte beta-adrenergic receptor and distinguish it from low affinity, higher capacity sites which were heat-labile and not stereoselective. When isoproterenol was used to define the nonspecific binding, saturation studies showed a single binding site with a capacity of approximately 100 fmol/mg membrane protein (corresponding to approximately 50,000 sites/adipocyte). Binding was saturated by 10 nM (--)(/sup 3/H)dihydroalprenolol. Approximate KD's of 204 nM were observed. Kinetic analysis of (--)(/sup 3/H)dihydroalprenolol ...

1982-09-01

25

5'-Azido-[3,6-3H2]-1-napthylphthalamic acid, a photoactivatable probe for naphthylphthalamic acid receptor proteins from higher plants: identification of a 23-kDa protein from maize coleoptile plasma membranes.  

UK PubMed Central (United Kingdom)

1-Naphthylphthalamic acid (NPA) is a specific inhibitor of polar auxin transport that blocks carrier-mediated auxin efflux from plant cells. To allow identification of the NPA receptor thought to be...Full Text Available

1992-01-15

26

Short-term regulation of muscarinic acetylcholine receptors: An assessment utilizing mouse brain and mouse neuroblastoma cells  

Energy Technology Data Exchange (ETDEWEB)

The effects of muscarinic agonists and diisopropylfluorophosphate (DFP) on muscarinic receptor density and muscarinic receptor-mediated responses was assessed in mouse brain and mouse neuroblastoma cells (clone N1E-115). Utilizing the antagonist ({sup 3}H)quinuclidinyl benzilate (({sup 3}H)QNB), there was no difference in the maximal binding capacity (B{sub max}) or equilibrium dissociation constant (K{sub d}) between untreated and 24 hour DFP-treated mice. However, one administration of DFP produced a 24% and 33% decrease in B{sub max} measured by ({sup 3}H)N-methylscopolamine (({sup 3}H)NMS) after 18 and 24 hours which was rapidly reversible within 36 hours after DFP treatment. The loss of ({sup 3}H)NMS binding sites following acute DFP treatment was not accompanied by a change in a particular muscarinic receptor binding conformation. Furthermore, the magnitude of muscarinic ...

1988-01-01

27

New tools for human fat cell alpha-2A adrenoceptor characterization. Identification on membranes and on intact cells using the new antagonist (3H)RX821002  

Energy Technology Data Exchange (ETDEWEB)

The pharmacology of the alpha-2 adrenoceptor of the human adipocyte was improved by using some new alpha-2 antagonists from different chemical families (imidazolines, benzazepines and benzofuroquinolizines) in biological and binding assays. Moreover, investigations were also carried out to define the binding properties of a new imidazolinic antagonist, RX821002 (2-(2-methoxy-1,4-benzodioxan-2yl)-2-imidazoline), which could be a potential radioligand. (3H)RX821002 binding was very rapid and reversible. Saturation isotherms indicated that (3H)RX821002 labeled, with high affinity, a homogeneous population of noninteracting binding sites with a mean Kd of 0.98 +/- 0.05 nM (n = 6). The binding of (3H)RX821002 on the human fat cell alpha-2 adrenoceptor displayed a specificity which is strictly similar to that obtained with (3H)rauwolscine and which is classical for an alpha-2 A adrenoceptor. The binding parameters of (3H)RX821002 were compared with ...

1990-01-01

28

The structure of myostatin:follistatin 288: insights into receptor utilization and heparin binding  

Science.gov (United States)

Myostatin is a member of the transforming growth factor-{beta} (TGF-{beta}) family and a strong negative regulator of muscle growth. Here, we present the crystal structure of myostatin in complex with the antagonist follistatin 288 (Fst288). We find that the prehelix region of myostatin very closely resembles that of TGF-{beta} class members and that this region alone can be swapped into activin A to confer signalling through the non-canonical type I receptor Alk5. Furthermore, the N-terminal domain of Fst288 undergoes conformational rearrangements to bind myostatin and likely acts as a site of specificity for the antagonist. In addition, a unique continuous electropositive surface is created when myostatin binds Fst288, which significantly increases the affinity for heparin. This translates into stronger interactions with the cell surface and enhanced myostatin degradation in the presence of either Fst288 or Fst315. ...

2009-09-29

29

Anti-muscarinic actions of mitoxantrone in isolated heart muscles of guinea pigs.  

Science.gov (United States)

A hypotheses that mitoxantrone is a competitive antagonist at muscarinic cholinergic receptors was examined in guinea-pig hearts. In isolated left atrial muscle preparations, electrically paced at 2 Hz, the muscarinic agonist, carbachol, caused a concentration-dependent decrease in developed tension. Mitoxantrone caused a parallel right-ward shift of the concentration-response curve for carbachol. Schild plots for the effect of mitoxantrone on the carbachol concentration-response relationship were linear with a slope of 0.88 which was not significantly different from the unity. The right-ward shift of the carbachol concentration-response relationship by mitoxantrone significantly reversed after an additional incubation with a mitoxantrone-free solution, although the reversal was incomplete after a 2-h incubation in the mitoxantrone-free solution. Mitoxantrone caused a concentration-dependent displacement of specific [3H]quinuclidinyl benzilate ...

2000-10-27

30

Prosocial effects of nicotine and ethanol in adolescent rats through partially dissociable neurobehavioral mechanisms  

Science.gov (United States)

The widespread use of tobacco and alcohol among adolescents might be related to the ability of nicotine and ethanol to facilitate social interactions. To investigate the neurobehavioral mechanisms underlying the prosocial effects of nicotine and ethanol, we focused on social play behavior, the most characteristic social activity in adolescent rats. Social play behavior is rewarding, and it is modulated through opioid, cannabinoid and dopaminergic neurotransmission, which are also involved in the reinforcing properties of nicotine and ethanol. We found that nicotine and ethanol increased social play, without affecting locomotion or social exploration. Their effects depended on the level of social activity of the partner, and were comparable in familiar and unfamiliar environments. At doses that increased social play, nicotine and ethanol had no anxiolytic effects in the elevated plus-maze. By contrast, the prototypical anxiolytic drug diazepam reduced social play at doses that reduced ...

2009-08-05

31

Kinetics of in vivo binding of antagonist to muscarinic cholinergic receptor in the human heart studied by Positron Emission Tomography  

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 ...

1984-08-27

32

Kinetic analysis of transport and opioid receptor binding of ( sup 3 H)(-)-cyclofoxy in rat brain in vivo: Implications for human studies  

Energy Technology Data Exchange (ETDEWEB)

(3H)Cyclofoxy (CF: 17-cyclopropylmethyl-3,14-dihydroxy-4,5-alpha-epoxy-6-beta-fluoromorp hinan) is an opioid antagonist with affinity to both mu and kappa subtypes that was synthesized for quantitative evaluation of opioid receptor binding in vivo. Two sets of experiments in rats were analyzed. The first involved determining the metabolite-corrected blood concentration and tissue distribution of CF in brain 1 to 60 min after i.v. bolus injection. The second involved measuring brain washout for 15 to 120 s following intracarotid artery injection of CF. A physiologically based model and a classical compartmental pharmacokinetic model were compared. The models included different assumptions for transport across the blood-brain barrier (BBB); estimates of nonspecific tissue binding and specific binding to a single opiate receptor site were found to be essentially the same with both models. The nonspecific binding equilibrium ...

1991-03-01

33

Rapid inhibition of vasoconstriction in renal afferent arterioles by aldosterone  

DEFF Research Database (Denmark)

Aldosterone has been suggested to elicit vessel contraction via a nongenomic mechanism. We tested this proposal in microdissected, perfused rabbit renal afferent arterioles. Aldosterone had no effect on internal diameter in concentrations from 10(-10) to 10(-5) mol/L, but aldosterone abolished the ability of 100 mmol/L KCl to induce vascular contraction. The inhibitory effect of aldosterone was observed from 1 pmol/L. The inhibitory effect was significant after 5 minutes and maximal after 20 minutes and was fully reversible. Actinomycin D (10(-6) mol/L) prolonged the effect of aldosterone. The effect was abolished by the mineralocorticoid receptor antagonist spironolactone (10(-7) mol/L) but not by the glucocorticoid receptor antagonist mifepristone (10(-6) mol/L). The K+-mediated increase of intracellular calcium concentration in afferent arterioles was not affected by aldosterone. Mineralocorticoid ...

2003-01-01

35

Polymorphism in HTR3D shows different risks for acute chemotherapy-induced vomiting after anthracycline chemotherapy  

British Library Electronic Table of Contents (United Kingdom)

Aims: Serotonin (5-hydroxytryptamine 3; 5-HT3) receptors are involved in chemotherapy-induced nausea and vomiting (CINV), and 5-HT3 antagonists are part of the `gold standard' antiemetic treatment during chemotherapy. We investigated the correlation of common variants in 5-HT3 receptor subunit genes with the occurrence of CINV. Materials & methods: A total of 110 previously characterized chemotherapy-naive women with primary breast cancer treated with anthracycline-containing chemotherapy served as a study group for mutational analysis by direct sequencing. Eight common SNPs in the 5-HT3 receptor genes, HTR3A, HTR3B, HTR3D and HTR3E, were selected for association analysis. Results: A nonsynonymous variant in HTR3D, p.G36A (rs6443930), was found to be over-represented in nonresponders, assu...

2010-01-01

36

Development of gamma-emitting, receptor binding radiotracers for imaging the brain and pancreas  

Energy Technology Data Exchange (ETDEWEB)

This progress report covers period from Nov. 1, 1989 to Aug. 31, 1990. The long term objective was to develop receptor-binding radiotracers for SPECT or PET imaging of CNS or peripheral nervous system. The specific chemistry aims, as understood on the basis of past findings, were: to synthesize and develop a more polar analogs of 4IQNB, possessing similar binding characteristics but eliminated more rapidly from the surrounding tissues and the target organ, to design a method of introducing a technetium chelating group onto a molecule or cholinergic agent without drastic lowering of its apparent affinity, to synthesize and develop radiotracers based on m-AChR antagonists selective for one of the subtypes of the receptor. The chemistry service aims were to prepare and characterize (R,R)- and (R,S)-4IQNB and derivatives, to provide the triazene intermediate to other investigators, and to provide ({sup 123}I)4IQNB for in vivo ...

1990-01-01

37

The p75"N"T"R tumor suppressor induces cell cycle arrest facilitating caspase mediated apoptosis in prostate tumor cells  

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 ...

2006-03-24

38

Prostaglandin (PG) E3 synthesis elicted by adrenergic stimuli in guinea-pig trachea (GPT) is mediated primarily by B2 adrenergic receptors  

Science.gov (United States)

The purpose of this study was to examine arachidonic acid (AA) metabolism and to characterize the type of adrenergic receptor (AR) involved in the production of the major metabolite of this fatty acid. ({sup 14}C)AA was incubated with GPT-rings and the radiolabelled products were extracted and separated by TLC method. The medium was also assayed for radiolabelled immunoreactive PG's (iPG's) and leukotrienes (LT) B4 and C4 by RIA or Enzyme immunoassay (EIA) after exposure to various AR agonists. ({sup 14}C)AA was incorporated into GPT-rings and metabolized mainly into iPGE2 and smaller amounts into PGF2{alpha}. Trace amounts of PGD2 and 6-keto-PGF1{alpha} but not LTB4 or LTC4 were detected by RIA and/or EIA. Incubation of GPT rings for 15 minutes with isoproterenol and salbutamol resulted in a significant increase of PGE2 synthesis (optimum conc: 10{sup {minus}7}, 10{sup {minus}7}M respectively). In contrast, dobutamine, norepinephrine, ...

1990-02-26

39

Prostaglandin (PG) E3 synthesis elicted by adrenergic stimuli in guinea-pig trachea (GPT) is mediated primarily by B2 adrenergic receptors  

International Nuclear Information System (INIS)

The purpose of this study was to examine arachidonic acid (AA) metabolism and to characterize the type of adrenergic receptor (AR) involved in the production of the major metabolite of this fatty acid. ["1"4C]AA was incubated with GPT-rings and the radiolabelled products were extracted and separated by TLC method. The medium was also assayed for radiolabelled immunoreactive PG's (iPG's) and leukotrienes (LT) B4 and C4 by RIA or Enzyme immunoassay (EIA) after exposure to various AR agonists. ["1"4C]AA was incorporated into GPT-rings and metabolized mainly into iPGE2 and smaller amounts into PGF2#alpha#. Trace amounts of PGD2 and 6-keto-PGF1#alpha# but not LTB4 or LTC4 were detected by RIA and/or EIA. Incubation of GPT rings for 15 minutes with isoproterenol and salbutamol resulted in a significant increase of PGE2 synthesis (optimum conc: 10"-"7, 10"-"7M respectively). In contrast, dobutamine, norepinephrine, phenylnephrine and xylazine (up to 10"-"6M) did not ...

1991-04-21

40

Effect of systemic blockade of ?(1)-noradrenergic receptors on sex behavior and vaginal-cervical stimulation-induced Fos in female rats.  

Science.gov (United States)

It is hypothesized that systemic ??-noradrenergic antagonists may interfere with the transmission of sensory stimulation, particularly vaginal--cervical stimulation (VCS), which is crucial for reproductive functioning. To determine if ??-noradrenergic transmission receptor activity is necessary for transmission of sensory information important for VCS-dependent events, we conducted an experiment using prazosin, a ??-noradrenergic receptor antagonist. First, three doses of prazosin (1.0, 0.5 or 0.1 mg/kg) or the 10% ETOH in sesame oil vehicle were administered i.p. and sexual receptivity was assessed 30 min later in ovariectomized, hormone-treated female rats. The 1 mg/kg dose of prazosin significantly inhibited lordosis quotients and lordosis ratings. This dose of prazosin (1.0 mg/kg) was then administered 30 min prior to VCS or control scapular stimulation (CSS) and Fos-IR was examined in the ...

2010-10-01

41

Capsaicin-induced avoidance behavior in the terrestrial Gastropoda Megalobulimus abbreviatus: Evidence for TRPV-1 signaling and opioid modulation in response to chemical noxious stimuli  

British Library Electronic Table of Contents (United Kingdom)

The aim of this study was to measure the nociceptive response (avoidance latency) of the land snail Megalobulimus abbreviatus (N=8 in each group) after topical capsaicin exposure (0.1% and 0.5% in 20% ethanol) and to compare it to a well-studied stressful (50??C) thermal stimulus model. We also tested if ruthenium red, and capsazepine, respectively nonselective and selective TRPV1 receptor antagonists, could modify both capsaicin- and thermal-evoked responses. Finally, animals were pretreated with morphine, naloxone or morphine plus naloxone prior to capsaicin stimuli. Latencies were measured when the animal lifted its head?foot complex 1?cm from the substrate. Data were compared using ANOVA and LSD post hoc, and the Student T Test (pM. abbreviatus.

2007-01-01

42

cap alpha. -2 adrenergic receptor: a radiohistochemical study  

Energy Technology Data Exchange (ETDEWEB)

..cap alpha..-2 adrenergic agents have been shown to influence blood pressure, heart rate and other physiological and behavioral functions through interactions with adrenergic pathways within the central nervous system. Pharmacologically relevant ..cap alpha..-1 adrenergic receptors were biochemically characterized and radiohistochemically analyzed in intact tissue sections of the rat and human central nervous system. The anatomical distribution of the ..cap alpha..-2 receptors, labeled with the agonist (/sup 3/H)para-aminoclonidine, verified the concept that ..cap alpha..-2 receptors are closely associated with adrenergic nerve terminals and that ..cap alpha..-2 agents can influence autonomic and endocrine function through an action in the central nervous system. Since ..cap alpha..-2 agonists can influence sympathetic outflow, ..cap alpha..-2 binding sites were closely analyzed in the intermediolateral cell column of the ...

1984-01-01

43

CHRNA5 as negative regulator of nicotine signaling in normal and cancer bronchial cells: effects on motility, migration and p63 expression  

British Library Electronic Table of Contents (United Kingdom)

Genome-wide association studies have linked lung cancer risk with a region of chromosome 15q25.1 containing CHRNA3, CHRNA5 and CHRNB4 encoding a3, a5 and b4 subunits of nicotinic acetylcholine receptors (nAChR), respectively. One of the strongest associations was observed for a non-silent single-nucleotide polymorphism at codon 398 in CHRNA5. Here, we have used pharmacological (antagonists) or genetic (RNA interference) interventions to modulate the activity of CHRNA5 in non-transformed bronchial cells and in lung cancer cell lines. In both cell types, silencing CHRNA5 or inhibiting receptors containing nAChR a5 with a-conotoxin MII exerted a nicotine-like effect, with increased motility and invasiveness in vitro and increasing calcium influx. The effects on motility were enhanced by addit...

2011-01-01

44

Presentation of Type B Peptide-MHC Complexes from Hen Egg White Lysozyme by TLR Ligands and Type I IFNs Independent of H2-DM Regulation.  

Science.gov (United States)

In APCs, presentation by MHC II molecules of the chemically dominant peptide from the protein hen egg white lysozyme (HEL) generates different conformational isomers of the peptide-MHC II complexes (pMHC). Type B pMHCs are formed in early endosomes from exogenous peptides in the absence of H2-DM, whereas in contrast, type A pMHC complexes are formed from HEL protein in late vesicles after editing by H2-DM. Thus, H2-DM edits off the more unstable pMHC complexes, which are not presented from HEL. In this study, we show that type B pMHC complexes were presented from HEL protein only after stimulation of dendritic cells (DC) with TLR ligands or type I IFN. Type I IFN contributed to most TLR ligand-induced type B pMHC generation, as presentation decreased in DC lacking the receptor for type I IFNs (IFNAR1(-/-)). In contrast, presentation of type ...

2011-07-25

45

Effects of opioid peptides on thermoregulation  

Energy Technology Data Exchange (ETDEWEB)

In a given species, injected opioid peptides usually cause changes in temperature similar to those caused by nonpeptide opioids. The main effect in those species most studied, the cat, rat, and mouse, is an increase in the level about which body temperature is regulated; there is a coordinated change in the activity of thermoregulatory effectors such that hyperthermia is produced in both hot and cold environments. Larger doses may depress thermoregulation, thereby causing body temperature to decrease in the cold. Elicitation of different patterns of response over a range of environmental temperatures and studies with naloxone and naltrexone indicate that stimulation of a number of different receptors by both peptide and nonpeptide opioids can evoke thermoregulatory responses. ..beta..-Endorphin is readily antagonized by naloxone whereas methionine-enkephalin can act on naloxone-insensitive receptors. Moreover, synthetic peptide analogs do not ...

1981-11-01

46

B chain is a functional subunit of beta-bungarotoxin for inducing apoptotic death of human neuroblastoma SK-N-SH cells.  

Science.gov (United States)

beta-Bungarotoxin (beta-Bgt), a presynaptic phospholipase A(2) (PLA(2)) neurotoxin isolated from the venom of Bungarus multicinctus, consists of A chain and B chain. The goal of the present study is to explore the functional contribution of the two subunits to the toxicity of beta-Bgt. beta-Bgt was found to induce apoptotic death of SK-N-SH cells via elevating intracellular Ca(2+) and intracellular ROS production. Moreover, an activation of p38 MAPK was associated with the cytotoxicity of beta-Bgt. SB202190 (p38 MAPK inhibitor), N-acetylcysteine (antioxidant reagent), 1,2-bis(2-aminophenoxy)ethane-N,N,N,N-tetraacetic acid (BAPTA) (Ca(2+) chelator) and the inhibitors of Ca(2+) release from intracellular depots (ruthenium red and 2-aminoethoxydiphenyl borate) effectively attenuated the cytotoxicity of beta-Bgt. In sharp contrast to the inability of A chain, B chain was able to induce cytotoxic effects on SK-N-SH cells as beta-Bgt did. Abolishment of PLA(2) activity did not significantly ...

2007-10-13

47

Radiolabelled D2 agonists as prolactinoma imaging agents  

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 ...

1989-08-01

48

Nuclear Medicine Program progress report for quarter ending September 30, 1992  

Energy Technology Data Exchange (ETDEWEB)

The radioiodination and in vivo evaluation of p-iodocaramiphen a muscarinic antagonist which binds with high affinity to the M[sub 1] receptor subtype in vitro are described. Biodistribution studies in female Fischer rats demonstrated that [[sup 125]I]-piodocaraminphen had significant cerebral localization, but the uptake did not demonstrate specific uptake in those cerebral regions rich in muscarinic receptors, and radioactivity washed out rapidly from the brain. In addition there was no significant blockage of activity when the rats were preinjected with quinuclidinyl benzilate. These results suggest that p-iodocaramiphen is not a good candidate for the in vivo study of M[sub 1] muscarinic receptor populations by SPECT. Because of the widespread interest and expected importance of the availability of large amounts of tungsten-188 required for the tungsten-188/rhenium-188 generator systems, we have ...

1992-12-01

49

Selective metabolic stimulation of the subfornical organ and pituitary neural lobe by peripheral angiotensin II  

Energy Technology Data Exchange (ETDEWEB)

The subfornical organ is a major receptor area for one of the principal stimuli of thirst, the octapeptide, angiotensin II. In conscious water-sated rats, the authors examined the effects of intravenous infusion of angiotensin II on the rate of glucose utilization in the subfornical organ and in structures anatomically and functionally connected with it. Angiotensin II produced pressor and drinking responses and increased glucose utilization selectively in the subfornical organ and pituitary neural lobe and in no other brain structure. Treatment with the angiotensin II antagonist, sar1-leu8-angiotensin II, before intravenous administration of angiotensin II prevented metabolic stimulation of the subfornical organ and neural lobe. Captopril, an inhibitor of angiotensin-converting enzyme, reduced subfornical organ glucose metabolism to a level similar to that found in control animals. These results demonstrate that peripheral angiotensin II ...

1985-01-01

50

Protracted ethanol withdrawal in rats: Tolerance to the anxiolytic effects of diazepam and pentobarbital but not phenobarbital  

Science.gov (United States)

Anxiety is a common symptom during ethanol withdrawal contributing to its continuous abuse and alcoholism. Ethanol withdrawal in rats produces an interoceptive discriminative stimulus (IDS) similar to that produced by the anxiogenic drug pentylenetetrazol (PTZ). This stimulus peaks at 12 hours after last dose of ethanol and thereafter the IDS is detected for several days (protracted withdrawal) by sensitization to a probe drug. previously, the authors have shown that during the protracted withdrawal, the IDS is enhanced by GABA receptor antagonists suggesting alteration of brain GABA systems. This report provides further evidence that chronic ethanol alters GABAergic systems. Rats were trained to discriminate PTZ (20 mg/kg, ip) from saline. Diazepam, pentobarbital and phenobarbital blocked the PTZ-IDS dose dependently. Ethanol, 4.5% w/v, was then given in a nutritionally complete diet for a week. On termination of the ethanol diet, rats ...

1990-02-26

51

Ophidian envenomation strategies and the role of purines.  

Science.gov (United States)

Snake envenomation employs three well integrated strategies: prey immobilization via hypotension, prey immobilization via paralysis, and prey digestion. Purines (adenosine, guanosine and inosine) evidently play a central role in the envenomation strategies of most advanced snakes. Purines constitute the perfect multifunctional toxins, participating simultaneously in all three envenomation strategies. Because they are endogenous regulatory compounds in all vertebrates, it is impossible for any prey organism to develop resistance to them. Purine generation from endogenous precursors in the prey explains the presence of many hitherto unexplained enzyme activities in snake venoms: 5'-nucleotidase, endonucleases (including ribonuclease), phosphodiesterase, ATPase, ADPase, phosphomonoesterase, and NADase. Phospholipases A(2), cytotoxins, myotoxins, and heparinase also participate in purine liberation, in addition to their better known functions. Adenosine contributes to prey immobilization ...

2002-04-01

52

Studies on the mechanism of action of enterotoxin-induced fluid secretion in the gut  

International Nuclear Information System (INIS)

The mechanism of action of Clostridium difficile enterotoxin A (CA), of Escherichia coli enterotoxin (STa) and of cholera toxin (CT), which are known to cause severe diarrhea, were studied in a preparation of ligated jejunal loops of anesthetized rats in vivo. The toxins were administered intraluminally. Pharmacological agents, which were tested for their potency to influence toxin-related effects, were administered subcutaneously. Net fluid transport was determined gravimetrically, prostaglandin (PG) E_2-output into the lumen, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) contents in the mucosa were measured by radioimmunoassay, serotonin-(5-HT)-output into the lumen was determined by high performance liquid chromatography. The histopathological effects of CA and CT were examined by light- and scanning electron microscopy. All three toxins caused net fluid secretion (FS). 5-HT_2-(ketanserin) and 5-HT_3-receptor ...

1992-01-01

53

Structure-activity relationships of anthraquinones on the suppression of DNA-binding activity of the aryl hydrocarbon receptor induced by 2,3,7,8-tetrachlorodibenzo-p-dioxin.  

Science.gov (United States)

Anthraquinones are widely present in plant kingdom, and clinically used as laxatives. Environmental contaminants, dioxins, develop various adverse effects through transformation of a cytosolic aryl hydrocarbon receptor (AhR). We investigated the effects of 18 anthraquinones and 7 of their structurally related compounds on transformation of the AhR estimated by its DNA-binding activity in the cell-free system. 1,4-Dihydroxyanthraquinone (quinizarin), 1,5-dihydroxyanthraquinone (anthrarufin), 1,8-dihydroxyanthraquinone (danthron), and 5-hydroxy-1,4-naphthoquinone (juglone) strongly suppressed DNA-binding activity of the AhR induced by 0.1 nM 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), with their IC(50) values around 1 muM. On the other hand, anthraquinone, 2,6-dihydroxyanthraquinone (anthraflavic acid), and 2-hydroxy-1,4-naphthalendione (lawsone) showed moderate effects. Quantitative structure-activity relationships analysis demonstrated that hydroxyl groups at C1 or ...

2009-03-01

54

Succession of Indigenous Pseudomonas spp. and Actinomycetes on Barley Roots Affected by the Antagonistic Strain Pseudomonas fluorescens DR54 and the Fungicide Imazalil  

UK PubMed Central (United Kingdom)

In recent years, the interest in the use of bacteria for biological control of plant-pathogenic fungi has increased. We studied the possible side effects of coating barley seeds with the antagonistic...Full Text Available

2001-03-01

57

Disruption of contact inhibition in rat liver epithelial cells by various types of AhR ligands  

Energy Technology Data Exchange (ETDEWEB)

The maintenance of a balance between cell gain and cell loss is essential for proper liver function. The exact role of aryl hydrocarbon receptor (AhR) in regulating cell proliferation and apoptosis of liver cells remains unclear, since ligand-dependent activation of AhR has been shown to induce cell cycle arrest, proliferation, differentiation or apoptosis, depending on the cellular model used. AhR can directly interact with retinoblastoma protein in hepatic cells, forming protein complexes that can efficiently block cell cycle progression by inducing G1 arrest, or to induce the expression of inhibitors of cyclin-dependent kinases, such as p271. On the other hand, it has been suggested that AhR could play a stimulatory role in cell proliferation, either directly or by mediating a release from contact inhibition. It is now generally accepted that progenitor cells exist in the liver, are activated in various liver diseases and can form a potential target cell ...

2004-09-15

58

Radioiodination of 3-quinuclidinyl benzilate using a no-carrier-added concentration of iodine-125/sodium-iodine  

Energy Technology Data Exchange (ETDEWEB)

3-Quinuclidinyl benzilate (QNB) is a potent muscarinic antagonist that binds to muscarinic acetylcholine receptors. Iodination of QNB is difficult because it contains rings that are deactivated, while phenol rings are activated. The purpose of this research is to develop an appropriate method for the iodination of QNB at no-carrier-added concentrations of /sup 125/I/NaI. Phenol was chose as the test compound for direct iodination by adding chloramine T and nonradioactive sodium iodide to the phenol in a phosphate buffer and methanol system. A simple method to radioiodinate QNB at several concentrations was developed in situ in the presence of QNB, thallic trifluoroacetate /sup 125/I/NaI, /sup 127/I/NaI, and aluminium chloride. Using milligram amounts of QNB (7.12 x 10/sup -6/ moles), three reaction steps were involved: QNB was reacted with thallic trifluoroacetate at 60/sup 0/C for 24 hours, then radioactive /sup 125/I/NaI and aluminium ...

1986-01-01

59

Involvement of a glutamergic mechanism in gamma-dendrotoxin-induced hippocampal neuronal cell loss in the rat.  

Science.gov (United States)

The epileptogenic and neurodegenerative effects of gamma-dendrotoxin, from Dendroaspis angusticeps, a specific blocker of a non-inactivating, voltage-sensitive K+ channel, were studied after focal injection into one dorsal hippocampus in rats pretreated with CGP040116, a N-methyl-D-aspartate (NMDA) receptor antagonist, and in rats bearing a monolateral surgical lesion of the Schaffer collaterals whose terminals originate from CA3 pyramids and release glutamate in the CA1 hippocampal area. Administration of 35 pmol gamma-dendrotoxin elicited in all of the treated animals (n=8) bilateral EEG discharges and damage to the hippocampal formation. Quantitation of the damage revealed significant bilateral neuronal cell loss in the CA1, CA3 and CA4 pyramidal cell layers. The lowest dose (0.35 pmol; n=4) of the toxin used did not affect EEG activity and failed to cause significant hippocampal cell loss whereas the 3.5 pmol (n=6) dose caused EEG seizures ...

2004-03-01

60

Transformation of Verapamil by Cunninghamella blakesleeana  

UK PubMed Central (United Kingdom)

A filamentous fungus, Cunninghamella blakesleeana AS 3.153, was used as a microbial model of mammalian metabolism to transform verapamil, a calcium channel antagonist. The metabolites...Full Text Available

2004-05-01

61

Theoretical and practical considerations on the problem of metal--metal interaction.  

UK PubMed Central (United Kingdom)

The interaction between two metals, which can be either synergistic or antagonistic, implies that the behavior of one is changed by the presence of the other. Possible mechanisms of these interactions,...Full Text Available

1978-08-01

62

TNF-alpha antagonist therapy modify the tuberculin skin test response  

British Library Electronic Table of Contents (United Kingdom)

Tumour necrosis factor-alpha (TNF-?) antagonist drugs have been associated with increased risk of tuberculosis (TB). Tuberculin skin test (TST) is the most frequently used tool for identification of latent TB infection. We herein aimed to analyse the effect of TNF-? antagonists on the TST responses in a prospective study. The study group consisted of 182 patients (99 female, 83 male) who received TNF-? antagonists for various rheumatic disorders. All patients were evaluated with TST along with other parameters on the day of referral and on the 12th month visit. For those patients with a response of <5?mm induration at the initial evaluation, the TST was repeated to observe the booster effect. Out of 182 patients, 87 patients (48%) had a negative (0?4?mm) and 95 (52%) had a positive (?5?mm)...

2011-01-01

63

Regulation of Senescence in Cancer and Aging  

UK PubMed Central (United Kingdom)

Senescence is regarded as a physiological response of cells to stress, including telomere dysfunction, aberrant oncogenic activation, DNA damage, and oxidative stress. This stress response has an antagonistically...Full Text Available

64

Synthesis and PET imaging of the benzodiazepine receptor tracer [N-methyl-"1"1C]iomazenil  

International Nuclear Information System (INIS)

The central benzodiazepine receptor tracer [N-methyl-"1"1C]iomazenil (Ro 16-0154) was synthesized by alkylation of the desmethyl precursor noriomazenil with ["1"1C]methyl iodide. The ["1"1C]CH_3I (prepared by reduction of ["1"1C]CO_2 with LiAlH_4 followed by reaction with HI) was reacted with noriomazenil inN,N -dimethylformamide and Bu_4N"+OH"- for 1 min at 80 deg. C and purified by HPLC (C_1_8, 34% CH_3CN/H_2O, 7 mL/min). The product was obtained with synthesis time 35 #+-# 5 min (mean #+-# SD, n = 7), radiochemical yield (EOB) 36 #+-# 16%, radiochemical purity 99 #+-# 1%, and specific activity 5100 #+-# 2800 mCi/#mu#mol. Absorbed radiation doses were calculated from previously acquired human biodistribution data. The urinary bladder wall received the highest dose (0.099 mGy/MBq) for 4.8 h voiding interval and the effective dose equivalent was 0.015 mSv/MBq. After i.v. injection of ["1"1C]iomazenil in an adult baboon or ...

1995-07-01

65

?H2AX and cancer  

UK PubMed Central (United Kingdom)

Histone H2AX phosphorylation on a serine four residues from the carboxyl terminus (producing γH2AX) is a sensitive marker for DNA double-strand breaks (DSBs). DSBs may lead to cancer...Full Text Available

2008-12-01

66

The structure of receptor-associated protein (RAP)  

UK PubMed Central (United Kingdom)

The receptor-associated protein (RAP) is a molecular chaperone that binds tightly to certain newly synthesized LDL receptor family members in the endoplasmic reticulum (ER) and facilitates their delivery...Full Text Available

2007-08-01

67

Structure and function of an acetylcholine receptor.  

UK PubMed Central (United Kingdom)

Structural analysis of an acetylcholine receptor from Torpedo californica leads to a three-dimensional model in which a "monomeric" receptor is shown to contain subunits arranged around a central ionophoretic...Full Text Available

1982-01-01

68

Orphan GPCR research  

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

2008-03-01

69

Bioengineered bugs expressing oligosaccharide receptor mimics  

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

2010-05-01

70

AMPA-receptor trafficking and injury-induced cell death  

UK PubMed Central (United Kingdom)

AMPA receptors (AMPARs) are critical for synaptic plasticity, and are subject to alterations based on subunit composition and receptor trafficking to and from the plasma membrane. One of the...Full Text Available

2010-07-01

71

Prolonged signaling at the parathyroid hormone receptor by peptide ligands targeted to a specific receptor conformation  

UK PubMed Central (United Kingdom)

The parathyroid hormone receptor (PTHR) is a class B G protein-coupled receptor that plays critical roles in bone and mineral ion metabolism. Ligand binding to the PTHR involves interactions to both...Full Text Available

2008-10-28

72

Leptin receptor gene expression and number in the brain are regulated by leptin level and nutritional status  

UK PubMed Central (United Kingdom)

Hormone potency depends on receptor availability, regulated via gene expression and receptor trafficking. To ascertain how central leptin receptors are regulated, the effects of leptin challenge, high-fat...Full Text Available

2009-07-15

73

Intracellular delivery of an antisense?oligonucleotide via endocytosis of a G protein-coupled receptor  

UK PubMed Central (United Kingdom)

Gastrin-releasing peptide receptor (GRPR), a member of the G protein-coupled receptor superfamily, has been utilized for receptor-mediated targeting of imaging and therapeutic agents; here we extend...Full Text Available

2010-10-01

75

Agonist-dependent up-regulation of thyrotrophin-releasing hormone receptor protein.  

UK PubMed Central (United Kingdom)

To study the effect of agonist on the TRH (thyrotrophin-releasing hormone) receptor protein, an epitope-tagged receptor was stably expressed in HEK-293 cells (human embryonic kidney 293 cells) and receptor...Full Text Available

2004-06-15

77

A randomized trial of microdose leuprolide acetate protocol versus luteal phase ganirelix protocol in predicted poor responders  

British Library Electronic Table of Contents (United Kingdom)

We performed a randomized trial to compare IVF outcomes in 54 poor responder patients undergoing a microdose leuprolide acetate (LA) protocol or a GnRH antagonist protocol incorporating a luteal phase E2 patch and GnRH antagonist in the preceding menstrual cycle. Cancellation rates, number of oocytes retrieved, clinical pregnancy rates (PR), and ongoing PRs were similar between the two groups.

2011-01-01

78

Electronic energy bands and optical properties of LaH"2 and NdH"2  

International Nuclear Information System (INIS)

Electronic energy bands of LaH"2 and NdH"2 have been calculated by the composite-wave variational version of the augmented plane wave method. Crystal potentials for both the hydrides were constructed by the superposition of the atomic potentials of Herman and Skillman. From the band structure data, density of states, joint density of states, optical absorption spectra and Fermi surfaces of these two hydrides have been calculated. The results of the optical studies have been successfully compared with the experimental results of Weaver et al. From the theoretical point of view the present results for LaH"2 have been satisfactorily compared with the results of Gupta et al. Since no theoretical calculation exists for ndH"2, theoretical comparison, in this case, was not possible for ...

79

Coordination lanthanide compounds with thiosemicarbazide diacetic acid  

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.

80

In vitro competitive adhesion and production of antagonistic compounds by lactic acid bacteria against fish pathogens  

British Library Electronic Table of Contents (United Kingdom)

The present study describes the screening of five lactic acid bacteria (LAB) for use as probiotics based on their competitive adhesion and production of antagonistic substances against some fish pathogens. A reduction of adhesion of all pathogenic strains tested was obtained with three of the LAB strains (Lactococcus lactis subsp. lactis CLFP100, Lactococcus lactis subsp. cremoris CLFP102 and Lactobacillus curvatus CLFP150). With the exception of fish pathogens Flavobacterium psychrophilum and Renibacterium salmoninarum that were not inhibited by LAB strains, production of antagonistic compounds by all tested LAB was observed against at least one of the indicator strains. Based on mucus adhesion, competitive exclusion, and suppression of fish pathogen growth, the selected LAB strains can b...

2007-01-01

81

Study of the susceptibility of an austenitic stainless steel stabilized with niobium to stress corrosion damage in a H_2S medium (SSC) and to intergranular corrosion (IGC) in other aggressive environments  

International Nuclear Information System (INIS)

Behavior to hydrogen damage caused by stress corrosion in a H_2S medium (SSC) and to intergranular corrosion (IGC) in different mediums, such as oxalic acid (C_2H_2.2H_2O), iron sulphate-50% sulfuric acid (Fe_2(SO_4)_3-50% H_2SO_4), nitric acid (HNO_3), copper sulphate-16% sulfuric acid (CuSO_4.5H_2O-16% H_2SO_4) and cooper sulphate-50% sulfuric acid (CuSO_4.5H_2O-50% H_2SO_4), is studied in an AISI 347 austenitic stainless steel stabilized with 0.61 mass % Nb and hot rolled to a seamless pipe with 273.1 mm in diameter and 18.2 mm in thickness. (Author) 12 refs.

1998-01-01

82

Modulation of Retinoic Acid Receptor-related Orphan Receptor ? and ? Activity by 7-Oxygenated Sterol Ligands*  

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

2010-02-12

83

Gastrin releasing peptide (GRP) receptor targeted radiopharmaceuticals: A concise update  

Energy Technology Data Exchange (ETDEWEB)

The gastrin releasing peptide (GRP) receptor is becoming an increasingly attractive target for development of new radiolabeled peptides with diagnostic and therapeutic potential. The attractiveness of the GRP receptor as a target is based upon the functional expression of GRP receptors in several tumors of neuroendocrine origin including prostate, breast, and small cell lung cancer. This concise review outlines some of the efforts currently underway to develop new GRP receptor specific radiopharmaceuticals by employing a variety of radiometal chelation systems.

2003-11-01

84

Progressive ratio performance following challenge with antipsychotics, amphetamine, or NMDA antagonists in adult rats treated perinatally with phencyclidine  

UK PubMed Central (United Kingdom)

RationalePrevious research has shown that rats exposed perinatally to phencyclidine (PCP) exhibited neuroanatomical abnormalities and altered cognition. In addition...Full Text Available

2004-12-01

86

Micturition in conscious rats with and without bladder outlet obstruction: role of spinal alpha 1-adrenoceptors.  

UK PubMed Central (United Kingdom)

1. In normal rats and rats with bladder hypertrophy secondary to outflow obstruction, undergoing continuous cytometry, we examined the responses to the selective alpha 1-adrenoceptor antagonist doxazosin...Full Text Available

1996-03-01

87

Effects of a growth hormone-releasing hormone antagonist on telomerase activity, oxidative stress, longevity, and aging in mice  

UK PubMed Central (United Kingdom)

Both deficiency and excess of growth hormone (GH) are associated with increased mortality and morbidity. GH replacement in otherwise healthy subjects leads to complications, whereas individuals with...Full Text Available

2010-12-21

88

Cardiovascular Safety of Degarelix: Results From a 12-Month, Comparative, Randomized, Open Label, Parallel Group Phase III Trial in Patients With Prostate Cancer  

UK PubMed Central (United Kingdom)

PurposeWe assessed the cardiovascular safety profile of degarelix, a new gonadotropin-releasing hormone antagonist.Materials...Full Text Available

2010-12-01

89

Brg1 Is Required for Cdx2-Mediated Repression of Oct4 Expression in Mouse Blastocysts  

UK PubMed Central (United Kingdom)

During blastocyst formation the segregation of the inner cell mass (ICM) and trophectoderm is governed by the mutually antagonistic effects of the transcription factors Oct4 and Cdx2. Evidence indicates...Full Text Available

90

Antagonistic crosstalk between APC and HIF-1?  

UK PubMed Central (United Kingdom)

Most colorectal cancers have mutations in the tumor suppressor APC. The best-understood function of APC is its participation in a protein complex that regulates the availability of β-catenin....Full Text Available

2011-05-15

91

Antagonistic Gcn5-Hda1 interactions revealed by mutations to the Anaphase Promoting Complex in yeast  

UK PubMed Central (United Kingdom)

BackgroundHistone post-translational modifications are critical for gene expression and cell viability. A broad spectrum of histone lysine residues have been identified in yeast...Full Text Available

92

Antagonist HIV-1 Gag Peptides Induce Structural Changes in HLA B8  

UK PubMed Central (United Kingdom)

In the cellular immune response, recognition by CTL-TCRs of viral antigens presented as peptides by HLA class I molecules, triggers destruction of the virally infected cell (Townsend, A.R.M., J. Rothbard,...Full Text Available

1996-12-01

93

Adenomatous Polyposis Coli and Hypoxia-inducible Factor-1? Have an Antagonistic Connection  

UK PubMed Central (United Kingdom)

The tumor suppressor adenomatous polyposis coli (APC) is mutated in the majority of colorectal cancers and is best known for its role as a scaffold in a Wnt-regulated protein complex that determines...Full Text Available

2010-11-01

94

A population pharmacokinetic meta-analysis of maraviroc in healthy volunteers and asymptomatic HIV-infected subjects  

UK PubMed Central (United Kingdom)

AimsTo develop a population pharmacokinetic model for maraviroc, a noncompetitive CCR5 antagonist, after oral administration of tablets to healthy volunteers and asymptomatic HIV-infected...Full Text Available

2008-04-01

95

The Pregnane X Receptor: From Bench to Bedside  

UK PubMed Central (United Kingdom)

BackgroundThe pregnane X receptor (PXR; NR1I2), a member of the nuclear receptor superfamily, regulates the expression of metabolic enzymes and transporters involved...Full Text Available

2008-07-01

96

Surface structure recognized for covalent modification of the aspartate receptor in chemotaxis.  

UK PubMed Central (United Kingdom)

The aspartate receptor involved in chemotaxis is modified by methyl esterification at four distinct glutamate residues during the adaptive response of this receptor. To explain the high degree of specificity...Full Text Available

1986-09-01

97

Receptor Binding Sites and Antigenic Epitopes on the Fiber Knob of Human Adenovirus Serotype 3  

UK PubMed Central (United Kingdom)

The adenovirus fiber knob causes the first step in the interaction of adenovirus with cell membrane receptors. To obtain information on the receptor binding site(s), the interaction of labeled cell...Full Text Available

1998-11-01

98

Lineage-specific co-evolution of the Egf receptor/ligand signaling system  

UK PubMed Central (United Kingdom)

BackgroundThe epidermal growth factor receptor (Egfr) with its numerous ligands has fundamental roles in development, cell differentiation and physiology. Dysfunction of the receptor-ligand...Full Text Available

99

Involvement of the chemokine-like receptor GPR33 in innate immunity?  

UK PubMed Central (United Kingdom)

Chemokine receptors control leukocyte chemotaxis and cell-cell communication but have also been associated with pathogen entry. GPR33, an orphan member of the chemokine-like receptor family,...Full Text Available

2010-05-28

100

Influence of atrial stretch receptors on hypothalamic neurosecretory neurones.  

UK PubMed Central (United Kingdom)

1. The effects of stimulation of atrial receptors on hypothalamic neurosecretory cells were investigated in anaesthetized dogs and cats. Atrial receptors were activated by stretching the left and the...Full Text Available

1978-12-01

101

In vitro selection of RNA molecules that displace cocaine from the membrane-bound nicotinic acetylcholine receptor  

UK PubMed Central (United Kingdom)

The nicotinic acetylcholine receptor (AChR) controls signal transmission between cells in the nervous system. Abused drugs such as cocaine inhibit this receptor. Transient kinetic investigations indicate...Full Text Available

1998-11-24

102

Immunoglobulins in myasthenia gravis. Kinetic properties of the acetylcholine-receptor antibody studied during lymph drainage.  

UK PubMed Central (United Kingdom)

A specific immunoglobulin, the receptor antibody, can be found in most patients with myasthenia gravis. In order to study the kinetic properties of this antibody, serial determinations of receptor antibody,...Full Text Available

1978-10-01

103

Hormone Receptor Status in Breast Cancer and its Relation to Age and Other Prognostic Factors  

UK PubMed Central (United Kingdom)

Background:Increasing evidence shows the importance of young age, estrogen receptor (ER), progesterone receptor (PR) status, and HER-2 expression in patients with breast cancers.Patients...Full Text Available

104

Continuous monitoring of receptor-mediated changes in the metabolic rates of living cells.  

UK PubMed Central (United Kingdom)

Activation of beta-adrenergic or muscarinic acetylcholine receptors expressed in transfected cells or epidermal growth factor receptors in human keratinocytes produces 15% to 200% changes in cellular...Full Text Available

1990-05-01

105

Changes in Androgen Receptor, Estrogen Receptor alpha, and Sexual Behavior with Aging and Testosterone in Male Rats1  

UK PubMed Central (United Kingdom)

Reproductive aging in males is characterized by a diminution in sexual behavior beginning in middle age. We investigated the relationships among testosterone, androgen receptor (AR) and estrogen...Full Text Available

2010-07-01

106

A Hot New Twist to Hair Biology  

UK PubMed Central (United Kingdom)

The vanilloid receptor-1 (VR1, or transient receptor potential vanilloid-1 receptor, TRPV1) is activated by capsaicin, the key ingredient of hot peppers. TRPV1 was originally described on sensory neurons...Full Text Available

2005-04-01

107

2-[(4-MepyH)2]2+ - GLTRS - NASA  

Science.gov (United States)

Synthesis and Structural Characterization of a Novel Indium Mercapto Derivative [Clln(SCH2(CO)O)2]2-[(4-MepyH)2]2+. AUTHOR(S): ...

108

Rapidly adapting receptors in a rabbit model of mitral regurgitation  

UK PubMed Central (United Kingdom)

Unlike in normal rabbits, pulmonary rapidly adapting receptors (RARs) in rabbits with chronic mitral regurgitation (MR) do not respond to small changes in extravascular...Full Text Available

1999-12-15

109

New Developments in the Use of Histamine and Histamine Receptors  

UK PubMed Central (United Kingdom)

Histamine and the histamine receptors are important regulators of a plethora of biological processes, including immediate hypersensitivity reactions and acid secretion in the stomach. In these...Full Text Available

2011-04-01

110

Anesthetic stimulation of insect water receptors.  

UK PubMed Central (United Kingdom)

Halothane, chloroform, and carbon tetrachloride, in the vapor and liquid phases, stimulate the water receptor of the blowfly Phormia regina. There are three successive phases of response to long-lasting...Full Text Available

1976-09-01

112

Molar extinction coefficients in aqueous solutions of some alkaline earth chlorides  

International Nuclear Information System (INIS)

Molar extinction coefficients for the solid solutes in aqueous solutions of some alkaline earth chlorides such as MgCl_2.6H_2O, CaCl_2, SrCl_2.6H_2O and BaCl_2.2H_2O have been determined at 81, 356, 511, 662, 1173 and 1332 keV energies in different concentration using the narrow beam transmission methods. (author)

1999-12-21

113

Application of 'waste' wood-shaving bottom ash for adsorption of azo reactive dye.  

Science.gov (United States)

The utilization of wood-shaving bottom ash (WBA) for the removal of Red Reactive 141 (RR141), an azo reactive dye, was investigated. WBA/H(2)O and WBA/H(2)SO(4) were made by treating WBA with water and 0.1M H(2)SO(4), respectively, to increase adsorption capacity. Adsorption of RR141 from reactive dye solution (RDS) and reactive dye wastewater (RDW) by WBA/H(2)O and WBA/H(2)SO(4) involved the BET surface area and pore size diameter. Properties of adsorbents, effect of contact time, initial pH of solution, dissolved metals and elution studies indicated that the decolorisation mechanism involved both chemical adsorption and precipitation with calcium ions. In addition, the WBA/H(2)SO(4) surface might contain sulphate-cation complexes that ...

2008-04-23

114

Spectral investigation of primary uranyl orthophosphate  

International Nuclear Information System (INIS)

By methods of vibrational (infrared, Raman) and PMR spectroscopy, crystallohydrate forms of monosubstituted uranyl orthophosphate have been examined. The vibrational frequencies of the groupings from the compounds were identified. The existence of non-equivalent H_2PO_4"--groups in the substances under investigation was ascertained. It has been suggested that one of them is a bridged group, and the other is the end group. A fragment of the VO_2(H_2PO_4)_2 hydrate structure is given, its main constituents being uranylphosphate chains. The analysis of water vibrations assumes coordination of one mole of H_2O in VO_2(H_2PO_4)_2:3H_2O to uranium, while two other molecules are only hydrogen-bonded with phosphate anions. Absorption within the region of 2100-2550 cm"-"1 is assigned to ...

115

A Computer Simulation of the Electronic Structure of Leucine in Aqueous Solution  

British Library Electronic Table of Contents (United Kingdom)

In order to obtain the electronic structure of leucine (Leu) in aqueous solution, we studied three systems: Leu+7H2O, Leu+8H2O and Leu+9H2O. The results indicated that the system Leu+8H2O was the only choice which was both acceptable and doable: its computational effort was affordable, and it could simulate a main part of the solvent effect on the electronic structure of Leu in solution. Based on the system Leu+8H2O, all-electron, ab initio calculations were performed to construct an equivalent potential of water for the electronic structure of Leu with dipoles. The results showed that the main effect of water on the electronic structure of Leu was raising the occupied states about 0.0824 Ry on average, and broadening the energy gap by 11%. The water effect on the electronic ...

2011-01-01

116

Solar syngas production from CO"2 and H"2O in a two-step thermochemical cycle via Zn/ZnO redox reactions: Thermodynamic cycle analysis  

British Library Electronic Table of Contents (United Kingdom)

Solar syngas production from CO"2 and H"2O is considered in a two-step thermochemical cycle via Zn/ZnO redox reactions, encompassing: 1) the ZnO thermolysis to Zn and O"2 using concentrated solar radiation as the source of process heat, and 2) Zn reacting with mixtures of H"2O and CO"2 yielding high-quality syngas (mainly H"2 and CO) and ZnO; the ZnO is recycled to the first, solar step, resulting in net reaction @bCO"2 + (1 - @b)H"2O -> @bCO + (1 - @b)H"2. Syngas is further processed to liquid hydrocarbon fuels via Fischer-Tropsch or other catalytic processes. Second-law thermodynamic analysis is applied to determine the cycle efficiencies attainable with and without heat recuperation for varying molar fractions of CO"2:H"2O and solar ...

2011-01-01

117

H2/Ar and vacuum annealing effect of ZnO thin films deposited by RF magnetron sputtering system  

British Library Electronic Table of Contents (United Kingdom)

The properties of ZnO films were investigated as functions of annealing temperatures in H2/Ar and vacuum. The resistivities and mobilities of ZnO films decreased with increase of annealing temperatures in vacuum and H2/Ar ambients. However, the carrier densities of ZnO films increased with increase of annealing temperatures in vacuum and H2/Ar ambients. The resistivities of ZnO2 films annealed at 300degreeC were 2186cm and 798cm in H2/Ar and vacuum ambients, respectively. The resistivities of ZnO films annealed in vacuum and H2/Ar ambients at 600degreeC were similar with 0.040cm and 0.035cm, respectively. The hydrogen donor was more dominant than the oxygen vacancy or Zn interstitial donor in ZnO films annealed in ambient H2/Ar at low ...

2010-01-01

118

Elucidation of hydrogen mobility in tetralin under coal liquefaction conditions using a tritium tracer method. Effects of the addition of H2S and H2O; Tritium tracer ho wo mochiita sekitan ekika hanno jokenka deno tetralin no suiso idosei hyoka. Ryuka suiso oyobi mizu no tenka koka  

Energy Technology Data Exchange (ETDEWEB)

It was previously reported that the tritium tracer method is useful for the quantitative consideration of hydrogen behavior in coal during coal liquefaction reaction. Tetralin is excellent hydrogen donating solvent, and is considered as one of the model compounds of coal. In this study, effects of H2S and H2O on the hydrogen exchange reaction between tetralin and gaseous hydrogen labeled by tritium were investigated. It was suggested that the conversion of tetralin and the hydrogen exchange reaction between gaseous hydrogen and tetralin proceed through the radical reaction mechanism with a tetralyl radical as an intermediate product. When H2S existed in this reaction, the hydrogen exchange yield increased drastically without changing the conversion yield. This suggested that the hydrogen exchange reaction proceeds even in the reaction where radical does not give ...

1996-10-28

122

Role of B2 Adrenergic Receptors in Labor Pain  

Science.gov (United States)

Pain; Pain Threshold; Labour Pain

2010-10-01

126

Effects of single or combined histamine H1-receptor and leukotriene CysLT1-receptor antagonism on nasal adenosine monophosphate challenge in persistent allergic rhinitis  

UK PubMed Central (United Kingdom)

BackgroundThe effects of single or combined histamine H1-receptor and leukotriene CysLT1-receptor antagonism on nasal adenosine monophosphate (AMP) challenge...Full Text Available

2004-06-01

127

Limitation of immunohistochemical localization of estrogen receptor  

Energy Technology Data Exchange (ETDEWEB)

Although the radioreceptor method is widely used for estrogen receptor assay in human tissue, it has several limitations and a number of alternative methods are being explored. An immunohistochemical method of estrogen receptor assay using a specific antibody to estradiol has been proposed as a suitable alternative. The present study was designed to evaluate the validity of this method in detecting true estrogen receptors in human tumor tissue. Using radioiodinated antibody to estrogen, we have demonstrated that the estrogen antibody can detect the estrogen when it is bound to 4S type receptor but is unable to bind to estrogen when the hormone is bound to 8S type receptor. Our observations suggest that the immunohistochemical method of detection of intracellular cytosolic receptor for estrogen is not a suitable alternative to the currently used radioreceptor ...

1986-10-01

128

Cloning and expression of a human kidney cDNA for an /alpha//sub 2/-adrenergic receptor subtype  

Energy Technology Data Exchange (ETDEWEB)

An /alpha//sub 2/-adrenergic receptor subtype has been cloned from a human kidney cDNA library using the gene for the human platelet /alpha//sub 2/-adrenergic receptor as a probe. The deduced amino acid sequence resembles the human platelet /alpha//sub 2/-adrenergic receptor and is consistent with the structure of other members of he family of guanine nucleotide-binding protein-coupled receptors. The cDNA was expressed in a mammalian cell line (COS-7), and the /alpha//sub 2/-adrenergic ligand (/sup 3/H)rauwolscine was bound. Competition curve analysis with a variety of adrenergic ligands suggests that this cDNA clone represents the /alpha//sub 2/B-adrenergic receptor. The gene for this receptor is on human chromosome 4, whereas the gene for the human platelet /alpha//sub 2/-adrenergic receptor (/alpha//sub 2/A) lies on chromosome 10. This ...

1988-09-01

129

Internalized insulin-receptor complexes are unidirectionally translocated to chloroquine-sensitive degradative sites. Dependence on metabolic energy  

Energy Technology Data Exchange (ETDEWEB)

Insulin receptors on the surface of isolated rat adipocytes were photoaffinity labeled at 12 degrees C with the iodinated photoreactive insulin analogue, 125I-B2 (2-nitro-4-azidophenylacetyl)-des-PheB1-insulin, and the pathways in the intracellular processing of the labeled receptors were studied at 37 degrees C. During 37 degrees C incubations, the labeled 440-kDa insulin receptors were continuously internalized (as assessed by trypsin inaccessibility) and degraded such that up to 50% of the initially labeled receptors were lost by 120 min. Metabolic poisons (0.125-0.75 mM 2,4-dinitrophenol (DNP) and 1-10 mM NaF), which led to dose-dependent depletion of adipocyte ATP pools, inhibited receptor loss, and caused up to 3-fold increase in intracellular receptor accumulation. This effect was due to inhibition of intracellular receptor ...

1988-04-25

130

Novel high-throughput screening system for identifying STAT3-SH2 antagonists  

International Nuclear Information System (INIS)

Constitutive activation of the oncogenic transcription factor STAT3 frequently occurs in various human malignancies. STAT3 activation involves dimerization via intermolecular pTyr-SH2 interaction. Thus, antagonizing this interaction is a feasible approach to inhibit STAT3 activation for cancer therapy. In order to identify selective STAT3 inhibitors, we developed a biochemical HTS system based on AlphaScreen technology, which measures the abilities of test compounds to antagonize pTyr-SH2 interactions. We screened our chemical libraries using this system and identified 5,15-diphenylporphyrin (5,15-DPP) as a selective STAT3-SH2 antagonist. Selective inhibition of STAT3 nuclear translocation and DNA biding activity was observed in cells treated with 5,15-DPP. IL-6-dependent dimerization of STAT3, c-myc promoter binding and c-myc protein expression were all suppressed by 5,15-DPP, whereas no decrement in either expression or phosphorylation level of STAT3 was ...

2009-03-13

131

Effects of the. cap alpha. -adrenoceptor antagonists phentolamine, phenoxybenzamine, and Idazoxan on sympathetic blood flow control in the periodontal ligament of the cat  

Energy Technology Data Exchange (ETDEWEB)

Blood flow changes in the periodontal ligament (PDL) were measured indirectly by monitoring the local clearance of /sup 125/I/sup -/ during electric sympathetic nerve stimulation or close intra-arterial infusions of either noradrenaline (NA) or adrenaline (ADR) before and after administration of phentolamine (PA), phenoxybenzamine (PBZ) or Idazoxan (RX). At the doses used in the present study, PA was the only antagonist that significantly reduced the blood flow decrease seen on activation of sympathetic fibers, although PBZ also reduced this response. Idazoxan, however, did not induce the consistent effect on blood flow decreases seen on sympathetic activation. All three ..cap alpha..-adrenoceptor antagonists almost abolished the effects of exogenously administered NA and ADR. The results suggest the presence of functional post-junctional adrenoceptors of both the ..cap alpha.. 1 and ..cap alpha.. 2 subtypes in the sympathetic regulation of the ...

1988-01-01

132

Quantitative RT-PCR Expression Analysis of Lipodepsipeptides Synthetase and Defence-related Genes in Orange Fruit in Response to Antagonist-pathogen Interaction  

British Library Electronic Table of Contents (United Kingdom)

Abstract Strains of Pseudomonas syringae are effective in controlling postharvest diseases of citrus fruits, and antagonistic activity has been correlated with in vitro production of lipodepsipeptides. Additionally, biocontrol agents can induce a range of defence mechanisms of resistance in citrus tissue that result in a broad spectrum of metabolic modifications, such as systemic acquired resistance, induced systemic resistance and production of reactive oxygen species. The aim of this study was to evaluate the expression of syringomycin (syrB1) and syringopeptin (sypA) synthetase genes from P.syringae pv. syringae biocontrol strains in vitro on different culture media and in vivo on citrus fruits (Citrus sinensis cv. Tarocco) during the interaction with Penicillium digitatum by quantitati...

2011-01-01

133

Inflammatory spine disease as a cause of back pain  

International Nuclear Information System (INIS)

The aim of this review is to evaluate the role of inflammatory spine disease in patients with chronic back pain. The contribution of imaging modalities for the diagnostic evaluation of back pain is discussed. A systematic literature search based on the classification of seronegative spondyloarthropathies and rheumatoid arthritis was performed. The results of this search and the experiences in a large collective of rheumatological patients are analyzed. The prevalence of rheumatoid arthritis (1-2%) is comparable to that of spondyloarthropathies (1.9%). The etiology of these entities is not fully elucidated. Magnetic resonance imaging is increasingly used for early detection and surveillance of therapy with TNF-#alpha# antagonists. Bone marrow edema, which is only detectable with MRI, represents an early sign of inflammation. Therapy with TNF-#alpha# antagonists is based on clinical and laboratory criteria, and signs of inflammation in MRI. MRI ...

2006-06-01

134

Effect of the GnRH antagonist, acyline, on canine testicular characteristics.  

Science.gov (United States)

The primary objective was to assess the effects and clinical safety of a single high-dose of the third generation GnRH antagonist, acyline, on testicular characteristics in male dogs. Seven dogs were followed up weekly for six, 2-week periods (-2, -1, 1, 2, 3 and 4). At the end of the second period, they were given acyline (330 microg/kg sc). Responses to treatment varied among individual animals. Testicular consistency and scrotal diameter were slightly diminished (P>0.05) in Periods 1, 2, and 3. Libido and erection decreased during Periods 1 and 2 (Pdecreased semen quality with no adverse effects. PMID:17586037

2007-06-21

135

Particle size effects on the desorption properties of nanostructured magnesium dihydride (MgH2) synthesized by controlled reactive mechanical milling (CRMM)  

International Nuclear Information System (INIS)

In the present work the hydrogen desorption properties of nanostructured magnesium hydride (MgH2) synthesized by controlled reactive mechanical milling (CRMM) of elemental Mg powder under hydrogen are investigated. A profound effect of the particle size of synthesized MgH2 hydride on its hydrogen desorption characteristics measured by differential scanning calorimetery (DSC) has been found. All synthesized MgH2 powders are characterized by a double hydrogen desorption peak. Furthermore, below a certain threshold particle size the DSC desorption temperature of the peak doublet starts decreasing rapidly with decreasing of the mean hydride powder particle size (expressed as equivalent circle diameter-ECD). In contrast, the nanograin (crystallite) size of MgH2 does not seem to have apparent effect on the DSC desorption ...

2006-11-09

136

GABAB Receptors Modulate NMDA Receptor Calcium Signals in Dendritic Spines  

British Library Electronic Table of Contents (United Kingdom)

Summary Metabotropic GABAB receptors play a fundamental role in modulating the excitability of neurons and circuits throughout the brain. These receptors influence synaptic transmission by inhibiting presynaptic release or activating postsynaptic potassium channels. However, their ability to directly influence different types of postsynaptic glutamate receptors remains unresolved. Here we examine GABAB receptor modulation in layer 2/3 pyramidal neurons from the mouse prefrontal cortex. We use two-photon laser-scanning microscopy to study synaptic modulation at individual dendritic spines. Using two-photon optical quantal analysis, we first demonstrate robust presynaptic modulation of multivesicular release at single synapses. Using two-photon glutamate uncaging, we then reveal that GABAB r...

2010-01-01

137

Cloning of the cDNA and gene for a human D sub 2 dopamine receptor  

Energy Technology Data Exchange (ETDEWEB)

A clone encoding a human D{sub 2} dopamine receptor was isolated from a pituitary cDNA library and sequenced. The deduced protein sequence is 96% identical with that of the cloned rat receptor with one major difference: the human receptor contains an additional 29 amino acids in its putative third cytoplasmic loop. Southern blotting demonstrated the presence of only one human D{sub 2} receptor gene. Two overlapping phage containing the gene were isolated and characterized. DNA sequence analysis of these clones showed that the coding sequence is interrupted by six introns and that the additional amino acids present in the human pituitary receptor are encoded by a single exon of 87 base pairs. The involvement of this sequence in alternative splicing and its biological significance are discussed.

1989-12-01

138

Wind-To-Hydrogen Project: Operational Experience, Performance Testing, and Systems Integration  

Energy Technology Data Exchange (ETDEWEB)

The Wind2H2 system is fully functional and continues to gather performance data. In this report, specifications of the Wind2H2 equipment (electrolyzers, compressor, hydrogen storage tanks, and the hydrogen fueled generator) are summarized. System operational experience and lessons learned are discussed. Valuable operational experience is shared through running, testing, daily operations, and troubleshooting the Wind2H2 system and equipment errors are being logged to help evaluate the reliability of the system.

2009-03-01

139

Synthesis and Structural Characterization of a Novel Indium Mercapto Derivative [Clln(SCH2(CO)O)2]2-[(4-MepyH)2]2+  

Science.gov (United States)

The synthesis and structural characterization of a novel In(III) complex is described. The reaction

2004-01-01

140

Symbiotic N2 fixation by legumes growing in pots. 2. Uptake of VN-labelled NO3 , C2H2 reduction and H2 evolution by Trifolium subterraneum L. , Medicago truncatula Gaertn. and Acacia dealbata Link  

Energy Technology Data Exchange (ETDEWEB)

The objectives of this study were to estimate symbiotic nitrogen fixation by two common pasture legumes, Trifolium subterraneum L. and Medicago truncatula Gaertn., and an Australian native legume, Acacia dealbata Link, growing in pots using an indirect isotopic method. This method was also used to calibrate the C2H2 reduction assay of the intact plants. In addition, hydrogen evolution was measured in an attempt to explain the variations in C2H2:N2 ratios between the species. 25 refs.; 1 figure; 4 tabs.

1983-01-01

141

Solvothermal Synthesis of a New Photochromic Azo Polymer and its Self-assembly Behavior  

British Library Electronic Table of Contents (United Kingdom)

An amphiphilic azobenzene diblock copolymer {2-[4-(4-methoxy phenyl azo)phenoxy]hexyl acrylate co-acrylic acid} was synthesized via reversible addition-fragmentation chain transfer polymerization in a hydrothermal reactor. The products were characterized by 1H-NMR, DSC, GPC and UV-Vis spectroscopy. Different self-assembly behaviors of this amphiphilic diblock copolymer in different organic solvent with different water content were investigated. In THF/H2O solution, the diblock copolymer self-assembled into spheres and the spheres would then change to vesicles with smaller size by increasing the volume of H2O. However, in DMSO/H2O solution, the sizes and morphologies of the self-assembled spheres would not change significantly with an enhanced amount of H2O. Photochromic behaviors of the am...

2010-01-01

142

Dynamic response of a PEM fuel cell under reactant gas starvation  

Science.gov (United States)

The fuel cell control problem was studied. Attempts were made to control the output current of the fuel cell by starving it of hydrogen and oxygen. The motivation of this work was to increase efficiency by minimizing waste of fuel. The following findings were obtained: H2 starvation works better than O2 starvation; An optimal H2 to O2 ratio exists for combined H2&O2 starvation; The control scheme for H2&O2 starvation works well for 3 different disturbance tests and at 25 degrees C, 60 degrees C, and 80 degrees C; Fuel cell under reactant starvation is stable for at least 72 hrs.

2005-08-05

143

Durability of Membrane Electrode Assemblies (MEAs) in PEM Fuel ...  

Science.gov (United States)

Proton exchange membrane (PEM) fuel cells are energy sources that have the ... for H2 /02 PEM fuel cells because their catalysts have properties suitable for 0 ...

144

p53 mutation in breast cancer. Correlation with cell kinetics and cell of origin  

UK PubMed Central (United Kingdom)

Aim: Several studies have investigated the expression of the cytokeratins (CKs), vimentin, the epithelial growth factor receptor (EGFR), the oestrogen receptor (ER), and the progesterone...Full Text Available

2002-06-01

145

Thymol, a constituent of thyme essential oil, is a positive allosteric modulator of human GABAA receptors and a homo-oligomeric GABA receptor from Drosophila melanogaster  

UK PubMed Central (United Kingdom)

The GABA-modulating and GABA-mimetic activities of the monoterpenoid thymol were explored on human GABAA and Drosophila melanogaster...Full Text Available

2003-12-01

146

The Melanocortin 3 Receptor: A Novel Mediator of Exercise-Induced Inflammation Reduction in Postmenopausal Women?  

UK PubMed Central (United Kingdom)

The purpose of this study was to determine whether resistance exercise training-induced reductions in inflammation are mediated via melanocortin 3 receptor expression in obese (BMI 32.7 ± 3.7)...Full Text Available

147

The Cytokinin Receptors of Arabidopsis Are Located Mainly to the Endoplasmic Reticulum1[W][OA]  

UK PubMed Central (United Kingdom)

The plant hormone cytokinin is perceived by membrane-located sensor histidine kinases. Arabidopsis (Arabidopsis thaliana) possesses three cytokinin receptors: ARABIDOPSIS HISTIDINE...Full Text Available

2011-08-01

148

The Anti-Inflammatory Drug Leflunomide Is an Agonist of the Aryl Hydrocarbon Receptor  

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

149

T cell-engaging BiTE antibodies specific for EGFR potently eliminate KRAS- and BRAF-mutated colorectal cancer cells  

UK PubMed Central (United Kingdom)

Epidermal growth factor receptor (EGFR)-specific monoclonal antibodies predominantly inhibit colorectal cancer (CRC) growth by interfering with receptor signaling. Recent analyses have shown that patients...Full Text Available

2010-07-13

150

Structure of Natural Killer Cell Receptor KLRG1 Bound to E-Cadherin Reveals Basis for MHC-Independent Missing Self Recognition  

UK PubMed Central (United Kingdom)

SUMMARYThe cytolytic activity of natural killer (NK) cells is regulated by inhibitory receptors that detect the absence of self molecules on target cells. Structural studies of...Full Text Available

2009-07-17

151

Spontaneous expression of the interleukin 2 receptor gene and presence of functional interleukin 2 receptors on T lymphocytes in the blood of individuals with active pulmonary sarcoidosis.  

UK PubMed Central (United Kingdom)

Current concepts of the pathogenesis of sarcoidosis suggest that the expanded numbers of activated T-helper/inducer cells at sites of disease activity result, at least in part, from their proliferation...Full Text Available

1988-09-01

152

Sodium/Calcium Exchangers Selectively Regulate Calcium Signaling in Mouse Taste Receptor Cells  

UK PubMed Central (United Kingdom)

Taste cells use multiple signaling mechanisms to generate appropriate cellular responses to discrete taste stimuli. Some taste stimuli activate G protein coupled receptors (GPCRs) that cause calcium...Full Text Available

2010-07-01

153

Signal transduction underlying the control of urinary bladder smooth muscle tone by muscarinic receptors and ?-adrenoceptors  

UK PubMed Central (United Kingdom)

The normal physiological contraction of the urinary bladder, which is required for voiding, is predominantly mediated by muscarinic receptors, primarily the M3 subtype, with the M2...Full Text Available

2008-06-01

154

Sensitivity limits for voltage control of P2Y receptor-evoked Ca2+ mobilization in the rat megakaryocyte  

UK PubMed Central (United Kingdom)

G-protein-coupled receptor signalling has been suggested to be voltage dependent in a number of cell types; however, the limits of sensitivity of this potentially important phenomenon are unknown. Using...Full Text Available

2004-02-15

155

Retinoic acid X receptor in the diploblast, Tripedalia cystophora  

UK PubMed Central (United Kingdom)

Nuclear hormone receptors comprise a characteristic family of transcription factors found in vertebrates, insects and nematodes. Here we show by cDNA and gene cloning that a Cnidarian, Tripedalia...Full Text Available

1998-11-10

156

Replication of Extended Lifespan Phenotype in Mice with Deletion of Insulin Receptor Substrate 1  

UK PubMed Central (United Kingdom)

We previously reported that global deletion of insulin receptor substrate protein 1 (Irs1) extends lifespan and increases resistance to several age-related pathologies in female mice....Full Text Available

157

Relative potencies for barbiturate binding to the Torpedo acetylcholine receptor.  

UK PubMed Central (United Kingdom)

1. The structural requirements of an allosteric barbiturate binding site on acetylcholine receptor-rich membranes isolated from Torpedo electroplaques have been characterized by the ability of fourteen...Full Text Available

1990-11-01

158

Regulation of rat hepatic low density lipoprotein receptors. In vivo stimulation by growth hormone is not mediated by insulin-like growth factor I.  

UK PubMed Central (United Kingdom)

Growth hormone (GH) has an important role in the regulation of hepatic LDL receptor expression and plasma lipoprotein levels. This investigation was undertaken to evaluate if these effects of GH on...Full Text Available

1996-01-15

159

Receptor mechanisms and dose-response models for the effects of dioxins.  

UK PubMed Central (United Kingdom)

There is increasing evidence that receptor-mediated events impact one or more stages responsible for tumor development in experimental animals and humans. Although many chemicals and endogenous hormones...Full Text Available

1993-04-22

160

Receptor in group C and G streptococci detects albumin structures present in mammalian species.  

UK PubMed Central (United Kingdom)

The presence of albumin structures with the capacity to bind to a surface receptor in group C and G streptococci was studied in serum samples from 45 mammalian species representing 15 different orders,...Full Text Available

1982-05-01

161

Rapid detection of epidermal growth factor receptor mutations with multiplex PCR and primer extension in lung cancer  

UK PubMed Central (United Kingdom)

Epidermal growth factor receptor (EGFR) kinase domain mutations hyperactivate the kinase and confer kinase addiction of the non-small-cell lung cancer (NSCLC) tumor...Full Text Available

162

Quantitative Analysis of Endocytosis and Turnover of Epidermal Growth Factor (EGF) and EGF Receptor  

UK PubMed Central (United Kingdom)

Binding of epidermal growth factor (EGF) to the EGF receptor (EGFR) initiates signal transduction, ultimately leading to altered gene expression. Ligand-activated EGFR is also rapidly internalized...Full Text Available

2010-03-01

163

Purification of functional baculovirus particles from silkworm larval hemolymph and their use as nanoparticles for the detection of human prorenin receptor (PRR) binding  

UK PubMed Central (United Kingdom)

BackgroundBaculovirus, which has a width of 40 nm and a length of 250-300 nm, can display functional peptides, receptors and antigens on its surface by their fusion with a baculovirus...Full Text Available

164

Predictive and prognostic markers for epidermal growth factor receptor inhibitor therapy in non-small cell lung cancer  

UK PubMed Central (United Kingdom)

Epidermal growth factor receptor (EGFR) related therapies – mainly tyrosine kinase inhibitors (TKIs) such as erlotinib and gefitinib, but also monoclonal antibodies targeting EGFR, for example,...Full Text Available

2009-11-01

165

Polymorphisms in the epidermal growth factor receptor gene and the risk of primary lung cancer: a case-control study  

UK PubMed Central (United Kingdom)

BackgroundPolymorphisms in Epidermal Growth Factor Receptor (EGFR) gene may influence EGFR production and/or activity, thereby modulating susceptibility to lung...Full Text Available

166

New insights into purinergic receptor signaling in neuronal differentiation, neuroprotection, and brain disorders  

UK PubMed Central (United Kingdom)

Ionotropic P2X and metabotropic P2Y purinergic receptors are expressed in the central nervous system and participate in the synaptic process particularly associated with acetylcholine, GABA, and glutamate...Full Text Available

2007-09-01

167

Neurotensin Receptor 1 Is Expressed in Gastrointestinal Stromal Tumors but Not in Interstitial Cells of Cajal  

UK PubMed Central (United Kingdom)

Gastrointestinal stromal tumors (GIST) are thought to derive from the interstitial cells of Cajal (ICC) or an ICC precursor. Oncogenic mutations of the KIT or PDGFRA receptor tyrosine kinases are present...Full Text Available

168

Multiple Functions of the 37/67-kd Laminin Receptor Make It a Suitable Target for Novel Cancer Gene Therapy  

UK PubMed Central (United Kingdom)

The 37/67-kd laminin receptor, LAMR, is a multifunctional protein that associates with the 40S ribosomal subunit and also localizes to the cell membrane to interact with the extracellular matrix. LAMR...Full Text Available

2010-01-01

169

Lack of LDL Receptor Enhances Amyloid Deposition and Decreases Glial Response in an Alzheimer's Disease Mouse Model  

UK PubMed Central (United Kingdom)

BackgroundApolipoprotein E (ApoE), a cholesterol carrier associated with atherosclerosis, is a major risk factor for Alzheimer's disease (AD). The low-density lipoprotein receptor...Full Text Available

170

Kinetic Complexity of the Global Response to Glucocorticoid Receptor Action  

UK PubMed Central (United Kingdom)

We have characterized the kinetic response of gene targets throughout the murine genome to transcriptional modulation by the glucocorticoid receptor (GR). In contrast to a model in which multiple genes...Full Text Available

2009-04-01

171

Isolation and partial characterization of a specific alpha-fetoprotein receptor on human monocytes.  

UK PubMed Central (United Kingdom)

Since a large body of data has suggested a significant role for alpha-fetoprotein (AFP) in the regulation of the immune response at a number of levels, we examined the possibility of a specific receptor...Full Text Available

1992-10-01

172

Insulin-Like Growth Factor I Receptor Signaling Is Required for Exercise-Induced Cardiac Hypertrophy  

UK PubMed Central (United Kingdom)

The receptors for IGF-I (IGF-IR) and insulin (IR) have been implicated in physiological cardiac growth, but it is unknown whether IGF-IR or IR signaling are critically required. We generated mice with...Full Text Available

2008-11-01

173

Induction of Oxidative Stress Responses by Dioxin and other Ligands of the Aryl Hydrocarbon Receptor  

UK PubMed Central (United Kingdom)

TCDD and other polyhalogenated aromatic hydrocarbon ligands of the aryl hydrocarbon receptor (AHR) have been classically considered as non-genotoxic compounds because they fail to be directly mutagenic...Full Text Available

174

Identification of LRRc17 as a Negative Regulator of Receptor Activator of NF-?B Ligand (RANKL)-induced Osteoclast Differentiation*S?  

UK PubMed Central (United Kingdom)

Osteoblasts are the primary cells responsible for bone formation. They also support osteoclast formation from bone marrow precursors in response to osteotropic factors by inducing receptor activator...Full Text Available

2009-05-29

175

Functional Analysis of the Murine Cytomegalovirus Chemokine Receptor Homologue M33: Ablation of Constitutive Signaling Is Associated with an Attenuated Phenotype In Vivo?  

UK PubMed Central (United Kingdom)

The murine cytomegalovirus (MCMV) M33 gene is conserved among all betaherpesviruses and encodes a homologue of seven-transmembrane receptors (7TMR) with the capacity for constitutive signaling. Previous...Full Text Available

2008-02-01

176

Expression of Fc receptors is suppressed in alveolar macrophages from patients with sarcoidosis.  

UK PubMed Central (United Kingdom)

To study the expression of Fc receptors in human alveolar macrophages (AM), the cells were collected from 12 healthy controls and 22 patients with sarcoidosis and the activity involved in binding to...Full Text Available

1988-09-01

177

Evidence for an association between TSH and IGF-1 receptors  

UK PubMed Central (United Kingdom)

TSH receptor (TSHR) plays a central role in regulating thyroid function and is targeted by IgGs in Graves’ disease (GD-IgG). Whether TSHR is involved in the pathogenesis of thyroid associated...Full Text Available

2008-09-15

178

Effects of metabotropic glutamate receptor 2/3 agonism and antagonism on schizophrenia-like cognitive deficits induced by phencyclidine in rats  

UK PubMed Central (United Kingdom)

Dysregulation of glutamate neurotransmission may play a role in cognitive deficits in schizophrenia. Manipulation of glutamate signaling using drugs acting at metabotropic glutamate receptors...Full Text Available

2010-08-10

179

Development of a Selective Modulator of Aryl Hydrocarbon (Ah) Receptor Activity that Exhibits Anti-Inflammatory Properties  

UK PubMed Central (United Kingdom)

The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that mediates the toxicity of 2,3,7,8-tetrachlorodibenzo-p-dioxin. However, the role of the AHR...Full Text Available

2010-05-17

180

Deletion of the Receptor for Advanced Glycation End Products Reduces Glomerulosclerosis and Preserves Renal Function in the Diabetic OVE26 Mouse  

UK PubMed Central (United Kingdom)

OBJECTIVEPrevious studies showed that genetic deletion or pharmacological blockade of the receptor for advanced glycation end products (RAGE) prevents the early structural changes...Full Text Available

2010-08-01

181

Cloning of the mouse hepatitis virus (MHV) receptor: expression in human and hamster cell lines confers susceptibility to MHV.  

UK PubMed Central (United Kingdom)

The cellular receptor for murine coronavirus mouse hepatitis virus (MHV)-A59 is a member of the carcinoembryonic antigen (CEA) family of glycoproteins in the immunoglobulin superfamily. We isolated...Full Text Available

1991-12-01

182

Characterisation of the Expression of NMDA Receptors in Human Astrocytes  

UK PubMed Central (United Kingdom)

Astrocytes have long been perceived only as structural and supporting cells within the central nervous system (CNS). However, the discovery that these glial cells may potentially express receptors capable...Full Text Available

183

Biochemical characterization of the molecular interaction between recombinant basic fibroblast growth factor and a recombinant soluble fibroblast growth factor receptor.  

UK PubMed Central (United Kingdom)

The extracellular domain of human fibroblast growth factor receptor (XC-FGF-R) was expressed in Escherichia coli. The protein was purified to homogeneity and the interaction with basic fibroblast growth...Full Text Available

1993-09-15

184

Attenuation of Cocaine's Reinforcing and Discriminative Stimulus Effects via Muscarinic M1 Acetylcholine Receptor StimulationS?  

UK PubMed Central (United Kingdom)

Muscarinic cholinergic receptors modulate dopaminergic function in brain pathways thought to mediate cocaine's abuse-related effects. Here, we sought to confirm and ...Full Text Available

2010-01-01

185

Association Analysis of Nuclear Receptor Rev-erb Alpha Gene (NR1D1) and Japanese Methamphetamine Dependence  

UK PubMed Central (United Kingdom)

Several investigations suggested abnormalities in circadian rhythms are related to the pathophysiology of psychiatric disorders, including drug addiction. Recently, orphan nuclear receptor rev-erb alpha...Full Text Available

2011-03-01

186

Antigenic analysis of the second extra-cellular loop of the human beta-adrenergic receptors.  

UK PubMed Central (United Kingdom)

Polyclonal antibodies were raised in rabbits by immunization with free peptides corresponding to positions 197-222 of the human beta 1-adrenergic receptor (beta 1 peptide) and the corresponding sequence...Full Text Available

1989-10-01

187

An analysis by low-angle neutron scattering of the structure of the acetylcholine receptor from Torpedo californica in detergent solution.  

UK PubMed Central (United Kingdom)

The acetylcholine receptor from the electric tissue of Torpedo californica is a large, integral membrane protein containing four different types of polypeptide chains. The structure of the purified...Full Text Available

1979-12-01

188

Activated PPAR? Targets Surface and Intracellular Signals That Inhibit the Proliferation of Lung Carcinoma Cells  

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

2008-01-01

189

Acetylcholine receptor kinetics. A description from single-channel currents at snake neuromuscular junctions.  

UK PubMed Central (United Kingdom)

Single-channel currents from acetylcholine receptor channels of garter snake neuromuscular junctions were recorded using the patch-clamp technique. Low concentrations of acetylcholine or carbamylcholine...Full Text Available

1982-09-01

190

A multigene predictor of metastatic outcome in early stage hormone receptor-negative and triple-negative breast cancer  

UK PubMed Central (United Kingdom)

IntroductionVarious multigene predictors of breast cancer clinical outcome have been commercialized, but proved to be prognostic only for hormone receptor (HR) subsets overexpressing...Full Text Available

2010-01-01

191

A Randomized Clinical Trial Investigating the Relationship Between Aprotinin and Hypercoagulability in Off-Pump Coronary Surgery  

UK PubMed Central (United Kingdom)

BACKGROUNDOff-pump coronary artery bypass (OPCAB) surgery is associated with a hypercoagulable state in which the platelet thrombin receptor, protease-activated receptor-1...Full Text Available

2009-11-01

192

A Point Mutation in a Domain of Gamma Interferon Receptor 1 Provokes Severe Immunodeficiency  

UK PubMed Central (United Kingdom)

Gamma interferon (IFN-γ) and the cellular responses induced by it are essential for controlling mycobacterial infections. Most patients bearing an IFN-γ receptor ligand-binding chain...Full Text Available

2001-01-01

193

In vivo modulation of murine serum tumour necrosis factor and interleukin-6 levels during endotoxemia by oestrogen agonists and antagonists.  

UK PubMed Central (United Kingdom)

Oestrogen has been reported to modulate tumour necrosis factor (TNF), interleukin (IL)-1 and IL-6 cytokine levels in human mononuclear cell cultures. In the present study, the effects of exogenous oestrogen...Full Text Available

1995-09-01

194

Discrimination between UTP- and P2-purinoceptor-mediated depolarization of rat superior cervical ganglia by 4,4'-diisothiocyanatostilbene-2,2'- disulphonate (DIDS) and uniblue A.  

UK PubMed Central (United Kingdom)

1. Using a grease-gap recording technique we have investigated the effects of some antagonists of P2-purinoceptors on the depolarization of the rat isolated superior cervical ganglion evoked by 100...Full Text Available

1995-06-01

196
197

Purinergic receptors are involved in tooth-pulp evoked nocifensive behavior and brainstem neuronal activity  

UK PubMed Central (United Kingdom)

BackgroundTo evaluate whether P2X receptors are involved in responses to noxious pulp stimulation, the P2X3 and P2X2/3 receptor agonist α,β-methyleneATP...Full Text Available

198

P2X1 receptor mobility and trafficking; regulation by receptor insertion and activation  

UK PubMed Central (United Kingdom)

P2X1 receptors for ATP contribute to signalling in a variety of cell types and following stimulation undergo rapid desensitisation (within 1 s), and require ∼5 min to recover. In HEK293 cells...Full Text Available

2010-06-01

199

Nuclear receptor co-repressor SMRT regulates mitochondrial oxidative metabolism and mediates aging related metabolic deterioration  

UK PubMed Central (United Kingdom)

SummaryThe transcriptional co-repressor SMRT utilizes two major receptor interacting domains (RID1 and RID2) to mediate nuclear receptor (NR) signaling through epigenetic modification....Full Text Available

2010-12-01

200

Mechano-transduction in Osteoblastic Cells Involves Strain-regulated Estrogen Receptor ?-mediated Control of Insulin-like Growth Factor (IGF) I Receptor Sensitivity to Ambient IGF, Leading to Phosphatidylinositol 3-Kinase/AKT-dependent Wnt/LRP5 Receptor-independent Activation of ?-Catenin Signaling*  

UK PubMed Central (United Kingdom)

The capacity of bones to adjust their mass and architecture to withstand the loads of everyday activity derives from the ability of their resident cells to respond appropriately to the strains engendered....Full Text Available

2010-03-19

201

Global analysis of estrogen receptor beta binding to breast cancer cell genome reveals an extensive interplay with estrogen receptor alpha for target gene regulation  

UK PubMed Central (United Kingdom)

BackgroundEstrogen receptors alpha (ERα) and beta (ERβ) are transcription factors (TFs) that mediate estrogen signaling and define the hormone-responsive phenotype...Full Text Available

202

Forkhead Box Transcription Factor FOXO3a Regulates Estrogen Receptor Alpha Expression and Is Repressed by the Her-2/neu/Phosphatidylinositol 3-Kinase/Akt Signaling Pathway  

UK PubMed Central (United Kingdom)

The expression status of the estrogen receptor alpha (ERα) and that of the epidermal growth factor receptor Her-2/neu frequently correlate inversely in breast cancers. While ERα-dependent...Full Text Available

2004-10-01

203

Extraribosomal functions associated with the C terminus of the 37/67?kDa laminin receptor are required for maintaining cell viability  

UK PubMed Central (United Kingdom)

The 37/67 kDa laminin receptor (LAMR) is a multifunctional protein, acting as an extracellular receptor, localizing to the nucleus, and playing roles in rRNA processing and ribosome assembly....Full Text Available

2010-05-01

204

Cloning and characterization of a 77-kDa oestrogen receptor isolated from a human breast cancer cell line.  

UK PubMed Central (United Kingdom)

We have cloned and characterized a 77-kDa oestrogen receptor (ER) from an oestrogen-independent subclone of the MCF-7 human breast cancer cell line. This receptor contains an in-frame, tandem duplication...Full Text Available

1997-01-01

205

Synthesis, crystal structure, spectroscopic and photoluminescence studies of manganese(II), cobalt(II), cadmium(II), zinc(II) and copper(II) complexes with a pyrazole derived Schiff base ligand  

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 ...

2011-01-01

206

Sealant Research for solid oxide fuel cells  

International Nuclear Information System (INIS)

The objective of this work is to develop sealing materials for solid oxide fuel cells (SOFCs). A suitable sealant must form strong, dense bonds with SOFC components, be chemically and mechanically compatible with the components, be stable at 1000 degrees C in the operating environment of the SOFC (H_2 and H_2O on the anode side, O_2 on the cathode side), and must be nonconductive.

1992-07-01

207

Novel inorganic hydrogen-bonded crystals with nonlinear optical properties  

International Nuclear Information System (INIS)

Four inorganic hydrogen-bonded crystals with second-order nonlinear properties have been discovered: K_4LiH_3(SO_4)_4, Na_2SeO_4#centre dot#H_2SeO_3#centre dot#H_2O, Cs_1_,_5Li_1_,_5H(SO_4)_2 and NH_4HSeO_4. (author)

2000-01-01

208

HupUV proteins of Rhodobacter capsulatus can bind H2: evidence from the H-D exchange reaction.  

UK PubMed Central (United Kingdom)

The H-D exchange reaction has been measured with the D2-H2O system, for Rhodobacter capsulatus JP91, which lacks the hupSL-encoded hydrogenase, and R. capsulatus BSE16, which lacks the HupUV proteins....Full Text Available

1997-01-01

209

A precise structure redetermination of nickel ammonium sulfate hexahydrate, Ni(H_2O)_6.2NH_4.2SO_4  

International Nuclear Information System (INIS)

The Ni(H_2O)_6 ion is located at an inversion center. Six octahedral water molecules surround the Ni"I"I ion and form hydrogen bonds with the sulfate groups. Each ammonium group binds to the sulfate groups through hydrogen bonds. (orig.).

1994-05-01

210

Effect of hydrogen sulfide on chemical looping of coal-derived synthesis gas over bentonite-supported metal---oxide oxygen carriers  

Science.gov (United States)

The effect of hydrogen sulfide (H2S) on the chemical looping combustion of coal-derived synthesis gas with bentonite-supported metal oxidesssuch as iron oxide, nickel oxide, manganese oxide, and copper oxideswas investigated by thermogravimetric analysis, mass spectrometry, and X-ray photoelectron spectroscopy (XPS). During the reaction with synthesis gas containing H2S, metal-oxide oxygen carriers were first reduced by carbon monoxide and hydrogen, and then interacted with H2S to form metal sulfide, which resulted in a weight gain during the reduction/sulfidation step. The reduced/sulfurized compounds could be regenerated to form sulfur dioxide and oxides during the oxidation reaction with air. The reduction/oxidation capacities of iron oxide and nickel oxide were not affected by the presence of H2S, but both ...

2009-01-01

211

Dodecanuclear rhenium cluster complexes with an interstitial carbon atom: Synthesis, structures and properties of two new compounds K6[Re12CS17(OH)6]?4H2O and Na12Re12CS17(SO3)6?48.5H2O  

British Library Electronic Table of Contents (United Kingdom)

The dodecanuclear rhenium anionic complex with terminal hydroxo ligands [Re12CS17(OH)6]6? was obtained by the reaction of K6[Re12CS17(CN)6]?20H2O with molten KOH at 300 ?C. The cluster complex was crystallized as a potassium salt from aqueous solution. The reaction between K6[Re12CS17(OH)6]?4H2O and Na2S2O4 in water under reflux results in the formation of the complex Na12[Re12CS17(SO3)6]?48.5H2O. Both new compounds were characterized by single-crystal X-ray diffraction, elemental analyses and IR spectroscopy. The electronic structure of [Re12CS17(OH)6]6? was also elucidated by DFT calculation

2010-01-01

212

Characterization of an oligopeptide chemoattractant receptor on human blood monocytes using a new radioligand  

Energy Technology Data Exchange (ETDEWEB)

The study of chemoattractant receptors on human monocytes had been limited by the lack of a radioligand suitable for use with the small numbers of cells routinely available from human donors. A new synthetic oligopeptide radioligand f(/sup 35/S)Met-leu-phe, with a higher specific radioactivity than was available with the tritiated compound, was used to characterize a chemoattractant receptor on freshly isolated human blood monocytes. These cells bind f(/sup 35/)met-leu-phe with a dissociation constant (KD) of 30.2 +/- 5.6 nM and contain 84,000 +/- 11,300 receptors per cell. f(/sup 35/)met-leu-phe does not bind specifically to blood lymphocytes. The specificity of the oligopeptide receptor on monocytes is indistinguishable from the oligopeptide chemoattractant receptor on human polymorphonuclear leukocytes. Using f(/sup 35/)met-leu-phe, it will now be feasible to study the ...

1984-03-01

213

Herschel observations in the ultracompact HII region Mon R2: Water in dense Photon-dominated regions (PDRs)  

CERN Document Server

Mon R2, at a distance of 830 pc, is the only ultracompact HII region (UC HII) where the photon-dominated region (PDR) between the ionized gas and the molecular cloud can be resolved with Herschel. HIFI observations of the abundant compounds 13CO, C18O, o-H2-18O, HCO+, CS, CH, and NH have been used to derive the physical and chemical conditions in the PDR, in particular the water abundance. The 13CO, C18O, o-H2-18O, HCO+ and CS observations are well described assuming that the emission is coming from a dense (n=5E6 cm-3, N(H2)>1E22 cm-2) layer of molecular gas around the UC HII. Based on our o-H2-18O observations, we estimate an o-H2O abundance of ~2E-8. This is the average ortho-water abundance in the PDR. Additional H2-18O and/or ...

2010-01-01

214

Insulin-like growth factor II receptor is phosphorylated by a tyrosine kinase in adipocyte plasma membranes  

Energy Technology Data Exchange (ETDEWEB)

Incorporation of /sup 32/P from (gamma-32P)ATP into tyrosine residues of the insulin-like growth factor (IGF)-II receptor was observed in a Triton X-100-insoluble fraction of rat adipocyte plasma membranes. IGF-II receptor phosphorylation proceeded to a stoichiometry of approximately 0.5 mol of phosphate/IGF-II binding site after 10 min of incubation at 4 degrees C. A Km for ATP of 6 microM was calculated for this phosphorylation reaction. Addition of IGF-II caused an approximately 2-fold increase in tyrosine phosphorylation of the IGF-II receptor in this preparation. In contrast, phosphorylation of angiotensin II by the Triton X-100 washed membranes was not stimulated by IGF-II. Incubation of purified receptor immobilized on IGF-II agarose or of receptor-enriched low density microsomal membranes with (gamma-32P)ATP did not result in appreciable incorporation of (/sup 32/P)phosphate ...

1986-06-15

215

Dissociation of insulin receptor phosphorylation and stimulation of glucose transport in BC3H-1 myocytes  

Energy Technology Data Exchange (ETDEWEB)

The authors have investigated insulin receptor phosphorylation in differentiated cultured BC3H-1 myocytes. As for other insulin-responsive cell systems in partially purified wheat germ agglutinin receptor preparations, insulin stimulates the phosphorylation of its own receptor (95K ..beta..-subunits) in a dose dependent manner (0-400 nM), as identified by immunoprecipitation with antiinsulin receptor antibodies and SDS-PAGE. In the same preparations they show that 12-0-tetradecanyl phorbol acetate (TPA), which in many respect ..beta..-subunits in the same dose dependent manner (0-5 ..mu..M). In addition, antiinsulin receptor antibodies (B-10) also induced phosphorylation of mimics insulin action, also induced phosphorylation of the insulin receptor and HPLC tryptic maps of the /sup 32/P-labeled ..beta..-subunit were identical to those for insulin-induced ...

1986-05-01

216

Thermodynamic study of systems with lower critical solution temperatures: H_2O + (C_2H_5)_3N, D_2O + (C_2H_5)_3N  

International Nuclear Information System (INIS)

Molar excess enthalpies and molar excess volumes are reported for the systems H_2O + (C_2H_5)_3N and D_2O + (C_2H_5)_3N at temperatures below and above their lower critical solution temperatures. The molar excess enthalpies are slightly less exothermic for the D_2O system. The molar excess volumes of the H_2O and D_2O systems are within experimental error of one another. Compositions of conjugate solutions estimated from the calorimetric and volumetric measurements agree with those obtained from published liquid-liquid phase diagrams. (Auth.).

1979-01-01

217

Thermal- and radiation-induced interactions of water on U02 surfaces.  

Energy Technology Data Exchange (ETDEWEB)

Most plans for the disposition of surplus nuclear materials involve storage in sealed containers where the evolution of gases from reactions of adsorbed water could present both pressure and flammability hazards[l] . Despite efforts such as calcining the material to minimize the water content prior to packaging, both residual moisture and readsorbed water may be present in the final containers . Given the anticipated temperature excursions during transportation and storage, this water may thermally desorb, increasing the pressure, and/or thermally dissociate to produce H2 gas, increasing flammability hazards . In addition, the radiation from the nuclear material may induce radiolysis of the water with the likely products being water vapor, H2, 02 and H2O2. In order to better understand the relative importance of the thermal- and radiationinduced chemistry, we ...

2003-01-01

218

The disruption of l-carnitine metabolism by aluminum toxicity and oxidative stress promotes dyslipidemia in human astrocytic and hepatic cells  

British Library Electronic Table of Contents (United Kingdom)

l-Carnitine is a critical metabolite indispensable for the metabolism of lipids as it facilitates fatty acid transport into the mitochondrion where b-oxidation occurs. Human astrocytes (CCF-STTG1 cells) and hepatocytes (HepG2 cells) exposed to aluminum (Al) and hydrogen peroxide (H2O2), were characterized with lower levels of l-carnitine, diminished b-oxidation, and increased lipid accumulation compared to the controls. g-Butyrobetainealdehyde dehydrogenase (BADH) and butyrobetaine dioxygenase (BBDOX), two key enzymes mediating the biogenesis of l-carnitine, were sharply reduced during Al and H2O2 challenge. Exposure of the Al and H2O2-treated cells to a-ketoglutarate (KG), led to the recovery of l-carnitine production with the concomitant reduction in ROS levels. It appears that the chann...

2011-01-01

219

Synthesis and Crystal Structures of Octahedral Metal Complexes containing the New Dianion [PhP(Se,O)Se-Se(O,Se)PPh]2-  

British Library Electronic Table of Contents (United Kingdom)

The synthesis and structures of three new compounds are reported. [Mg2{PhP(Se,O)Se-Se(O,Se)PPh}2(thf)7(H2O)3] (1), [Mg{PhP(Se,O)Se-Se(O,Se)PPh}(thf)3(H2O)] (2), and [Mn{PhP(Se,O)Se-Se(O,Se)PPh}(thf)3(H2O)] (3) were prepared by treatment of Woollins reagent [PhP(Se)(m-Se)]2 with the corresponding hydrated metal acetates.

2007-01-01

220

Species and Organ Diversity in the Effects of Hydrogen Peroxide on Superoxide Dismutase Activity In Vitro  

British Library Electronic Table of Contents (United Kingdom)

Abstract Superoxide dismutase (SOD) is ubiquitous in aerobic organisms and constitutes the first link in the enzyme scavenging system of reactive oxygen species. In the present study, species and organ diversity of SOD activity in a solution and in an in-gel assay system, as well as the effects of hydrogen peroxide (H2O2) on SOD activity, were investigated. In a solution assay system, SOD activity of jackfruit root, shoot, leaves, axes, and cotyledons, of maize embryos and endosperms, of mung bean leaves and seeds, of sacred lotus axes and cotyledons, and of rice and wheat leaves was increased by 1-15 mmol/L H2 O2. However, SOD activity in rice root and seeds, maize roots and leaves, mung bean roots and shoots, and wheat seeds was decreased by 1-15 mmol/L H2O2. The SOD activity of wheat ro...

2006-01-01

221

Pretreatment of empty palm fruit bunch for production of chemicals via catalytic pyrolysis  

British Library Electronic Table of Contents (United Kingdom)

The effect of chemical pretreatments using NaOH, H2O2, and Ca(OH)2 on Empty Palm Fruit Bunches (EPFB) to degrade EPFB lignin before pyrolyis was investigated. Spectrophotometer analysis proved consecutive addition of NaOH and H2O2 decomposed almost 100% of EPFB lignin compared to 44% for the Ca(OH)2, H2O2 system while NaOH and Ca(OH)2 used exclusively could not alter lignin much. Next, the pretreated EPFB was catalytically pyrolyzed. Experimental results indicated the phenolic yields over Al-MCM-41 and HZSM-5 catalysts were 90wt% and 80wt%, respectively compared to 67wt% yield for the untreated sample under the same set of conditions. Meanwhile, the experiments with HY zeolite yielded 70wt% phenols.

2009-01-01

222

Preconceptual study of an advanced MAPLE research reactor  

International Nuclear Information System (INIS)

The Advanced MAPLE is a research reactor design under development as a high-flux neutron source. The main performance goals for the reactor are a high peak thermal neutron flux in a heavy-water reflector tank, and a high average fast neutron flux in a central irradiation facility, with a maximum linear fuel rod rating of less than 120 kW/m. This study investigated the neutronic and reactor design consequences of the use of H_2O coolant as opposed to D_2O. The neutronics results, and several other considerations, indicate that H_2O coolant has a number of advantages. It is suggested that the H_2O coolant option be considered in the design of the Advanced MAPLE reactor. (L.L.) 9 refs., 4 figs., tab.

1990-06-03

223

Interaction of iodine-containing acids with o-methylacetanilide in aqueous solutions  

International Nuclear Information System (INIS)

The systems CH_3COHNC_6H_4CH_3-HI-H_2O, CH_3CONHC_6H_4CH_3-HIO_3-H_2O, CH_3CONHC_6H_4CH_3-H_5IO_6-H_2O have been studied by the solubility method. It has been ascertained that the systems containing periodic and iodic acids are referred to systems of simple eutonic type. Formation of compound of o-methylacetanilide with iodic acid of equimolecular composition has been proved. Concentrational boundaries of its existence in solutions have been established, its certain physicochemical characteristics being determined.

224

Graphene-Pt nanocomposite for nonenzymatic detection of hydrogen peroxide with enhanced sensitivity  

British Library Electronic Table of Contents (United Kingdom)

A sensitive hydrogen peroxide (H2O2) sensor was fabricated based on graphene-Pt (GN-Pt) nanocomposite. The GN-Pt was synthesized by photochemical reduction of K2PtCl4 on GNs, and characterized by atomic force microscope (AFM), transmission electron microscope (TEM), and energy-dispersive X-ray spectroscopy (EDS). Electrochemical investigations indicated that the GN-Pt exhibited a high peak current and low overpotential towards the reduction of H2O2. The GN-Pt modified glass carbon electrode displayed a wide linear range (2-710mM), low limit of detection (0.5mM) and good selectivity for detection of H2O2 with a much higher sensitivity than that of Pt nanoparticles or graphene modified electrode.

2011-01-01

225

Conversion of ortho-para H2O isomers in water and a jump in erythrocyte fluidity through a microcapillary at a temperature of 36.6?0.3?C  

British Library Electronic Table of Contents (United Kingdom)

A mechanism is proposed for the previously observed [1] jump in erythrocyte fluidity through a microcapillary 1.3 ?m in diameter at a temperature of 36.6?0.3?C. Our interpretation is based on the experimental evidence both for existence of ortho and para H2O isomers in water and on spin-selective interaction of proteins with para H2O isomers as hydration shells of biomolecules are being formed [2]. It is important that the formation of hydration shells of proteins and DNA in aqueous solutions is accompanied by an increase in the Brillouin shift to 0.4 cm?1 (?0.25 cm?1 in water), which points to the formation of icelike structures. We believe that the coincidence of the translational energy kT of the Brownian motion and the energy of the rotational quanta for the 313?202 transition of para ...

2009-01-01

226

Low-level microwave irradiations affect central cholinergic activity in the rat  

Energy Technology Data Exchange (ETDEWEB)

Sodium-dependent high-affinity choline uptake was measured in various regions of the brains of rats irradiated for 45 min with either pulsed or continuous-wave low-level microwaves (2,450 MHz; power density, 1 mW/cm2; average whole-body specific absorption rate, 0.6 W/kg). Pulsed microwave irradiation (2-microseconds pulses, 500 pulses/s) decreased choline uptake in the hippocampus and frontal cortex but had no significant effect on the hypothalamus, striatum, and inferior colliculus. Pretreatment with a narcotic antagonist (naloxone or naltrexone; 1 mg/kg i.p.) blocked the effect of pulsed microwaves on hippocampal choline uptake but did not significantly alter the effect on the frontal cortex. Irradiation with continuous-wave microwaves did not significantly affect choline uptake in the hippocampus, striatum, and hypothalamus but decreased the uptake in the frontal cortex. The effect on the frontal cortex was not altered by pretreatment with narcotic ...

1987-01-01

227

Light-dependent regulation of DEL1 is determined by the antagonistic action of E2Fb and E2Fc.  

Science.gov (United States)

Endoreduplication represents a cell cycle variant during which multiple rounds of DNA replication occur without subsequent chromosome separation and cytokinesis, resulting into a cellular increase of the DNA content. Although the DNA ploidy level of cells is controlled by external stimuli such as light, currently limited knowledge is available on how environmental signals regulate the endoreduplication cycle at the molecular level. Previously, we have demonstrated that the conversion from the mitotic cell cycle into an endoreduplication cycle is mediated by the atypical E2F transcription factor DEL1 that operates as a repressor of endocycle onset. Here, we identified DEL1 as a transcriptional target of the classical E2Fb and E2Fc transcription factors that antagonistically control DEL1 transcript levels through competition for a single E2F cis-acting binding site. Correspondingly with the reported opposite effect of light on the E2Fb and E2Fc protein levels, the ...

2011-09-01

228

Aging, tumor suppression and cancer: High-wire act!  

Energy Technology Data Exchange (ETDEWEB)

Evolutionary theory holds that aging is a consequence of the declining force of natural selection with age. We discuss here the evidence that among the causes of aging in complex multicellular organisms, such as mammals, is the antagonistically pleiotropic effects of the cellular responses that protect the organism from cancer. Cancer is relatively rare in young mammals, owing in large measure to the activity of tumor suppressor mechanisms. These mechanisms either protect the genome from damage and/or mutations, or they elicit cellular responses--apoptosis or senescence--that eliminate or prevent the proliferation of somatic cells at risk for neoplastic transformation.We focus here on the senescence response, reviewing its causes, regulation and effects. In addition, we describe recent data that support the idea that both senescence and apoptosis may indeed be the double-edged swords predicted by the evolutionary hypothesis of antagonistic ...

2004-08-15

229

The development of sigma-receptor specific radiopharmaceuticals for spect imaging of human tumors  

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 ...

1994-08-21

230

Suppression of receptors for prolactin and estrogen in rat liver due to treatment with the growth hormone analogue produced by the tapeworm Spirometra mansonoides.  

Science.gov (United States)

Somatogenic hormones play an important role in regulation of receptors for prolactin (PRL) and estrogen. Plerocercoids of the tapeworm, S. mansonoides produce a factor which mimics some, but not all of the actions reported for GH. Intact female rats were subjected to a constant infusion of plerocercoid growth factor (PGF) via a subcutaneous infection for two weeks to determine if PGF influences receptors for PRL, GH or estradiol. The rate of weight gain in the PGF-treated rats was accelerated in spite of a marked reduction in serum GH. Partially-purified PGF specifically displaced [125I]hGH from rat liver receptors but microsomes prepared from rats treated with PGF specifically bound significantly less [125I]hGH than microsomes from control rats. The reduction in [125I]hGH binding was not due to occupancy or to a change in affinity but to a suppression in receptor concentration. Scatchard analysis of ...

1986-01-01

231

hysics Facility - NASA  

Science.gov (United States)

vehicles including the H2-A rocket and the space shuttle. .... The vacuum can's main function is to provide a high vacuum so that the science experiment and its sensors ... EMI-shielded power conversion from the incoming ISS power supply. 4. ...

232

The optical and structural properties of polycrystalline Cu(In,Ga)(Se,S)2 absorber thin films  

British Library Electronic Table of Contents (United Kingdom)

The pentenary compound semiconductor Cu(In,Ga)(Se,S)2 is one of the most attractive materials for high-efficiency solar cells due to its tunable band gap to match well the solar spectrum. In this study, semiconducting Cu(In,Ga)(Se,S)2 thin films were prepared by a classical two-step growth process, which involves the selenization and/or sulfurization of In/Cu?Ga precursor. During the precursor formation step metallic In/Cu?Ga alloys were deposited onto the Mo-coated soda-lime glass substrates by DC magnetron sputter process. The respective precursors were subsequently reacted with H2Se and/or H2S gasses, at elevated temperatures. By optimizing the selenization parameters, such as the gas concentrations, reaction time, reaction temperature, and the flow of H2Se and H2S, high quality, single...

2011-01-01

233

The Effect of O2, H2O, and N2 on the Fatigue Crack Growth Behavior of an Alpha + Beta Titanium Alloy at 24 C and 177 C  

Science.gov (United States)

To study the effects of atmospheric species on the fatigue crack growth behavior of an a+B titanium

2001-01-01

234

Technical Key Figures for Photo-biological Hydrogen Production by Micro-algae  

International Nuclear Information System (INIS)

One regenerative path to produce hydrogen is the photo-biological hydrogen production by the green micro-alga Chlamydomonas reinhardtii. This process can be divided into three phases: a growth phase, a phase in which the algae adapt from oxygen production and CO2-fixation to fermentative H2 production, and a phase in which H2 is produced. In a research project carried out at Ruhr-Universitat Bochum, a new developed flat panel bioreactor was investigated. A system analysis was conducted and energetic and environmental key figures were determined. The intention of this assessment on a very early technological stage was to collect first technical data in order to classify the current technological status of the photo-biological H2 production to identify future potentials and to uncover weaknesses. For this reason the key figures were evaluated for the status quo ...

2006-06-13

235

Solar photochemistry and heterogeneous photocatalysis  

International Nuclear Information System (INIS)

The search for alternative energy supplies continues since the oil crisis of 1973. One energy vector is dihydrogen, H_2. Of the group VI hydrides, water has been the focus of most studies in harnessing solar energy and generating H_2. Two basic photochemical strategies have been employed: molecular photocatalytic systems, and semiconductor based photocatalytic systems. The results have not met with the euphoric expectations of the mid-1970's because of the difficulties encountered in H_2O splitting (E"0 S"2 "-/S = + 0.51 eV, NHE) is another vehicle tapped as a potential source of H_2. Heterogeneous photocatalysis utilizing semiconductor particulates and sunlight as the photon source has been successful with interesting quantum efficiencies. To this end, novel photocatalytic devices have been developed; one of these uses ...

236

Probing active galactic nuclei with H2O megamasers.  

UK PubMed Central (United Kingdom)

We describe the characteristics of the rapidly rotating molecular disk in the nucleus of the mildly active galaxy NGC4258. The morphology and kinematics of the disk are delineated by the point-like...Full Text Available

1995-12-05

237

Plasma nitriding of austenitic stainless steel in N_2 and N_2/H_2 gas admixture  

International Nuclear Information System (INIS)

Plasma nitriding in glow discharge is a process of modifying surface properties of a material by which surface hardness, corrosion resistance, fatigue strength etc. of a material can be improved

2004-09-01

238

Onset of Quiescence Following p53 Mediated Down-Regulation of H2AX in Normal Cells  

UK PubMed Central (United Kingdom)

Normal cells, both in vivo and in vitro, become quiescent after serial cell proliferation. During this process, cells can develop immortality with genomic instability,...Full Text Available

239

Mechanisms of radical removal by SO2  

DEFF Research Database (Denmark)

It is well established from experiments in premixed, laminar flames, jet-stirred reactors, flow reactors, and batch reactors that SO2 acts to catalyze hydrogen atom removal at stoichiometric and reducing conditions. However, the commonly accepted mechanism for radical removal, SO2 + H(+M) reversible arrow HOSO(+M), HOSO + H/OH reversible arrow SO2 + H-2/H2O, has been challenged by recent theoretical and experimental results. Based on ab initio calculations for key reactions, we update the kinetic model for this chemistry and re-examine the mechanism of fuel/SO2 interactions. We find that the interaction of SO, with the radical pool is more complex than previously assumed, involving HOSO and SO, as well as, at high temperatures also HSO, SH, and S. The revised mechanism with a high rate constant for H + SO2 recombination and with SO + H2O, rather than SO2 + ...

2007-01-01

240

Magnetic moment measurements of gadolinium, holmium and ytterbium tartrate trihydrate crystals  

British Library Electronic Table of Contents (United Kingdom)

Magnetic moment and susceptibility of single crystals of rare earth tartrates of the type R(C4H4O6)(C4H5O6)3H2O (where R = Gd, Ho, and Yb), using a vibration sample magnetometer are reported. The experimental values of molar susceptibilities for Gd(C4H4O6)(C4H5O6)3H2O, Ho(C4H4O6)(C4H5O6)3H2O, and Yb(C4H4O6)(C4H5O6)3H2O are 2.58x10-2, 4.66x10-2, and 8.03x10-3 (in cgs em units), respectively. The calculated effective magnetic moments are in good agreement with the theoretical predictions on rare earth ions.

2008-01-01

241

H_2 emission arises outside photodissociation regions in ultra-luminous infrared galaxies  

CERN Document Server

Ultra-luminous infrared galaxies are among the most luminous objects in the local universe and are thought to be powered by intense star formation. It has been shown that in these objects the rotational spectral lines of molecular hydrogen observed at mid-infrared wavelengths are not affected by dust obscuration, leaving unresolved the source of excitation of this emission. Here I report an analysis of archival Spitzer Space Telescope data on ultra-luminous infrared galaxies and demonstrate that star formation regions are buried inside optically thick clouds of gas and dust, so that dust obscuration affects star-formation indicators but not molecular hydrogen. I thereby establish that the emission of H_2 is not co-spatial with the buried starburst activity and originates outside the obscured regions. This is rather surprising in light of the standard view that H_2 emission is directly associated with ...

2010-01-01

242

Effect of rib height and pitch of the thermal performance of a passage disturbed by detached solid ribs  

Energy Technology Data Exchange (ETDEWEB)

Laser holographic interferometry and pressure measurements are presented for the effects of rib-to-duct height ratio (H/2B), rib pitch-to-height ratio (Pi/H), and Reynolds number (Re) on the spatially periodic-fully developed turbulent heat transfer and friction in a rectangular duct of width-to-height ratio of 4:1 with an array of ribs detached from one wall at a clearance to rib-height ratio of 0.38. The ranges of H/2B, Pi/H, and Re examined were 0.13 to 0.26, 7 to 13, and 5 {times} 10{sup 3} to 5 {times} 10{sup 4}, respectively. The difference in the H/2B dependence of the thermal performance between the detached and attached solid-rib array is documented H/2B = 0.17 and Pi/H = 10 are found to provide the best thermal performance for the range of parameters tested. Compact heat transfer and friction correlations are ...

1998-07-01

243

Crystallohydrate forms of trisubstituted uranyl orthophosphate  

International Nuclear Information System (INIS)

The conditions of production and the stability regions have been studied for the following crystallohydrates of trisubstituted uranyl orthophosphates: (UO_2)_3(PO_4)_2x6H_2O, (UO_2)_3(PO_4)_2x4H_2O, and (UO_2)_3(PO_4)_2xH_2O. Their thermal stability has been studied. It is shown that thermal dehydration of high-water hydrates at 220-240 deg C gives (UO_2)_3(PO_4)_2xH_2O. The anion composition and crystal structure of the compound remain constant up to 1000 deg C. The mixture of the composition of U_3O_8xU_3(PO_4)_4 is the final product of decomposition at 1000 deg C. The thermodynamic constants of dehydration processes have been calculated. A conclusion has been made about the polymer structure of the compound in which water is located between the uranylphosphate layers.

244

Control of adsorption by microwave irradiation; Maikuroha nado wo mochiita gas no kyuchaku datsuri seigyo  

Energy Technology Data Exchange (ETDEWEB)

Introduced herein is microwave irradiation for the adsorption and desorption of environmental pollutants. Microwaves may be used in two ways, other than through elevation of temperature of a system as a whole with the adsorbent such as activated carbon serving as the heating medium. The first is the application by which desorption is caused to take place of specified molecules. For example, zeolite that has adsorbed water is regenerated when it is irradiated with microwaves in a stream of cooling gas. This is because only the moisture is heated since zeolite is a non-carbon adsorbent that absorbs microwaves but a little. Another case is reported in which microwaves are utilized to desorb H2S, H2O, CO, etc., from molecular sieves. In the second application, coexisting materials different in absorptivity are exposed to irradiation. The adsorption of microwave-absorbent materials is inhibited while that of ...

1997-01-25

245

+ 2004 - The NASA Glenn Research Center Technical Report Server  

Science.gov (United States)

May 31, 2011 ... Synthesis and Structural Characterization of a Novel Indium Mercapto Derivative [Clln(SCH2(CO)O)2]2-[(4-MepyH)2]2+. 284. System Mass ...

248

The interaction of trazodone with rat brain muscarinic cholinoceptors.  

UK PubMed Central (United Kingdom)

The muscarinic receptor binding of trazodone, a new nontricyclic antidepressant, was compared with established tricyclic antidepressants. The ability to inhibit the binding of [3H]-quinuclidinyl benzilate...Full Text Available

1980-01-01

249

The hepcidin-binding site on ferroportin is evolutionarily conserved  

UK PubMed Central (United Kingdom)

SummaryMammalian iron homeostasis is regulated by the interaction of the liver-produced peptide hepcidin and its receptor, the iron transporter ferroportin. Hepcidin binds to...Full Text Available

2008-08-01

250

The androgen receptor governs the execution, but not programming, of male sexual and territorial behaviors  

UK PubMed Central (United Kingdom)

SUMMARYTestosterone and estrogen are essential for male behaviors in vertebrates. How these two signaling pathways interact to control masculinization of the brain and behavior...Full Text Available

2010-04-29

251

THE STIMULATING EFFECT OF GLYCOLS AND THEIR POLYMERS ON THE TARSAL RECEPTORS OF BLOWFLIES  

UK PubMed Central (United Kingdom)

The rejection thresholds of Phormia regina Meigen for twenty-four glycols have been determined. A definite relationship between the concentration of the test material and the distribution...Full Text Available

1948-11-20

252

Site-Specific Methylation of the Promoter Alters Deoxyribonucleic Acid-Protein Interactions and Prevents ...  

Science.gov (United States)

... and R. L. Momparler. DNA methylation of retinoic acid receptor beta in breast cancer and possible therapeutic role of ... ...

253

Role of the 5HT3 Receptor in Alcohol Drinking and ...  

Science.gov (United States)

... Proc Natl Acad Sci USA 97:11032-7 27. Duman RS 2002 Genetics of childhood disorders: XXXIX. Stem cell research, part 3: ...

2005-09-01

254

Role of Obesity in Prostate Cancer Development  

Science.gov (United States)

... estrogen receptor status. Cancer Lett., 253, 291-300. 39. Xin,X ... and resistant mice. Brain Res.Bull., 52, 235-242. 40. Foster,BA ...

2011-04-01

255

Purinergic receptors in the splanchnic circulation  

UK PubMed Central (United Kingdom)

There is considerable evidence that purines are vasoactive molecules involved in the regulation of blood flow. Adenosine is a well known vasodilator that also acts as a modulator of the response to...Full Text Available

2008-09-01

257

Molecular Aspects of Thyroid Hormone Actions  

UK PubMed Central (United Kingdom)

Cellular actions of thyroid hormone may be initiated within the cell nucleus, at the plasma membrane, in cytoplasm, and at the mitochondrion. Thyroid hormone nuclear receptors (TRs) mediate the biological...Full Text Available

2010-04-01

258

Missense mutations in the growth hormone receptor dimerization region in Laron syndrome  

Energy Technology Data Exchange (ETDEWEB)

Laron syndrome (LS) is an autosomal recessively inherited condition characterized by insensitivity to endogenous and exogenous GH. Affected individuals have severe episodes and other characteristic features. GH receptor gene mutations are present in all affected individuals in whom molecular studies have been reported. The GH receptor is a plasma membrane-spanning protein in which the extracellular domain binds circulating GH and the intracellular domain interacts with the JAK-2 kinase and possibly other intracellular signaling molecules. GH receptor dimerization occurs on GH binding and is thought to be required for normal signal transduction. We have studied the GH receptor genes of four unrelated individuals affected with LS from the United States, Italy, Saudi Arabia, and India. We have identified four different missense mutations that alter consecutive amino acids 152 to 155 in or near the ...

1994-09-01

259

Influence of KDEL on the Fate of Trimeric or Assembly-Defective Phaseolin  

UK PubMed Central (United Kingdom)

The tetrapeptide KDEL is commonly found at the C terminus of soluble proteins of the endoplasmic reticulum (ER), and it contributes to their localization by interacting with a receptor that recycles...Full Text Available

2001-05-01

260

Hypothyroidism Enhances Tumor Invasiveness and Metastasis Development  

UK PubMed Central (United Kingdom)

BackgroundWhereas there is increasing evidence that loss of expression and/or function of the thyroid hormone receptors (TRs) could result in a selective advantage for tumor development,...Full Text Available

261

Effect of propylbenzilylcholine mustard on contraction and radioligand binding parameters of muscarinic receptors in guinea pig ileum  

Energy Technology Data Exchange (ETDEWEB)

The receptor occupancy-biological effect relationship for muscarinic receptors in guinea pig ileal smooth muscle has been studied by comparison of radioligand binding and contractile response. Muscarinic receptors in homogenates of ileal smooth muscle were labeled with (/sub 3/H)-1-Quinuclidinyl benzilate. Treatment with propylbenzilylcholine mustard (PrBCM), to inactivate irreversibly muscarinic receptors, caused a large dose dependent rightward shift of the dose-response curve to three agonistic furtrethonium derivatives with a concomitant decrease in maximal response. Using those data, the fraction of receptors remaining unoccupied (q-values) and true affinity constants (-log K/sub A/-values) were calculated. Exposure to 20 or 60 nM PrBCM for 15 minutes resulted in a 39% and a 61% reduction in specific (/sup 3/H)-1-Quinuclidinyl benzilate binding sites respectively to be compared ...

1987-10-26

262

ERG Expression Levels in Prostate Tumors Reflect Functional ...  

Science.gov (United States)

... Title : ERG Expression Levels in Prostate Tumors Reflect Functional Status of the Androgen Receptor (AR) as a Consequence of Fusion of ERG ...

263

Characterization of lymphocyte receptors for glycosaminoglycans.  

UK PubMed Central (United Kingdom)

This paper describes attempts to isolate and characterize glycosaminoglycan (GAG)-binding molecules on the surface of lymphocytes and lymphoma cell lines and relate their expression to splenic and lymph...Full Text Available

1991-02-01

264

Cardioprotection conferred by exercise training is blunted by blockade of the opioid system  

UK PubMed Central (United Kingdom)

OBJECTIVES:To investigate the effect of opioid receptor blockade on the myocardial protection conferred by chronic exercise and to compare exercise training with different strategies...Full Text Available

2011-01-01

265

Carbohydrate-specified endocytosis: localization of ligand in the lysosomal compartment.  

UK PubMed Central (United Kingdom)

Carbohydrate-directed endocytosis is mediated by a receptor, the hepatic binding protein; it is responsible for the clearance of galactose-terminated glycoproteins from the circulation. This process...Full Text Available

1981-11-01

266

Acetylcholine Receptor Binding Characteristics of Snake and ...  

Science.gov (United States)

... Naja oxiana neurotoxin 1, Bungarus multicinctus or-bungarotoxin) and short-chain group (Naja naja atra cobrotoxin, Naja oxiana neurotoxin 11. ...

2011-05-13

267

AN ELECTROPHYSIOLOGICAL ANALYSIS OF THE ACTION OF CARBOHYDRATES ON THE SUGAR RECEPTOR OF THE BLOWFLY*  

UK PubMed Central (United Kingdom)

Measurements of the taste thresholds of blowflies for a wide variety of carbohydrates, presented individually and in combination, showed that the stimulating effects of the compounds are not always...Full Text Available

1969-01-01

268

Synthesis and Structural Characterization of a Novel Indium Mercapto Derivative (Clln(SCH2(CO) O)2)2-((4-MepyH)2)2+.  

Science.gov (United States)

The synthesis and structural characterization of a novel In(III) complex is described. The reaction between InCl3 with sodium mercapto-acetic acid, (NaSCH2(CO)OH) in 4-methylpyridine, (CH3(C5H5N), (4-Mepy)) at 25 C affords (ClIn(SCH2(CO)O)2)2- ((4-MepyH)2...

2004-01-01

269

Structures and luminescent properties of new uranyl-based hybrid materials  

International Nuclear Information System (INIS)

Six uranyl coordination compounds, UO_2(OH)(PYCA) (1), UO_2(PYCA)_2(H_2O).2H_2O (2), UO_2(PIC)_2 (3), UO_2(H_2O)_2(NIC)_2 (4), UO_2(OH)(HINIC)(INIC) (5), and UO_2(PYTAC)_2(H_2O)_2 (6) were grown as single crystals via hydrothermal synthesis (PYCA - pyrazine-2-carboxylate, PIC - picolinate, NIC - nicotinate, INIC - iso-nicotinate, and PYTAC - 2-(pyridin-4-yl)thiazole-5-carboxylate) to study their optical properties. All six compounds have been identified via single crystal X-ray diffraction and fully characterized via powder X-ray diffraction, infrared spectroscopy, UV-Vis spectroscopy, and fluorescence spectroscopy. Three of the complexes, 1, 3, and 6, represent new structures, and their synthesis and structural characterization is detailed within. The structures of 2, 4, and 5 have previously been reported in the ...

2011-06-01

270

Polythermal study of the M(ClO_4)_2-H_2O systems, where M"2 = Mg"2"+, Ca"2"+, Sr"2"+, Ba"2"+  

International Nuclear Information System (INIS)

Crystallization points of aqueous solution of the systems M(ClO_4)_2-H_2O (M"2 = Mg"2"+, Ca"2"+, Sr"2"+, Ba"2"+), depending on the salt concentration, were identified by visual-polythermal method. Relying on model notions on the structure of the electrolyte solutions, specific features of strontium perchlorate solubility polytherm and concentration dependence of the relative dynamic viscosity of the salt aqueous solutions are discussed

2005-03-01

271

Outgassing study of thin films used for poly-SiGe based vacuum packaging of MEMS  

British Library Electronic Table of Contents (United Kingdom)

Thermal desorption spectroscopy (TDS) was used to study outgassing from polycrystalline SiGe (poly-SiGe), SiC and SiO"2 films used for poly-SiGe-based MEMS thin film vacuum package technology. Primary desorption products were found to be H"2, H"2O and CO"2. The CO"2 outgassing could be correlated with CF"4 plasma interface cleaning used for thick SiGe PECVD, which can leave carbon at the CF"4-plasma-cleaned interface.

2011-01-01

272

Carbon monoxide - hydrogen combustion characteristics in severe accident containment conditions. Final report  

International Nuclear Information System (INIS)

Carbon monoxide can be produced in severe accidents from interaction of ex-vessel molten core with concrete. Depending on the particular core-melt scenario, the type of concrete and geometric factors affecting the interaction, the quantities of carbon monoxide produced can vary widely, up to several volume percent in the containment. Carbon monoxide is a combustible gas. The carbon monoxide thus produced is in addition to the hydrogen produced by metal-water reactions and by radiolysis, and represents a possibly significant contribution to the combustible gas inventory in the containment. Assessment of possible accident loads to containment thus requires knowledge of the combustion properties of both CO and H_2 in the containment atmosphere. Extensive studies have been carried out and are still continuing in the nuclear industry to assess the threat of hydrogen in a severe reactor accident. However the contribution of carbon monoxide to the ...

1994-10-19

273

Visualization of inositol 1,4,5-trisphosphate receptors on the nuclear envelope outer membrane by deep etching electron microscopy  

UK PubMed Central (United Kingdom)

SummaryThe receptors for the second messenger InsP3 comprise a family of closely related ion channels that release Ca2+ from intracellular stores, most prominently...Full Text Available

2010-09-01

274

The Expression Level of CB1 and CB2 Receptors Determines Their Efficacy at Inducing Apoptosis in Astrocytomas  

UK PubMed Central (United Kingdom)

BackgroundCannabinoids represent unique compounds for treating tumors, including astrocytomas. Whether CB1 and CB2 receptors mediate this therapeutic effect...Full Text Available

275

The C'-terminal interaction domain of the thyroid hormone receptor confers the ability of the DNA site to dictate positive or negative transcriptional activity  

Energy Technology Data Exchange (ETDEWEB)

To investigate mechanisms responsible for positive and negative transcriptional control, the authors have utilized two types of promoters that are diffferentially regulated by thyroid hormone (T{sub 3}) receptors. Promoters containing the palindromic T{sub 3} response element TCAGGTCA TGACCTGA are positively regulated by the T{sub 3} receptor after the administration of T{sub 3}, whereas otherwise identical promoters containing the estrogen response element TCAGGTCA CTG TGACCTGA can be regulated negatively; converse effects are observed with the estrogen receptor. They describe evidence that the transcriptional inhibitory effects of the T{sub 3} or estrogen receptors on the estrogen or T{sub 3} response elements, respectively, are imposed by amino acid sequences in the C'-terminal region that colocalize with dimerization and hormone-binding domains and that these sequences can transfer ...

1990-10-01

276

Synergistic epigenetic reactivation of estrogen receptor-? (ER?) by combined green tea polyphenol and histone deacetylase inhibitor in ER?-negative breast cancer cells  

UK PubMed Central (United Kingdom)

BackgroundThe status of estrogen receptor-α (ERα) is critical to the clinical prognosis and therapeutic approach in breast cancer. ERα-negative breast cancer...Full Text Available

277

Selective stimulation of catecholamine release from bovine adrenal chromaffin cells by an ionotropic purinergic receptor sensitive to 2-methylthio ATP  

UK PubMed Central (United Kingdom)

Background2-Methylthioadenosine 5'-triphosphate (2-MeSATP), formerly regarded as a specific P2Y (metabotropic) purinergic receptor agonist, stimulates Ca2+ influx and...Full Text Available

278

Ryanodine produces a low frequency stimulation-induced NMDA receptor-independent long-term potentiation in the rat dentate gyrus in vitro.  

UK PubMed Central (United Kingdom)

1. The induction of long-term potentiation (LTP) was investigated in the rat dentate gyrus in the presence of ryanodine, an agent which is known to selectively bind to the ryanodine receptor (RyR) Ca2+...Full Text Available

1996-09-15

279

Roles of the TNF receptor-associated factor (TRAF)2/3 binding site in differential B cell signaling by CD40 and its viral oncogenic mimic, latent membrane protein 1 (LMP1)  

UK PubMed Central (United Kingdom)

The Epstein-Barr virus protein, LMP1, is a functional mimic of the cellular receptor CD40, but signals to B lymphocytes in an amplified and sustained manner compared to CD40. LMP1 contributes...Full Text Available

2009-09-01

280

Reduced expression of a human V beta 6.1 T-cell receptor allele.  

UK PubMed Central (United Kingdom)

We have previously described an allelic polymorphism in the V beta 6.1 T-cell receptor gene. The V beta 6.1B allele is associated with disease in a subgroup of patients with juvenile rheumatoid arthritis....Full Text Available

1993-05-15

281

Prolactin and Its Receptor Are Expressed in Murine Hair Follicle Epithelium, Show Hair Cycle-Dependent Expression, and Induce Catagen  

UK PubMed Central (United Kingdom)

Here, we provide the first study of prolactin (PRL) and prolactin receptor (PRLR) expression during the nonseasonal murine hair cycle, which is, in contrast to sheep, comparable with the human scalp...Full Text Available

2003-05-01

282

Pore properties and pharmacological features of the P2X receptor channel in airway ciliated cells  

UK PubMed Central (United Kingdom)

Airway ciliated cells express an ATP-gated P2X receptor channel of unknown subunit composition (P2Xcilia) which is modulated by Na+ and by long exposures to ATP. P2Xcilia...Full Text Available

2006-03-15

283

Pharmacokinetics and pharmacodynamics of terbogrel, a combined thromboxane A2 receptor and synthase inhibitor, in healthy subjects  

UK PubMed Central (United Kingdom)

AimsTo characterize the pharmacokinetics of terbogrel, a new combined thromboxane A2 (TxA2) receptor and synthase inhibitor, in healthy human subjects after...Full Text Available

2004-07-01

284

Neuroactive steroids have multiple actions to potentiate GABAA receptors  

UK PubMed Central (United Kingdom)

The effects of neuroactive steroids on the function of GABAA receptors were studied using cell-attached records of single channel activity recorded from HEK293 cells transfected with α1...Full Text Available

2004-07-01

285

Myocardial metabolic regulation through peroxisome proliferator-activated receptor alpha after myocardial infarction  

UK PubMed Central (United Kingdom)

Although peroxisome proliferator-activated receptor alpha (PPARα) is closely associated with myocardial fatty acid metabolism, the pathophysiological role of PPARα in myocardial infarction...Full Text Available

2003-01-01

286

Molecular recognition of nitrated fatty acids by PPAR[gamma  

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.

2010-03-08

287

Low concentrations of primaquine inhibit degradation but not receptor-mediated endocytosis of asialoorosomucoid by HepG2 cells  

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 ...

1991-02-01

288

Low concentrations of primaquine inhibit degradation but not receptor-mediated endocytosis of asialoorosomucoid by HepG2 cells  

International Nuclear Information System (INIS)

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 ...

289

Immunohistochemical localization of low density lipoprotein receptor-related protein 1 and ?2-Macroglobulin in retinal and choroidal tissue of proliferative retinopathies  

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

2010-08-01

290

Growth differentiation factor-9 stimulates progesterone synthesis in granulosa cells via a prostaglandin E2/EP2 receptor pathway  

UK PubMed Central (United Kingdom)

Growth differentiation factor-9 (GDF-9), an oocyte-secreted member of the transforming growth factor β superfamily, progesterone receptor, cyclooxygenase 2 (Cox2; Ptgs2), and the EP2 prostaglandin...Full Text Available

2000-08-29

291

Enhanced ?2-adrenergic receptor (?2AR) signaling by adeno-associated viral (AAV)-mediated gene transfer  

UK PubMed Central (United Kingdom)

Backgroundβ2-Adrenergic receptors2AR) play important regulatory roles in a variety of cells and organ systems and are important therapeutic...Full Text Available

292

Discordant expression and variable numbers of neighboring GGA- and GAA-rich triplet repeats in the 3' untranslated regions of two groups of messenger RNAs encoded by the rat polymeric immunoglobulin receptor gene.  

UK PubMed Central (United Kingdom)

An unusual S1-nuclease sensitive microsatellite (STMS) has been found in the single copy, rat polymeric immunoglobulin receptor gene (PIGR) terminal exon. In Fisher rats, elements within or beyond the...Full Text Available

1995-04-11

293

Decay-accelerating factor CD55 is identified as the receptor for echovirus 7 using CELICS, a rapid immuno-focal cloning method.  

UK PubMed Central (United Kingdom)

Using an anti-receptor mAb that blocks the attachment of echovirus 7 and related viruses (echoviruses 13, 21, 29 and 33), we have isolated a complementary DNA clone that encodes the human decay-accelerating...Full Text Available

1994-11-01

294

Cumulus expansion, nuclear maturation and connexin 43, cyclooxygenase-2 and FSH receptor mRNA expression in equine cumulus-oocyte complexes cultured in vitro in the presence of FSH and precursors for hyaluronic acid synthesis  

UK PubMed Central (United Kingdom)

The aim of this study was to investigate cumulus expansion, nuclear maturation and expression of connexin 43, cyclooxygenase-2 and FSH receptor transcripts in equine cumuli oophori during in vivo and...Full Text Available

295

CD5 Is Dissociated from the B-Cell Receptor in B Cells from Bovine Leukemia Virus-Infected, Persistently Lymphocytotic Cattle: Consequences to B-Cell Receptor-Mediated Apoptosis  

UK PubMed Central (United Kingdom)

Bovine leukemia virus (BLV), a retrovirus related to human T-cell leukemia virus types 1 and 2, can induce persistent nonneoplastic expansion of the CD5+ B-cell population, termed...Full Text Available

2001-02-01

296

Blockade of androgen receptors is sufficient to alter the sexual differentiation of the substantia nigra pars reticulata seizure-controlling network  

UK PubMed Central (United Kingdom)

The substantia nigra pars reticulata (SNR) controls seizures in a sex-specific manner. At postnatal day 15 (P15), SNR infusion of GABAA receptor agonist muscimol have proconvulsant...Full Text Available

2008-03-01

297

Autocrine regulation of T-cell activation by ATP release and P2X7 receptors  

UK PubMed Central (United Kingdom)

T-cell activation requires the influx of extracellular calcium, although mechanistic details regarding such activation are not fully defined. Here, we show that P2X7 receptors play a key...Full Text Available

2009-06-01

298

Assessment of Glucagon-Like Peptide-1 Analogue and Renin Inhibitor on the Binding and Regulation of GLP-1 Receptor in Type 1 Diabetic Rat Hearts  

UK PubMed Central (United Kingdom)

This study focuses on the effects of long-term renin-angiotensin system suppression and/or incretin mimetic therapies on the regulation and binding affinity of GLP-1 to its receptor in the coronary...Full Text Available

2011-01-01

299

An activated renin-angiotensin system maintains normal blood pressure in aryl hydrocarbon receptor heterozygous mice but not in null mice  

UK PubMed Central (United Kingdom)

It has been postulated that fetal vascular abnormalities in aryl hydrocarbon receptor null (ahr−/−) mice may alter cardiovascular homeostasis in adulthood....Full Text Available

2010-07-15

300

Adenosine A1 receptors (A1Rs) play a critical role in osteoclast formation and function  

UK PubMed Central (United Kingdom)

Adenosine regulates a wide variety of physiological processes via interaction with one or more G-protein-coupled receptors (A1R, A2AR, A2BR, and A3R)....Full Text Available

2010-07-01

301

Acute Ca2+-Dependent Desensitization of 5-Ht1A Receptors is Mediated by Activation of Pka in Rat Serotonergic Neurons  

UK PubMed Central (United Kingdom)

This report investigates acute changes in the sensitivity of 5-HT1A receptors in dorsal raphe (dr) neurons in response to elevated serotonin. DR neurons were isolated from adult rats...Full Text Available

2010-08-11

302

?1-Fetoprotein Transcription Factor (FTF)/Liver Receptor Homolog-1 (LRH-1) Is an Essential Lipogenic Regulator  

UK PubMed Central (United Kingdom)

α1-Fetoprotein transcription factor (FTF), also known as liver receptor homolog 1 (LRH-1) is highly expressed in liver and intestine, where it is implicated in the regulation...Full Text Available

2010-04-01

303

(-)-Epigallocatechin Gallate Regulates CD3-mediated T Cell Receptor Signaling in Leukemia through the Inhibition of ZAP-70 Kinase*  

UK PubMed Central (United Kingdom)

The ζ chain-associated 70-kDa protein (ZAP-70) of tyrosine kinase plays a critical role in T cell receptor-mediated signal transduction and the immune response. A high level of ZAP-70 expression...Full Text Available

2008-10-17

304

["3H]QNB binding and contraction of rabbit colonic smooth muscle cells  

International Nuclear Information System (INIS)

The authors used radioligand binding and studies of cell contraction to characterize muscarinic receptors on dispersed smooth muscle cells from rabbit proximal and distal colon. Cells obtained after serial incubations in collagenase were used to measure binding of tritiated quinuclidinyl benzilate (["3H]QNB). At 37 degree C, specific ["3H]QNB binding was saturable and linearly related to cell number. Nonlinear regression analysis was used to determine the affinity of ["3H]QNB for its receptor. The IC_5_0 for the muscarinic agonists bethanechol and oxotremorine were 80 and 0.57 #mu#M, respectively. Hill coefficients were 0.67 for both, suggesting more complex interaction involving receptors of different affinities. In studies of cell contraction, bethanechol stimulated a dose-dependent decrease in cell length with half the maximal contraction occurring at 100 pM. These results suggest that (1) contraction is mediated by ...

1987-01-01

305

Temporal development of GABA agonist induced alterations in ultrastructure and GABA receptor expression in cultured cerebellar granule cells  

DEFF Research Database (Denmark)

The temporal development of the effect of THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) on the ultrastructure composition and GABA receptor expression in cerebellar granule cells was investigated by quantitative electron microscopy (morphometric analysis) and GABA binding assays. It was found that the cytoplasmic density of smooth endoplasmic reticulum was decreased, while the cytoplasmic density of rough endoplasmic reticulum, Golgi apparatus, vesicles and coated vesicles was greatly enhanced after exposure of the cells to THIP (150 microM) for only 1 hr. In cerebellar granule cells exposed to THIP (150 microM) for 3 hr low affinity GABA receptors were induced. These findings show that the effect of THIP on the ultrastructure composition and GABA receptor expression in cultured cerebellar granule cells may be interrelated and moreover it is likely that the turn-over of GABA receptors is ...

1987-01-01

306

Radioiodination of chicken luteinizing hormone without affecting receptor binding potency  

Energy Technology Data Exchange (ETDEWEB)

By improving the currently used lactoperoxidase method, we were able to obtain radioiodinated chicken luteinizing hormone (LH) that shows high specific binding and low nonspecific binding to a crude plasma membrane fraction of testicular cells of the domestic fowl and the Japanese quail, and to the ovarian granulosa cells of the Japanese quail. The change we made from the original method consisted of (1) using chicken LH for radioiodination that was not only highly purified but also retained a high receptor binding potency; (2) controlling the level of incorporation of radioiodine into chicken LH molecules by employing a short reaction time and low temperature; and (3) fractionating radioiodinated chicken LH further by gel filtration using high-performance liquid chromatography. Specific radioactivity of the final {sup 125}I-labeled chicken LH preparation was 14 microCi/micrograms. When specific binding was 12-16%, nonspecific binding was as low as 2-4% in the ...

1989-12-01

307

Chromosomal localization of the human retinoid X receptors  

Energy Technology Data Exchange (ETDEWEB)

The recently described retinoid X receptors (RXRs) respond to the novel retinoid 9-cis-retinoic acid and also serve as heterodimeric partners for the vitamin D, thyroid hormone, and retinoic acid receptors (VDR, TR, and RAR, respectively). In this work, the authors report high-resolution localization of the human RXR genes within cytogenetic bands and also within a standard reference map of cosmid DNA markers on human chromosomes. They have determined the location of the human RXR genes by pairwise hybridization of the RXR cosmids and reference markers, using fluorescence in situ hybridization. They localized (i) RXR[alpha] (RXRA) to chromosome 9 band q34.3; (ii) RXR[beta] (RXRB) to chromosome 6 band 21.3; and (iii) RXR[gamma] (RXRG) to chromosome 1 band q22-q23. Six retinoid-responsive transcription factors have been identified so far, including three retinoic acid receptors in addition to the three RXRs. Interestingly, ...

1994-04-01

308

Formation of double hafnium sulfates in the systems HfO"2-H"2SO"4-Me"2SO"4-H"2O (Me-Na, K, Rb, Cs and NH"4)  

International Nuclear Information System (INIS)

Influence of alkali elements on formation, composition, solubility and region of stability of complex hafnium sulfates, separated in the HfO"2-H"2SO"4-Me"2SO"4-H"2O (Me-Na, K, Rb, Cs and NH"4 group) systems is studied. In all cases hafnium forms the complex sulfates of three types differing by basicity or ratio HfO"2:SO"3 1:1, 1:1.5, 1:2. Three basic and three medium sulfates are crystallized in the systems with sodium; with rubidium, cesium and ammonium - two basic and two medium sulfates and with potassium - two basic and one medium salts. Anhydrous salts do not form in the investigated systems. Potassium salt approximately 0.3% according to HfO"2 is characterized by minimum solubility from the salts of 2HfOSO"4x(1-3)Me"2SO"4x(4-6)xH"2O while solubility of the same salts with rubidium, cesium and sodium increases from (0.25-1.0); (0.5-1.5) till (1.0-5)% ...

1982-01-01

309

Effect of N_2 + H_2 gas mixtures in plasma nitriding on tribological properties of duplex surface treated steels  

International Nuclear Information System (INIS)

Thermo-reactive diffusion chromizing followed by pulsed plasma nitriding were carried out on AISI 52100 and 8620 bearing steels. The chromized samples were pulse-plasma nitrided for 5 h at 500 deg. C in various N_2-H_2 gas mixtures. The coated steels were characterized using scanning electron microscopy, X-ray diffraction and microhardness testing. The unlubricated wear behaviors of only chromized and duplex treated steels were investigated in ball-on-disc system tests at room temperature. X-ray diffraction patterns of the duplex treated samples containing H_2 indicated the formation of dominant CrN and Cr_2N nitrides as well as the formation of Cr_3C_2 and Cr_7C_3 carbides. Gas mixtures in the plasma nitriding, which was performed after chromizing, have a significant influence on the wear rate of the duplex treated steels. The wear and friction tests showed that the lowest friction coefficient and wear ...

2008-12-01

310

Comparative investigation on chemical looping combustion of coal-derived synthesis gas containing H2S over supported NiO oxygen carriers  

Energy Technology Data Exchange (ETDEWEB)

Chemical looping combustion (CLC) of simulated coal-derived synthesis gas was conducted with NiO oxygen carriers supported on SiO2, ZrO2, TiO2, and sepiolite. The effect of H2S on the performance of these samples for the CLC process was also evaluated. Five-cycle thermogravimetric analysis (TGA) tests at 800 C indicated that all oxygen carriers had a stable performance at 800 C, except NiO/SiO2. Full reduction/oxidation reactions of the oxygen carrier were obtained during the five-cycle test. It was found that support had a significant effect on reaction performance of NiO both in reduction and oxidation rates. The reduction reaction was significantly faster than the oxidation reaction for all oxygen carriers, while the oxidation reaction is fairly slow due to oxygen diffusion on NiO layers. The reaction profile was greatly affected by the presence of H2S, but there was no effect on the capacity due to ...

2010-01-01

311

ARM AND INTERARM STAR FORMATION IN SPIRAL GALAXIES  

International Nuclear Information System (INIS)

We investigate the relationship between spiral arms and star formation in the grand-design spirals NGC 5194 and NGC 628 and in the flocculent spiral NGC 6946. Filtered maps of near-IR (3.6 #mu#m) emission allow us to identify 'arm regions' that should correspond to regions of stellar mass density enhancements. The two grand-design spirals show a clear two-armed structure, while NGC 6946 is more complex. We examine these arm and interarm regions, looking at maps that trace recent star formation-far-ultraviolet (GALEX NGS) and 24 #mu#m emission (Spitzer SINGS)-and cold gas-CO (HERACLES) and H I (THINGS). We find the star formation tracers and CO more concentrated in the spiral arms than the stellar 3.6 #mu#m flux. If we define the spiral arms as the 25% highest pixels in the filtered 3.6 #mu#m images, we find that the majority (60%) of star formation tracers occur in the interarm regions; this result persists qualitatively even when considering the potential impact of finite data ...

2010-12-10

312

Reduction of cadmium toxicity to green microalga Stichococcus bacillaris by manganese  

Energy Technology Data Exchange (ETDEWEB)

Investigations of cadmium toxicity to microorganisms are now more concerned with the interactions of cadmium with different environmental factors and other metals. The interactions are complex and have not been thoroughly studied yet. Metal interactions may assume the form of synergism characterized by increase in toxicity, but also of antagonism in which one metal reduces the toxicity of another. Apart from cadmium interactions with such toxic metals as mercury and lead, interactions of cadmium with the essential trace elements seem to be very interesting because it has been assumed that algal cells take up cadmium by the system transporting these elements. A previous study showed that cadmium transport into Stichococcus bacillaris cells was inhibited by Mn/sup 2 +/ ions. Thus, it can be supported that there exist some possibilities of using those ions antagonistic to cadmium as counterposition. Showing those possibilities was the aim of the present paper.

1988-12-01

313

Histone deacetylase inhibitors and transforming growth factor-b induce 15-hydroxyprostaglandin dehydrogenase expression in human lung adenocarcinoma cells  

British Library Electronic Table of Contents (United Kingdom)

Histone deacetylase (HDAC) inhibitors have been actively exploited as potential anticancer agents. To identify gene targets of HDAC inhibitors, we found that HDAC inhibitors such as sodium butyrate, scriptaid, apicidin and oxamflatin induced the expression of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), a potential cyclooxygenase-2 (COX-2) antagonist and tumor suppressor, in a time and concentration dependent manner in A549 and H1435 lung adenocarcinoma cells. Detailed analyses indicated that HDAC inhibitors activated the 15-PGDH promoter-luciferase reporter construct in transfected A549 cells. A representative HDAC inhibitor, scriptaid, and its negative structural analog control, nullscript, were further evaluated at the chromatin level. Scriptaid but not nullscript induced a signific...

2006-01-01

314

Environmental analysis of endocrine disrupting effects from hydrocarbon contaminants in the ecosystem. 1997 annual progress report  

Energy Technology Data Exchange (ETDEWEB)

'The overall objective of the basic research grant is to characterize the potential of common hydrocarbon contaminants in ecosystems to act as endocrine disruptors. The three major lines of research include (1) a biotechnology based screening system to identify potential hormone mimics and antagonists; (2) an animal screening system to identify biomarkers of endocrine effects. and (3) a literature review to identify compounds at a variety of DOE sites that need to be examined for endocrine disrupting effects. By relating results obtained from this research project to contamination problems at various DOE sites. CBR will provide data and information on endocrine disrupting contaminants to DOE for consideration in risk analyses for determining clean-up levels and priorities needed at the sites.'

1997-01-01

315

Endophytic fungus Trichothecium roseum LZ93 antagonizing pathogenic fungi in vitro and its secondary metabolites  

British Library Electronic Table of Contents (United Kingdom)

The endophytic fungus Trichothecium roseum LZ93 from Maytenus hookeri was found to antagonize other pathogenic fungi in vitro. To identify which compound contributed substantially to the antagonism, we fermented the strain and purified its fermentation products. Eleven compounds were obtained, including two trichothecenes, five rosenonolactones, two cardiotonic cyclodepsipeptides, and two sterols. Compound 11?-hydroxyrosenonolactone (1) was assigned according to 1D and 2D-NMR data for the first time. At the same time, the 1H and 13C-NMR assignments for 6?-hydroxyrosenonolactone (2) were revised. Of all of them, only trichothecin (6) showed strong antifungal activity. Based on our observations of the antagonistic activity and the other experimental results, we suggest that the antifungal co...

2010-01-01

316

Development of a detailed kinetic model for gasoline surrogate fuels  

Energy Technology Data Exchange (ETDEWEB)

A detailed chemical kinetic model to describe the autoignition of gasoline surrogate fuels is presented consisting of the fuels iso-octane, n-heptane, toluene, diisobutylene and ethanol. Model predictions have been compared with shock tube ignition delay time data for surrogates of gasoline over practical ranges of temperature and pressure, and the model has been found to be sensitive to both changes in temperature and pressure. Moreover, the model can qualitatively predict the observed synergistic and antagonistic non-linear blending behaviour in motor octane number (MON) for different combinations of primary reference fuels (PRFs) and non-PRFs by correlating calculated autoignition delay times from peak pressures and temperatures in the MON test to experimental MON values. The reasons for the blending behaviour are interpreted in terms autoignition chemistry. 37 refs., 11 figs., 4 tabs.

2008-08-15

317

Afferent mechanisms of microwave-induced biological effects. Annual report, 1 June 1985-31 May 1986  

Energy Technology Data Exchange (ETDEWEB)

Effects of 2450-MHz circularly polarized microwave irradiation on central nervous system functions were studied. Pulsed (microsecond, 500 pps) microwaves decreased high-affinity sodium-dependent choline uptake in the hippocampus and frontal cortex of the rat. The effect on hippocampal choline uptake was blocked by pretreatment with narcotic antagonists. Continuous-wave microwaves of the same power density decreased choline uptake in the frontal cortex only. Furthermore, it was found that the effects of pulsed microwaves on central cholinergic activity are classically conditionable to cues in the exposure environment. The hypothesis that some of the neurological effects of pulsed microwave irradiation are caused by its effect on the auditory system was investigated. Effects of pink noise and pulsed microwaves were compared.

1986-07-01

318

Use of receptor affinity chromatography in purification of the growth hormone-like factor produced by plerocercoids of the tapeworm Spirometra mansonoides.  

Science.gov (United States)

The plerocercoid stage of the tapeworm Spirometra mansonoides produces a functional analog of human growth hormone (hGH). Among the similarities between plerocercoid growth factor (PGF) and hGH is competition for the same receptors on rabbit liver membranes. To take advantage of this characteristic in a purification scheme for PGF, rabbit liver microsomes were solubilized in Triton X-100 and the hGH receptors were purified over an hGH affinity column. The purified receptors from six rabbit livers were coupled to Affi-Gel-10 to create a receptor affinity column which was used to purify PGF. Chromatography of crude PGF over the receptor column resulted in a 1044 fold increase in specific activity. SDS-PAGE in the presence of 2-mercaptoethanol showed that the affinity-purified PGF contained three protein bands with apparent Mrs of 27.5 K, 22 K, and 16.7 K. Injections of the ...

1988-01-01

319

Topographical distribution of decrements and recovery in muscarinic receptors from rat brains repeatedly exposed to sublethal doses of soman  

Energy Technology Data Exchange (ETDEWEB)

(3H)Quinuclidinyl benzilate binding to rat brain muscarinic receptors decreased after repeated exposure to soman, a potent organophosphorus cholinesterase inhibitor. The topographical distribution of this decrement was analyzed by quantitative receptor autoradiography. After 4 weeks of soman, three times a week, quinuclidinyl benzilate binding decreased to 67 to 80% of control in frontal and parietal cortex, caudate-putamen, lateral septum, hippocampal body, dentate gyrus, superior colliculus, nucleus of the fifth nerve, and central grey. Minor or no decreases were observed in thalamic or hypothalamic nuclei, reticular formation, pontine nuclei, inferior colliculus, nucleus of the seventh nerve, and cerebellum. Scatchard analyses of saturation curves using frontal cortex sections from soman-treated rats revealed a decrease in maximal quinuclidinyl benzilate binding from that in control rats and a return toward control levels by 24 days without ...

1984-08-01

320

Topographical distribution of decrements and recovery in muscarinic receptors from rat brains repeatedly exposed to sublethal doses of soman  

International Nuclear Information System (INIS)

[3H]Quinuclidinyl benzilate binding to rat brain muscarinic receptors decreased after repeated exposure to soman, a potent organophosphorus cholinesterase inhibitor. The topographical distribution of this decrement was analyzed by quantitative receptor autoradiography. After 4 weeks of soman, three times a week, quinuclidinyl benzilate binding decreased to 67 to 80% of control in frontal and parietal cortex, caudate-putamen, lateral septum, hippocampal body, dentate gyrus, superior colliculus, nucleus of the fifth nerve, and central grey. Minor or no decreases were observed in thalamic or hypothalamic nuclei, reticular formation, pontine nuclei, inferior colliculus, nucleus of the seventh nerve, and cerebellum. Scatchard analyses of saturation curves using frontal cortex sections from soman-treated rats revealed a decrease in maximal quinuclidinyl benzilate binding from that in control rats and a return toward control levels by 24 days without ...

1984-01-01

321

Regulation of NMDA and AMPA receptors during the maturation phase of chicken brain development  

International Nuclear Information System (INIS)

Full text: The maturation of chicken forebrain is protracted and occurs well after synapse formation providing a good model for studying mechanisms of brain maturation. Using microslices from immature (10 day) and adult chicken forebrain prepared after decapitation, we have examined functional properties of NMDA and AMPA receptors by measuring agonist-induced uptake of "4"5Ca"2"+ . The rate and extent of NMDA induced "4"5Ca"2"+ accumulation decreased during maturation with no change in EC_5_0. The rate and extent of the AMPA induced response also decreased with a 60-fold increase in EC_5_0. However, the total NMDA receptor content did not change as indicated by 3 H-MK801 binding and NR1 immunoreactivity in P2 fractions. Similarly, there was no change in the B_m_a_x of "3H-AMPA, though there was a two-fold increase in K_D, and little or no change in the immunoreactivity in GluR1, 2, 2/3 or 4. These results suggest that it is the regulation of ...

2002-02-04

322

Natriuretic peptides in vascular physiology and pathology.  

Science.gov (United States)

Four major natriuretic peptides have been isolated: atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), C-type natriuretic peptide (CNP), and Dendroaspis-type natriuretic peptide (DNP). Natriuretic peptides play an important role in the regulation of cardiovascular homeostasis maintaining blood pressure and extracellular fluid volume. The classical endocrine effects of natriuretic peptides to modulate fluid and electrolyte balance and vascular smooth muscle tone are complemented by autocrine and paracrine actions that include regulation of coronary blood flow and, therefore, myocardial perfusion; modulation of proliferative responses during myocardial and vascular remodeling; and cytoprotective anti-ischemic effects. The actions of natriuretic peptides are mediated by the specific binding of these peptides to three cell surface receptors: type A natriuretic peptide receptor (NPR-A), type B natriuretic peptide ...

2008-01-01

323

Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells.  

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 ...

2008-07-30

324

Synthesis, crystallographic data, solubility and electrokinetic properties of copper-, nickel- and cobalt-uranylphosphate  

International Nuclear Information System (INIS)

A discussion is given concerning the transformation in acid medium of curite into copper-, nickel- and cobalt-uranylphosphate. From chemical, differentiel thermal and thermogravimetric analyses, the crystal-chemical formula are calculated as: Cu(UO_2/PO_4)_2.8H_2O, Ni(UO_2/PO_4)_2.7H_2O and Co(UO_2/PO_4)_2.7H_2O. The two last compounds crystallize in the triclinic system with space group P1 or P1(overscore) and the first one crystallizes in the tetragonal system with space group P4/nmm. The cell parameters are calculated. From solubility data, the solubility products are computed as 10sup(-12.8), 10sup(-9.5) and 10sup(-9.9) for the copper-, nickel- and colbalt-compound respectively. The electrokinetic properties of the three species are closely similar to those of natural meta-torbernite: the zeta-potential is negative and the point of zero charge be reached ...

325

Spectrophotometric determination of vanadium(V) with 2-carbethoxy-5-hydroxy-1-(4-tolyl)-4-pyridone  

International Nuclear Information System (INIS)

Vanadium(V) in aqueous HCl, HNO_3 or H_2SO_4 solutions is extracted with 2-carbethoxy-5-hydroxy-1-(4-tolyl)-4-pyridone (HA) dissolved in CHCl_3 and determined spectrophotometrically, Depending on the composition of the aqueous phase, two complexes are formed. At pH 1 (HCl, HNO_3, H_2SO_4) VO_2A(HA)_2 is formed with maximal absorption at 478 nm. However, from 4-5 M HCl, VO_2Cl(HA)_3 is extracted, and has maximal absorption at 615 nm. The same complex is extracted from 2-3 M HNO_3 or 3-4 M H_2SO_4 if enough chloride is added. Solutions of both complexes follow Beer's law and the molar extinction coefficients are 4.15x10"3 1.mole"-"1cm"-"1 at 478 nm and 5.10x10"3 at 615 nm. The determination of vanadium at both wavelengths is very simple, fast and selective. The composition of the complexes was established by the usual methods as well as by characterization of the ...

1975-01-01

326

Rapid Responding Palladium-Silver Surface Modified Microsensor for Hydrogen  

Science.gov (United States)

Most palladium thin film based hydrogen gas sensors have response and recovery times that are too long to make them useful in vehicular and stationary gas leak detection applications. In contrast, a palladium-silver thin film based microcantilever (MC) hydrogen gas microsensor is reported herein with near ideal response characteristics for use in these hydrogen economy related applications. Specifically, 3-10 second response and recovery times have been measured for these sensors in contrast to previous sensor response measurements of several to tens of minutes using Pd thin film and MC based sensing techniques. The much reduced response times observed in the present study are attributed to a wet chemical Pd-Ag thin film deposition technique and a gas conditioning protocol that produces a highly nanostructured, porous film that rapidly adsorbs and desorbs H2, allowing rapid equilibration with the H2 ...

2010-01-01

327

Pitting corrosion resistance of high-alloy OCTG in CO_2 environment as affected by chlorides and sulfides  

International Nuclear Information System (INIS)

High general corrosion resistance of high-alloy OCTG (oil country tubular goods) to CO_2 may be limited by pitting corrosion in presence of chlorides and sulfides. The pitting resistance of 13% Cr steel, duplex and high Ni austenitic stainless steels have been examined by electrochemical measurements in a high temperature, high pressure autoclave simulating the well conditions. Each steel shows the pitting potential in CO_2-NaCl-H_2O system, the value of which being less noble as the Cl"- concentration and the temperature increase. The presence of H_2S is also detrimental. High alloying additions of Cr and Mo enhance pitting resistance whether or not H_2S is present. The corrosion potentials of these steels in the simulating well conditions in which oxygen is absent do not exceed the pitting potential. Therefore, pitting corrosion can not occur by the passivity ...

328

Orion's Bar: Physical Conditions across the Definitive H+ / H0 / H2 Interface  

CERN Document Server

Previous work has shown the Orion Bar to be an interface between ionized and molecular gas, viewed roughly edge on, which is excited by the light from the Trapezium cluster. Much of the emission from any star-forming region will originate from such interfaces, so the Bar serves as a foundation test of any emission model. Here we combine X-ray, optical, IR and radio data sets to derive emission spectra along the transition from H+ to H0 to H2 regions. We then reproduce the spectra of these layers with a simulation that simultaneously accounts for the detailed microphysics of the gas, the grains, and molecules, especially H2 and CO. The magnetic field, observed to be the dominant pressure in another region of the Orion Nebula, is treated as a free parameter, along with the density of cosmic rays. Our model successfully accounts for the optical, IR and radio observations across the Bar by including a ...

2008-01-01

329

Hydrogen evolution reaction on single crystal WO3/C nanoparticles supported on carbon in acid and alkaline solution  

British Library Electronic Table of Contents (United Kingdom)

Single crystal tungsten oxide (WO3) nanoparticles were prepared via a microwave-assisted method. Electrochemical activity for hydrogen evolution reaction (HER) on WO3 supported on carbon black (WO3/C) electrocatalyst was first studied in acid solution (0.5 M H2SO4) and alkaline solution (1.0 M KOH) at room temperature. The overall experimental results revealed that the electrocatalytic activity for HER on WO3/C is one order magnitude higher than those obtained with carbon black in 0.5 M H2SO4 and is six times than in the case of carbon black in 1.0 M KOH. These results demonstrated that WO3 could enhance the electrocatalytic activity for hydrogen evolution reaction in acid solution (0.5 M H2SO4) and alkaline solution (1.0 M KOH). On the other hand, the kinetic reaction mechanisms were disc...

2011-01-01

330

Extended Gas in Seyfert Galaxies Near Infrared Observations of NGC 2110 and Circinus  

CERN Document Server

We present results of near--IR long-slit spectroscopy in the J and K bands of the Seyfert 2 galaxies NGC 2110 and Circinus, investigating the gaseous distribution, excitation, reddening and kinematics. In NGC 2110, the emission line ratio [FeII]/Pa beta increases towards the nucleus (to ~ 7). The nuclear [Fe II]1.257 (microns) and Pa beta lines are broader (FWHM ~ 500 km/s) than the H2 (2.121) line (FWHM ~ 300 km/s). Both these results suggest that shocks, driven by the radio jet, are an important source of excitation of [Fe II]. The H2 excitation appears to be dominated by X-rays from the nucleus. In Circinus, both [FeII]/Pa beta and H2/Br gamma decrease from ~ 2 at 4 arcsec from the nucleus to nuclear values of ~ 0.6 and ~ 1, respectively, suggesting that the starburst dominates the nuclear excitation, while the AGN dominates the excitation further out (r > ...

1998-01-01

331

Electron momentum spectroscopy of H_2 and D_2: Ionization to ground and excited final states  

International Nuclear Information System (INIS)

The symmetric noncoplanar (e,2e) cross sections (momentum profiles) of H_2 and D_2 for the transitions to the 2p#sigma#_u and 2s#sigma#_g excited ion states have been measured, relative to the ground-state ion transition, using a high-sensitivity multichannel momentum-dispersive electron momentum spectrometer (EMS) at an impact energy of 1200 eV. Newly calculated plane-wave impulse approximation (PWIA) cross sections, based on a full-configuration-interaction H_2 wave function, are compared to the experimental results. These calculations are in better agreement with the experimental results for the transition to the 2s#sigma#_g ion state than the earlier theoretical work of Liu and Smith, Jr. [Phys. Rev. A 31, 3003 (1985)] which has been found to be in error. Nevertheless, significant discrepancies between the relative experimental and theoretical cross sections are observed for the transitions to ...

332

Cosmic evolution of the atomic and molecular gas content of galaxies  

CERN Document Server

We study the evolution of the cold gas content of galaxies by splitting the interstellar medium into its atomic and molecular hydrogen components, using the galaxy formation model GALFORM in the LCDM framework. We calculate the molecular-to-atomic hydrogen mass ratio, H2/HI, in each galaxy using two different approaches; the pressure-based empirical relation of Blitz & Rosolowsky and the theoretical model of Krumholz, McKeee & Tumlinson, and apply them to consistently calculate the star formation rates of galaxies. We find that the model based on the Blitz & Rosolowsky law predicts an HI mass function, CO(1-0) luminosity function, correlations between the H2/HI ratio and stellar and cold gas mass, and infrared-CO luminosity relation in good agreement with local and high redshift observations. The HI mass function evolves weakly with redshift, with the number density of high mass galaxies ...

2011-01-01

333

Comparison of plasma chemistries for inductively coupled plasma etching of InGaAlP alloys  

International Nuclear Information System (INIS)

Two plasma chemistries, i.e., CH_4/H_2/Ar and Cl_2/Ar, were compared for the etching of InGaP, AlInP, and AlGaP under inductively coupled plasma (ICP) conditions. While the etching with CH_4/H_2/Ar discharges appears to be ion driven, Cl_2/Ar discharges showed an additional strong chemical enhancement. The highest etch rate (#approx#1 #mu#m/min) for InGaP was achieved at high ICP source power (#>=#750 W) with the Cl_2/Ar chemistry. Cl_2/Ar discharges provided very smooth surfaces in all three materials with root-mean-square roughness measured by atomic force microscopy around 2 nm. This result may be due to the efficient ion-assisted product desorption in this chemistry. The etched near-surface region of InGaP (#approx#100 Angstrom) with Cl_2/Ar maintained almost the same stoichiometry as that of the unetched control. By contrast, the CH_4/H_2/Ar plasma ...

1998-05-01

334

Characterization and reactivity of Fe3O4/FeMnOx core/shell nanoparticles for methylene blue discoloration with H2O2  

British Library Electronic Table of Contents (United Kingdom)

A magnetic core/shell Fe3O4/FeMnOx catalyst was prepared by a simple oxidation-precipitation method. The catalyst was characterized by X-ray diffraction, transmission electron microscope, X-ray photoelectron spectroscopy, Fourier transform infrared spectroscopy, thermogravimetric analysis and cyclic voltammetry. The characterization studies verified that Fe3O4 core was coated with a layer of Fe-Mn oxide. The Fe3O4/FeMnOx was found to be an effective and stable heterogeneous catalyst for the discoloration of methylene blue (MB) in aqueous solution by H2O2. The high catalytic activity is due to the FeMnOx shell, which not only increased the surface hydroxyl groups, but also enhanced the interfacial electron transfer. The discoloration of MB could be due to the decomposition of H2O2 into ?OH ...

2011-01-01

335

Biological Research for Radiation Protection  

International Nuclear Information System (INIS)

The work scope of 'Biological Research for the Radiation Protection' had contained the research about ornithine decarboxylase and its controlling proteins, thioredoxin, peroxiredoxin, S-adenosymethionine decarboxylase, and glutamate decarboxylase 67KD effect on the cell death triggered ionizing radiation and H_2O_2(toxic agents). In this study, to elucidate the role of these proteins in the ionizing radiation (or H_2O_2)-induced apoptotic cell death, we utilized sensesed (or antisensed) cells, which overexpress (or down-regulate) RNAs associated with these proteins biosynthesis, and investigated the effects of these genes on the cytotoxicity caused by ionizing radiation and H_2O_2(or paraquat). We also investigated whether genisteine(or thiamine) may enhance the cytotoxic efficacy of tumor cells caused by ionizing radiation (may enhance the preventing effect ...

336

Anodic Protection performance of Steels ASTM A 516-60 And JIS G 3131 SPHC In Concentrated Sulfuric Acid  

International Nuclear Information System (INIS)

One of the methods to protect a carbon steel material from corrosion attack of sulfuric acid environment is with anodic protection. This research was intended to investigate the effect of anodic protection quickened with potential polarization, The material under investigation were ASTM A 516 and JIS G 3131-SPHC in highly concentrated H_2SO_4 solution. The results showed that potential that was effective for anodic protection in ASTM A 516-60 were at 236-436 mV for 75%, 276-476 mV for 80%, 264-514 mV for 85%,285-485 mV for 90%, and 231-431 mV for 97% H_2SO_4 so that in JlS G 3131-SPHC were at 303 -503 mV for 75%, 290-490 mV for 80%, 269- 516 mV for 85%, 264-514 mV for 90%, and 287 -487 mV for 97% H_2SO_4.

2001-06-01

337

Absolute differential cross sections for the scattering of kilo-electron-volt O atoms  

International Nuclear Information System (INIS)

This paper reports measurements of absolute differential cross sections for the direct scattering of oxygen atoms by He, Ne, Ar, Kr, Xe, H_2, N_2, O_2, CO, CO_2, H_2O, SO_2, NH_3, CH_4, CF_4, and SF_6 targets. The measured cross sections include contributions from all elastic and inelastic processes that result in a fast neutral oxygen atom product. Cross sections are presented for 0.5- and 1.5-keV projectile energies over the laboratory angular range 0.2 degree endash 5 degree. When compared in the center-of-mass reference frame, these cross sections exhibit a high degree of similarity in both amplitude and angular dependence. The cross sections for N_2, CO, CO_2, and H_2O are inverted using a partial-wave analysis to yield empirical interaction potentials, which can then be used to extrapolate the measurements down to lower energies. Using these potentials, ...

338

Insight into Thyroid-Stimulating Autoantibody Interaction with the Thyrotropin Receptor N-Terminus Based on Mutagenesis and Re-Evaluation of Ambiguity in This Region of the Receptor Crystal Structure  

British Library Electronic Table of Contents (United Kingdom)

Background: Thyroid-stimulating autoantibodies (TSAb) bind to the thyrotropin receptor (TSHR) extracellular domain, or ectodomain (ECD), comprising a leucine-rich repeat domain (LRD) linked by a hinge region to the transmembrane domain (TMD). The LRD (residues 22???260; signal peptide 1???21) contains two disulfide-bonded loops at its N-terminus. In the crystal structure of the isolated LRD complexed with human TSAb monoclonal antibody (mAb) M22, N-terminal disulfide loop 1 (residues 22???30) could not be determined because of crystal disorder. Nevertheless, present crystal structure data are interpreted to exclude a role for the LRD N-terminal disulfide loops in the TSAb epitope(s), contradicting prior functional evidence of a role for these loops in TSAb function. Materials and Methods: ...

2011-01-01

339

Imaging of gastrinomas by nuclear medicine methods  

International Nuclear Information System (INIS)

Somatostatin receptor scintigraphy (SRS) is a valuable method for the detection of somatostatin receptor-positive lesions. Most gastrinomas (over-)express the somatostatin receptor subtype 2 which can be targeted by In-111 labeled Octreotide. Different studies show a high sensitivity of SRS for the localization and staging of gastrinomas. SRS seems to be superior to other non-invasive imaging modalities and has been proven to significantly contribute to patient management. However, the sensitivity depends on the size and exact localization of the tumors. Smaller lesions and lesions located in the duodenum show a significantly lower sensitivity. In any case, SRS belongs to the routine imaging procedure for gastrinomas for localization and staging and can also be used for evaluation of the tumor progression. (author)

340

Generation and Characterization of Monoclonal Antibodies to Human Keratinocyte Growth Factor Receptor  

British Library Electronic Table of Contents (United Kingdom)

Keratinocyte growth factor receptor (KGFR) and fibroblast growth factor receptor (FGFR) 2c share identical amino acid sequences, except for a 46-amino acid domain in the extracellular region. Monoclonal antibodies (MAbs) specific to KGFR have not been reported nor are commercially available. In this study, we generated murine MAbs specific to KGFR in non-obese diabetic (NOD) mice using a modified Repeated Immunizations at Multiple Sites (RIMMS) technology. Stable cell lines expressing the full-length human KGFR or FGFR2c were produced to facilitate the identification of KGFR-specific MAbs. Following the initial screening of hybridoma clones with a fluorescence-based, confocal cell detection method and ELISA, KGFR-specific MAbs were selected and confirmed by flow cytometry and Western blot ...

2006-01-01

341

The importance of an accurate target wave function in variational calculations for (e^{+}-H_{2}) scattering  

CERN Document Server

Using the complex Kohn method, we have calculated variational values of phase shifts and the annihilation parameter, Z_{eff}, for the elastic scattering of positrons by molecular hydrogen. Our results are sensitive to small changes in the accuracy of the wave function representing the target hydrogen molecule. We have developed a systematic approach to demonstrate that, at low positron energies, there are particular forms of the Kohn trial wave function for which the results of variational calculations are not reliable, even when the target wave function accounts for as much as 96.8% of the correlation energy of H_{2}. We find that reliable results can be recovered if our calculations are extended to admit more sophisticated target wave functions accounting for 99.7% of the correlation energy. Remaining discrepancies between theory and experiment are briefly discussed.

2008-01-01

342

Synthesis of monohydric alcohols from CO and H2 on Fe/Sibunit catalysts  

British Library Electronic Table of Contents (United Kingdom)

It was demonstrated that R 2?R 4 saturated monohydric alcohols can be synthesized from CO and H2 in the presence of Fe catalysts containing a carbon support of the Sibunit type with granule sizes of 3?5, 1?2, and 0.05?0.1 mm in a fixed-bed reactor at 3 MPa and 240?300?C. It was found that the activity of Fe/Sibunit catalysts and their selectivity for the formation of liquid synthetic products increased with the size of granules and the amount of iron. The catalysts make it possible to obtain fatty alcohols, in which the fraction of R 2?R 4 alcohols is as high as 75%, in yields to 56 g/m3.

2011-01-01

343

Synergistic effect of iodide ion and polyacrylic acid on corrosion inhibition of iron in H2SO4 investigated by electrochemical techniques  

British Library Electronic Table of Contents (United Kingdom)

Corrosion inhibition of iron in H2SO4 by polyacrylic acid (PAA) was investigated using electrochemical techniques at 30degreeC. Results obtained indicate that PAA inhibited the corrosion of iron in the acid medium. Inhibition efficiency increases with increase in PAA concentration and synergistically enhanced on addition of iodide ions. Potentiodynamic polarization results suggest that PAA functions as a modest cathodic inhibitor. The adsorption of PAA onto the iron surface followed Temkin adsorption isotherm. FTIR analysis revealed that the synergistic effect due to co-adsorption of iodide ions and PAA is co-operative in nature.

2010-01-01

344

Range-resolved gas concentration measurements using tunable semiconductor lasers  

British Library Electronic Table of Contents (United Kingdom)

A method for range-resolved gas sensing using path-integrated optical systems is presented. The method involves dividing an absorption path into several measurement segments and extracting the gas concentration in each segment from two path-integrated measurements. We implemented the method with tunable lasers (a 1389-nm VCSEL and a 10.9-?m pulsed quantum cascade laser) and a group of retro reflectors (RRs) distributed along absorption paths. Using a rotating mirror with the VCSEL configuration, we could scan a group of seven tape RRs spaced by 10?cm in ??9?ms to extract an H2O concentration profile. Reduced H2O concentrations were recorded in the segments purged with dry air. Hollow corner cube RRs were used in the quantum cascade laser configuration at distances up to 1.1?km from the las...

2008-01-01

345

RHEED, AES and XPS studies of the passive films formed on ion implanted stainless steel  

International Nuclear Information System (INIS)

P-implantation (10"1"7 ions cm"-"2, 40 KeV) into 304 stainless steel (ss) has been carried out, and an amorphous surface alloy was formed. Polarization studies in deaerated 1N H_2SO_4+ 2% NaCl showed that P-implantation improved both the general and localized corrosion resistance of 304 ss. A comparative study has been carried out between the implanted and unimplanted steel to determine what influence P-implantation has upon the properties of the passive film formed 1N H_2SO_4. The influence of Cl ions on pre-formed passive films was also studied. RHEED, XPS and AES were used to evaluate the nature of the passive films formed in these studies.

2005-05-26

346

Preparation of tetravalent praseodymium in potassium phosphotungstate aqueous solutions  

International Nuclear Information System (INIS)

The possibility has been studied of oxidizing Prsup((3)) to Prsup((4)) when Prsup((3)) is added to an aqueous weakly-acid solution containing K_1_0[P_2W_1_7O_6_1H_2O] x H_2O. A sharp change in the solution colouring has been observed as a result of Prsup((3)) oxidation to Prsup((4)). The absorption spectra of solution of Prsup((4)) have been recorded and the values of the molar extinction coefficients have been determined. On storage of the solution, Prsup((4))reduces to Prsup((3)) with a half-reduction period of 0.2-0.5 hour.

1977-01-01

347

Light emission from hydrogen-copper interaction at grazing incidence  

International Nuclear Information System (INIS)

The optical emission of excited H reflected from clean Cu(110) after impingement of H"+ and H_2"+ in the energy range of 250 eV to 20 keV per nucleon at 70"0 angle of incidence to the surface normal was measured. For incident 10 keV H_2"+, the highest excited hydrogen state detected was the n=10 level. The Hsub(#alpha#) yield was found to be fluence and energy dependent. This effect is attributed either to fast sputtered hydrogen, surface roughness or to an increase with hydrogen concentration in electron states of p-like symmetry near the Fermi level of copper. The Hsub(#alpha#) yield per reflected nucleon shows approximately an exponential dependence on both projectile energy per nucleon and scattered particle reciprocal velocity perpendicular to the surface. (orig.).

1983-07-01

348

Heteropolyanion-based ionic hybrid solid: A green bulk-type catalyst for hydroxylation of benzene with hydrogen peroxide  

British Library Electronic Table of Contents (United Kingdom)

A novel heteropolyanion-based ionic hybrid was prepared by combining the divalent ionic liquid (IL) cation of 1,1'-(butane-1,4-diyl)-bis(3-methylimidazolium) with the Keggin-structured V-containing heteropolyanion, and characterized by ^1H NMR, FT-IR, ESI-MS, XRD, SEM, TG, BET surface area, melting point, and elemental analysis. Its catalytic activity was evaluated in the hydroxylation of benzene with aqueous H2O2, including the testing of the influence of organic cations, catalytic reusability and optimization of reaction conditions. This hybrid is characterized to be semi-amorphous nanoparticles with a IL-like composition. The hybrid catalyst leads to the liquid-solid biphasic reaction system for hydroxylation of benzene with H2O2, presenting such advantages as high catalytic activity, c...

2011-01-01

349

Electron binding to isolated polar molecules and molecular dipole assemblies  

International Nuclear Information System (INIS)

In a sufficiently large cluster of several polar molecules, collective interactions lead to localization or 'solvation' of electrons. The existence of the solvated electron is known since 1863 in liquid ammonia and since 1962 for liquid water. In 1984, electron localization in clusters was experimentally demonstrated in (H_2O)_N_#>=#_1_1 and (NH_3)_N_#>=#_3_4 clusters. In cooperation with K. Bowen, we recently initiated a test of the theory of electron binding by a dipole and a new ground state dipole bound dimer anion, (H_2O..NH_3), was predicted and observed. We here describe results of a search for new dipole-bound and solvated electron systems. (author).

1994-03-20

350

Crystal structure of the human centromeric nucleosome containing CENP-A  

British Library Electronic Table of Contents (United Kingdom)

In eukaryotes, accurate chromosome segregation during mitosis and meiosis is coordinated by kinetochores, which are unique chromosomal sites for microtubule attachment. Centromeres specify the kinetochore formation sites on individual chromosomes, and are epigenetically marked by the assembly of nucleosomes containing the centromere-specific histone H3 variant, CENP-A. Although the underlying mechanism is unclear, centromere inheritance is probably dictated by the architecture of the centromeric nucleosome. Here we report the crystal structure of the human centromeric nucleosome containing CENP-A and its cognate ?-satellite DNA derivative (147 base pairs). In the human CENP-A nucleosome, the DNA is wrapped around the histone octamer, consisting of two each of histones H2A, H2B, H4 and CENP...

2011-01-01

351

Collisions between H"+ and H_2 at kilo-electron-volt energies: Absolute differential cross sections for small-angle direct, single-, and double-charge-transfer scattering  

International Nuclear Information System (INIS)

Measurements of absolute differential cross sections for H"+-H_2 direct, single-, and double-charge-transfer scattering at 0.5, 1.5, and 5.0 keV are reported at laboratory scattering angles less than 1 degree with an angular resolution of approximately 0.02 degree. The cross sections exhibit deep interference oscillations in single-charge-transfer scattering, but no such oscillations are present in direct and double-charge-transfer scattering. Theoretical cross sections derived using the diatoms-in-molecules method to describe the molecular states in a semiclassical molecular-orbital three-state close-coupling model within a semiclassical framework agree satisfactorily with the experimental results.

352

Characterization of the combustion of biomass producer gas in a constant volume combustion bomb  

British Library Electronic Table of Contents (United Kingdom)

In this article a methodology is presented for studying the influence of the biomass moisture content and the biomass/air ratio on the producer gas composition and on the chemiluminescent emissions during the combustion process. Firstly, a mathematical model based on the thermo-chemical processes inside the gasifier is used to predict the composition of the producer gas as a mixture of CO, CO2, H2, N2, CH4 and H2O gases. Secondly, the predicted composition is introduced into a constant volume combustion bomb (CVCB), which simulates the typical conditions inside the combustion chamber of an internal combustion engine, in order to characterize its combustion under gasoline-type conditions through the instantaneous pressure and the detection of the spontaneous luminous radiation (chemilumines...

2010-01-01

353

Biosorption of reactive dye by waste biomass of Nostoc linckia  

British Library Electronic Table of Contents (United Kingdom)

Potential of spent biomass of a cyanobacterium, Nostoc linckia HA 46, from a hydrogen bioreactor was studied for biosorption of a textile dye, reactive red 198. The waste biomass was immobilized in calcium alginate and used for biosorption of the dye from aqueous solution using response surface methodology (RSM). Kinetics of the dye in aqueous solution was studied in batch mode. Interactive effects of initial dye concentration (100-500mg/L), pH (2-6) and temperature (25-45^oC) on dye removal were examined using Box-Behnken design. Maximum adsorption capacity of the immobilized biomass was 93.5mg/g at pH 2.0, initial concentration of 100mg/L and 35^oC temperature, when 94% of the dye was removed. Fourier transform infrared (FT-IR) studies revealed that biosorption was mainly mediated by fun...

2011-01-01

354

Assembly of a water-insoluble strontium metal-organic framework with luminescent properties  

British Library Electronic Table of Contents (United Kingdom)

A new strontium metal-organic framework, [Sr2(BTEC)(H2O)4] 2H2O (1) (H4BTEC=benzene-1,2,4,5-tetracarboxylic acid), has been successfully synthesized by mixing the starting reagents. The single-crystal structure analysis showed that compound 1 displayed three-dimensional structures containing inorganic motifs with two-dimensional layers pillar-connected through organic linkers and forming water-coordinated neutral framework. Further studies revealed that compound 1 was insoluble in water and that it emitted strong luminescence at approximately 437nm after dehydration.

2011-01-01

355

Analysis of plasma treatment and vapor heat treatment for thin-film transistors by extracting trap densities at front and back interfaces  

International Nuclear Information System (INIS)

Hydrogen (H) plasma treatment, oxygen (O) plasma treatment and water (H_2O)-vapor heat treatment for polycrystalline-silicon (poly-Si) thin-film transistors (TFTs) have been analyzed by separately extracting trap density at a front silicon-oxide interface (D_F) and trap density at a back interface (D_B). It is found that the H plasma treatment is apt to generate D_F and D_B. The O plasma treatment reduces D_F, while the H_2O-vapor heat treatment reduces both D_F and D_B. Improvement of transistor characteristics of poly-Si TFTs depends on understanding these results.

2004-05-17

356

AFM Imaging of SWI/SNF action: mapping the nucleosome remodeling and sliding  

CERN Document Server

We propose a combined experimental (Atomic Force Microscopy) and theoretical study of the structural and dynamical properties of nucleosomes. In contrast to biochemical approaches, this method allows to determine simultaneously the DNA complexed length distribution and nucleosome position in various contexts. First, we show that differences in the nucleo-proteic structure observed between conventional H2A and H2A.Bbd variant nucleosomes induce quantitative changes in the in the length distribution of DNA complexed with histones. Then, the sliding action of remodeling complex SWI/SNF is characterized through the evolution of the nucleosome position and wrapped DNA length mapping. Using a linear energetic model for the distribution of DNA complexed length, we extract the net wrapping energy of DNA onto the histone octamer, and compare it to previous studies.

2007-01-01

357

A study on rf plasma nitriding at a constant power in different H_2-N_2 mixtures at different temperatures  

International Nuclear Information System (INIS)

Austenitic stainless steel AISI 304 has been nitrided by radio frequency (rf) plasma containing various nitrogen-hydrogen gas mixtures, in order to study the effect of hydrogen on structure and magnetic properties of the formed compound layer. The thermal temperature has been measured at the vicinity of the samples. The compound layer thus produced has been characterized using, X-ray diffractometer and vibration sample magnetometer. Providing the total pressure of nitrogen and hydrogen is held constant, the addition of hydrogen up to 50% gives new structural phases. The magnetization values of the plasma treated samples are strongly dependent on the percentage of H_2 in the gas phase. An excessive amount of hydrogen (#approx#75%) on the other hand, retards the nitriding process. The surface temperature of the sample and plasma condition is crucial factors for nitriding process.

2006-04-15

358

A Combinatorial Library of Micro-Topographies and Chemical Compositions for Tailored Surface Wettability  

British Library Electronic Table of Contents (United Kingdom)

Abstract Surface modification of topography and chemistry in order to achieve a specific water contact angle (CA) has been explored by using a novel combinatorial screening platform. The screening arrays consisted of 507 distinct combinations of micro-topographies and chemical compositions. By performing chemical modifications with 1H, 1H, 2H, 2H perfluoroethyltriethoxy-silane (PFS) and n-octadecyltriethoxysilane (ODS) on standard silicon wafers it was possible to include both superhydrophobic and very hydrophilic pad arrays in the same screening platform. Surfaces modified with PFS were more hydrophobic than surfaces modified with ODS, while the unmodified silicon surfaces were hydrophilic. For the PFS modified surfaces the largest CAs were achieved with a small pillar size of X-=-1-m and...

2011-01-01

359

metabotropic glutamate receptor 5 (mGluR5) has a critical role in inhibitory learning  

UK PubMed Central (United Kingdom)

The mechanisms that contribute to the extinction of previously acquired memories are not well understood. These processes, often referred to as inhibitory learning, are thought to be parallel...Full Text Available

2009-03-25

360

Zebrafish TRPA1 Channels are Required for Chemosensation but not for Thermosensation or Mechanosensory Hair Cell Function  

UK PubMed Central (United Kingdom)

Transient receptor potential (TRP) ion channels have been implicated in detecting chemical, thermal and mechanical stimuli in organisms ranging from mammals to Caenorhabditis elegans....Full Text Available

2008-10-01

361

Vitamin A Enhances Antitumor Effect of a Green Tea Polyphenol on Melanoma by Upregulating the Polyphenol Sensing Molecule 67-kDa Laminin Receptor  

UK PubMed Central (United Kingdom)

BackgroundGreen tea consumption has been shown to have cancer preventive qualities. Among the constituents of green tea, (-)-Epigallocatechin-3-O-gallate (EGCG)...Full Text Available

362

Tumor-derived extracellular mutations of PTPRT/PTP? are deficient in cell adhesion  

UK PubMed Central (United Kingdom)

Receptor protein tyrosine phosphatase T (PTPRT/PTPρ) is frequently mutated in human cancers including colon, lung, gastric and skin cancers. More than half of the identified tumor-derived...Full Text Available

2008-07-01

363

Trigeminal injury causes kappa opioid-dependent allodynic, glial and immune cell responses in mice  

UK PubMed Central (United Kingdom)

BackgroundThe dynorphin-kappa opioid receptor (KOR) system regulates glial proliferation after sciatic nerve injury. Here, we investigated its role in cell proliferation following...Full Text Available

364

Tone-Specific and Nonspecific Plasticity of the Auditory Cortex Elicited by Pseudoconditioning: Role of Acetylcholine Receptors and the Somatosensory Cortex  

UK PubMed Central (United Kingdom)

Experience-dependent plastic changes in the central sensory systems are due to activation of both the sensory and neuromodulatory systems. Nonspecific changes of cortical auditory neurons elicited by...Full Text Available

2008-09-01

365

Time-limited modulation of appetitive Pavlovian memory by D1 and NMDA receptors in the nucleus accumbens  

UK PubMed Central (United Kingdom)

Recent research has implicated the nucleus accumbens (NAc) in consolidating recently acquired goal-directed appetitive memories, including spatial learning and other instrumental processes. However,...Full Text Available

2005-04-26

366

The potential role of phrenic nucleus glutamate receptor subunits in mediating spontaneous crossed phrenic activity in neonatal rat  

UK PubMed Central (United Kingdom)

Cervical spinal cord hemisection rostral to the phrenic nucleus leads to paralysis of the ipsilateral hemidiaphragm in adult rats. Respiratory function can be restored to the paralyzed hemidiaphragm...Full Text Available

2009-08-01

367

The photoaffinity ligand [3,5-"3H] 4-azidoclonidine. Synthesis and characterization details  

International Nuclear Information System (INIS)

[3,5-"3H] 4-Azidoclonidine 6 was prepared from [3,5-"3H] 4-aminoclonidine 4 and has emerged as a valuable tool to study the alpha-2-adrenergic receptor. (author)

2004-07-01

368

The orphan nuclear receptor small heterodimer partner mediates male infertility induced by diethylstilbestrol in mice  

UK PubMed Central (United Kingdom)

Studies in rodents have shown that male sexual function can be disrupted by fetal or neonatal administration of compounds that alter endocrine homeostasis, such as the synthetic nonsteroidal estrogen...Full Text Available

2009-12-01

370

The effects of histamine and leukotriene receptor antagonism on nasal mannitol challenge in allergic rhinitis  

UK PubMed Central (United Kingdom)

AimsIt is unclear as to which mediators are involved in mediating the response to nasal mannitol challenge, a novel osmotic stimulus.MethodsA...Full Text Available

2003-06-01

371

The Receptor Tyrosine Kinase FGFR4 Negatively Regulates NF-kappaB Signaling  

UK PubMed Central (United Kingdom)

BackgroundNFκB signaling is of paramount importance in the regulation of apoptosis, proliferation, and inflammatory responses during human development and homeostasis, as...Full Text Available

372

The Case for Selection at CCR5-?32  

UK PubMed Central (United Kingdom)

The C-C chemokine receptor 5, 32 base-pair deletion (CCR5-Δ32) allele confers strong resistance to infection by the AIDS virus HIV. Previous studies have suggested...Full Text Available

2005-11-01

373

Temperature-induced opening of TRPV1 ion channel is stabilized by the pore domain  

UK PubMed Central (United Kingdom)

SummaryTRPV1 is the founding and best-studied member of the family of temperature-activated transient receptor potential ion channels (thermoTRPs). Voltage, chemicals, and heat...Full Text Available

2010-06-01

374

Tarantula Huwentoxin-IV Inhibits Neuronal Sodium Channels by Binding to Receptor Site 4 and Trapping the Domain II Voltage Sensor in the Closed Configuration*S?  

UK PubMed Central (United Kingdom)

Peptide toxins with high affinity, divergent pharmacological functions, and isoform-specific selectivity are powerful tools for investigating the structure-function relationships of voltage-gated...Full Text Available

2008-10-03

375

Synapse-Associated Protein 102/dlgh3 Couples the NMDA Receptor to Specific Plasticity Pathways and Learning Strategies  

UK PubMed Central (United Kingdom)

Understanding the mechanisms whereby information encoded within patterns of action potentials is deciphered by neurons is central to cognitive psychology. The multiprotein complexes formed by...Full Text Available

2007-03-07

376

Steroid hormones and brain development: some guidelines for understanding actions of pseudohormones and other toxic agents.  

UK PubMed Central (United Kingdom)

Gonadal, adrenal, and thyroid hormones affect the brain directly, and the sensitivity to hormones begins in embryonic life with the appearance of hormone receptor sites in discrete populations of neurons....Full Text Available

1987-10-01

377

Somatostatin receptor scintigraphy might be useful for detecting skeleton abnormalities in patients with multiple myeloma and plasmacytoma  

International Nuclear Information System (INIS)

Somatostatin receptor expression has been demonstrated on a number of plasma cell lines. Therefore, we questioned whether somatostatin receptor scintigraphy (SRS) can be used to demonstrate in vivo multiple myeloma (MM) activity. SRS was performed in newly diagnosed (n = 9) or relapsing (n = 18) MM patients or in patients with localized plasmacytoma (n = 2). The results were compared with radiographic findings. A positive SRS was demonstrated in 44% of the newly diagnosed patients, in 83% of the relapsed patients and in both patients with plasmacytoma. The SRS findings corresponded with radiographic abnormalities in 40% of the patients. However, in relapsed patients 60% demonstrated increased SRS uptake in areas without new radiographic abnormalities. The positive SRS corresponded with histologically proven disease activity and responded upon treatment. Moreover, immunohistochemical staining of MM material demonstrated concordant somatostatin ...

2010-01-01

378

Sigma-1 receptor agonist fluvoxamine for postoperative delirium in older adults: report of three cases  

UK PubMed Central (United Kingdom)

BackgroundPostoperative delirium is a topic of great importance in the geriatric surgical specialty. Although antipsychotic drugs are the medications most frequently used to treat...Full Text Available

379

Serum RANKL, osteoprotegerin (OPG), and RANKL/OPG ratio in nephrotic children  

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

2010-10-01

380

Serum HER2 Level Measured by Dot Blot: A Valid and Inexpensive Assay for Monitoring Breast Cancer Progression  

UK PubMed Central (United Kingdom)

Human epidermal growth factor receptor 2 (HER2) is one of the most important prognostic and predictive factors for breast cancer patients. Recently, serum HER2...Full Text Available

381

Selective imaging of adherent targeted ultrasound contrast agents  

UK PubMed Central (United Kingdom)

The goal of ultrasonic molecular imaging is the detection of targeted contrast agents bound to receptors on endothelial cells. We propose imaging methods that can distinguish adherent microbubbles...Full Text Available

2007-04-21

382

Selective endothelin A-receptor blockade attenuates coronary microvascular dysfunction after coronary stenting in patients with type 2 diabetes  

UK PubMed Central (United Kingdom)

Background:Endothelin-1 may be involved in the development of diabetic microangiopathy. We studied the effect of endothelin-1 blockade on myocardial microcirculation during coronary...Full Text Available

2009-01-01

383

STIMULATION OF TARSAL RECEPTORS OF THE BLOWFLY BY ALIPHATIC ALDEHYDES AND KETONES  

UK PubMed Central (United Kingdom)

Rejection of eight aldehydes, eight ketones, five secondary alcohols, and 3-pentanol has been studied in the blowfly Phormia regina Meigen. The data agree with results previously reported...Full Text Available

1949-03-20

384

Role of adenosine in regulating glucose uptake during contractions and hypoxia in rat skeletal muscle  

UK PubMed Central (United Kingdom)

The effect of A1-adenosine receptor antagonism via 8-cyclopentyl-1,3-dipropyl-xanthine (CPDPX) on the stimulation of skeletal muscle glucose uptake by...Full Text Available

1999-02-15

385

Role of Estrogen Receptor-? in the Regulation of Claudin-6 Expression in Breast Cancer Cells  

UK PubMed Central (United Kingdom)

PurposeIn our previous studies we showed that upregulating claudin-6 (CLDN6) expression may contribute to preventing breast cancer, and that 17β-estradiol induces a concentration-...Full Text Available

2011-03-01

386

Residence time probability analysis of sulfur concentrations at Grand Canyon National Park  

Energy Technology Data Exchange (ETDEWEB)

A statistical method is developed to determine the locations of major pollutant sources affecting a distant downwind receptor, provided that air trajectories can be estimated. Probability density functions are estimated which indicate the overall residence time of air parcels over a given geographic region as they travel toward a receptor and residence time for the case of high pollutant concentrations at the receptor. These functions are used to estimate a conditional probability function which indicates the potential for a source region to contribute to high air pollution concentrations. Finally, a source contribution function is formulated to indicate the relative contribution of different source regions to high concentrations at the receptor. The method is tested using data collected at Grand Canyon National Park in 1980. The dominant pathway for air masses arriving at Grand Canyon during this ...

1985-01-01

387

Radiolabelled D_2 agonists as prolactinoma imaging agents: Progress report for period February 1, 1988--January 31, 1989  

International Nuclear Information System (INIS)

Targeted studies completed include the evaluation of tritiated N-0437, evaluation of "3"5S-cysteamine, evaluation of "1"8F-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 ...

388

Radiolabelled D/sub 2/ agonists as prolactinoma imaging agents: Progress report for period February 1, 1988--January 31, 1989  

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 ...

1988-10-15

389

RXR activators molecular signalling: involvement of a PPAR?-dependent pathway in the liver and kidney, evidence for an alternative pathway in the heart  

UK PubMed Central (United Kingdom)

In this study we compared the molecular signalling elicited by rexinoids, selective retinoid X receptor (RXR)-activators, in several organs (i.e. liver, kidney,...Full Text Available

2003-03-01

390

Putative Biomarkers and Targets of Estrogen Receptor Negative Human Breast Cancer  

UK PubMed Central (United Kingdom)

Breast cancer is a progressive and potentially fatal disease that affects women of all ages. Like all progressive diseases, early and reliable diagnosis is the key for successful treatment and annihilation....Full Text Available

391

Prolactin Receptor Signaling Is Essential for Perinatal Brown Adipocyte Function: A Role for Insulin-like Growth Factor-2  

UK PubMed Central (United Kingdom)

BackgroundThe lactogenic hormones prolactin (PRL) and placental lactogens (PL) play central roles in reproduction and mammary development. Their actions are mediated via binding...Full Text Available

392

Prognostic Significance of Peritumoral Lymphatic Vessel Density and Vascular Endothelial Growth Factor Receptor 3 in Invasive Squamous Cell Cervical Cancer  

UK PubMed Central (United Kingdom)

Cervical cancer is known to metastasize primarily by the lymphatic system. Dissemination through lymphatic vessels represents an early step in regional tumor progression, and the presence of lymphatic...Full Text Available

393

Pretreatment with a soluble activin type IIB receptor/Fc fusion protein improves hypoxia-induced muscle dysfunction  

UK PubMed Central (United Kingdom)

Hypoxia, or reduced oxygen, occurs in a variety of clinical and environmental situations. Hypoxic exposure is associated with decreased muscle mass and a concomitant reduction in exercise capacity,...Full Text Available

2010-01-01

394

Prenatal cocaine reduces AMPA receptor synaptic expression through hyperphosphorylation of the synaptic anchoring protein GRIP  

UK PubMed Central (United Kingdom)

Prenatal cocaine exposure produces sustained neurobehavioral and brain synaptic changes closely resembling those of animals with defective alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic...Full Text Available

2009-05-13

395

Pore-forming toxins trigger shedding of receptors for interleukin 6 and lipopolysaccharide.  

UK PubMed Central (United Kingdom)

Cleavage of membrane-associated proteins with the release of biologically active macromolecules is an emerging theme in biology. However, little is known about the nature and regulation of the involved...Full Text Available

1996-07-23

396

Plasma membrane as the target site of cholic acid analogs.  

Science.gov (United States)

Although the mechanism is unknown, Calculus Bovis and its active components, cholic acid analogs (CAAs), have been used in China to treat a wide range of diseases. Based on the previous finding that the potency of CAA is strongly dependent on the intrinsic surface activity, this paper aimed to investigate the role of the plasma membrane in the pharmacological activity of CAAs. First, CAAs (0.1 mM) caused a surface activity-dependent depression on ATPase activity in the cell membrane extract, but it had no effects on other cellular extracts, suggesting an indispensable role of the membrane environment for pharmacological activity. Second, CAAs lowered the membrane fluidity of cultured Caco-2 cells with the same rank-order of potency sequence. Third, the hypothesis that any functional protein located on the membrane is influenced by changes in cellular membrane fluidity was supported by: ileal contraction that was induced by acetylcholine and mediated by the muscarinic ...

2011-08-03

397

Parallel helix bundles and ion channels: molecular modeling via simulated annealing and restrained molecular dynamics.  

UK PubMed Central (United Kingdom)

A parallel bundle of transmembrane (TM) alpha-helices surrounding a central pore is present in several classes of ion channel, including the nicotinic acetylcholine receptor (nAChR). We have modeled...Full Text Available

1994-10-01

398

Paradoxical function for the receptor for advanced glycation end products in mouse models of pulmonary fibrosis  

UK PubMed Central (United Kingdom)

Idiopathic pulmonary fibrosis (IPF) is a progressive disease with poor survival. The identification of therapeutic targets is essential to improving outcomes. Previous studies found that expression...Full Text Available

2011-03-31

399

P2Y2 Nucleotide Receptor-Mediated Responses in Brain Cells  

UK PubMed Central (United Kingdom)

Acute inflammation is important for tissue repair; however, chronic inflammation contributes to neurodegeneration in Alzheimer’s disease (AD) and occurs when glial cells undergo prolonged...Full Text Available

2010-06-01

400

Ontogenetic Profile of the Expression of Thyroid Hormone Receptors in Rat and Human Corpora Cavernosa of the Penis  

UK PubMed Central (United Kingdom)

IntroductionIn the last few years, various studies have underlined a correlation between thyroid function and male sexual function, hypothesizing a direct action of thyroid hormones...Full Text Available

2010-04-01

401

Nuclear receptor ERR? and coactivator PGC-1? are effectors of IFN-?-induced host defense  

UK PubMed Central (United Kingdom)

Macrophage activation by the proinflammatory cytokine interferon-γ (IFN-γ) is a critical component of the host innate response to bacterial pathogenesis. However, the precise nature...Full Text Available

2007-08-01

402

Nuclear Receptor Rev-erb Alpha (Nr1d1) Functions in Concert with Nr2e3 to Regulate Transcriptional Networks in the Retina  

UK PubMed Central (United Kingdom)

The majority of diseases in the retina are caused by genetic mutations affecting the development and function of photoreceptor cells. The transcriptional networks directing these processes are regulated...Full Text Available

403

Noradrenergic ?1 Receptors as a Novel Target for the Treatment of Nicotine Addiction  

UK PubMed Central (United Kingdom)

Nicotine is the main psychoactive ingredient in tobacco and its rewarding effects are considered primarily responsible for persistent tobacco smoking and relapse. Although dopamine has been extensively...Full Text Available

2010-07-01

404

Nonsteroidal Selective Androgen Receptor Modulators Enhance Female Sexual Motivation  

UK PubMed Central (United Kingdom)

Women experience a decline in estrogen and androgen levels after natural or surgically induced menopause, effects that are associated with a loss of sexual desire and bone mineral density. Studies in...Full Text Available

2010-08-01

405

Neuroprotective effect of paeoniflorin on cerebral ischemic rat by activating adenosine A1 receptor in a manner different from its classical agonists  

UK PubMed Central (United Kingdom)

The effects of paeoniflorin (PF), a compound isolated from Paeony radix, on neurological impairment and histologically measured infarction volume...Full Text Available

2005-10-01

406

Neural injury following stroke: are Toll-like receptors the link between the immune system and the CNS?  

UK PubMed Central (United Kingdom)

The CNS can exhibit features of inflammation in response to injury, infection or disease, whereby resident cells generate inflammatory mediators, including cytokines, prostaglandins, free radicals and...Full Text Available

2010-08-01

407

NMDA Receptor Blockade with Memantine Attenuates White Matter Injury in a Rat Model of Periventricular Leukomalacia  

UK PubMed Central (United Kingdom)

Hypoxia–ischemia (H/I) in the premature infant leads to white matter injury termed periventricular leukomalacia (PVL), the leading cause of subsequent neurological deficits. Glutamatergic...Full Text Available

2008-06-25

408

Myelin associated glycoprotein cross-linking triggers its partitioning into lipid rafts, specific signaling events and cytoskeletal rearrangements in oligodendrocytes  

UK PubMed Central (United Kingdom)

Myelin-associated glycoprotein (MAG) has been implicated in inhibition of nerve regeneration in the CNS. This results from interactions between MAG and the Nogo receptor and gangliosides on...Full Text Available

2004-02-01

409

Molecular conformation, receptor binding, and hormone action of natural and synthetic estrogens and antiestrogens.  

UK PubMed Central (United Kingdom)

The X-ray crystallographic structural determinations of synthetic estrogens and antiestrogens provide reliable information on the global minimum energy conformation of these molecules or a local minimum...Full Text Available

1985-09-01

410

Molecular Mechanistic Insights into the Endothelial Receptor Mediated Cytoadherence of Plasmodium falciparum-Infected Erythrocytes  

UK PubMed Central (United Kingdom)

Cytoadherence or sequestration is essential for the pathogenesis of the most virulent human malaria species, Plasmodium falciparum (P. falciparum). Similar to leukocyte-endothelium...Full Text Available

411

Modulation of the human hair follicle pigmentary unit by corticotropin-releasing hormone and urocortin peptides  

UK PubMed Central (United Kingdom)

Human skin is a local source of corticotropin-releasing hormone (CRH) and expresses CRH and CRH receptors (CRH-R) at mRNA and protein levels. Epidermal melanocytes respond to CRH by induction...Full Text Available

2006-05-01

412

Microglial Fc Receptors Mediate Physiological Changes Resulting From Antibody Cross-Linking of Myelin Oligodendrocyte Glycoprotein  

UK PubMed Central (United Kingdom)

Antibodies to myelin oligodendrocyte glycoprotein (MOG) have been implicated in Multiple Sclerosis demyelination through activation of complement and/or macrophage-effector processes. We presented...Full Text Available

2008-05-30

413

MFR, a Putative Receptor Mediating the Fusion of Macrophages  

UK PubMed Central (United Kingdom)

We had previously identified a macrophage surface protein whose expression is highly induced, transient, and specific, as it is restricted to actively fusing macrophages in vitro and in vivo. This protein...Full Text Available

1998-11-01

414

Long-Lasting Adaptations of the NR2B-containing NMDA Receptors in the Dorsomedial Striatum Play a Crucial Role in Alcohol Consumption and Relapse  

UK PubMed Central (United Kingdom)

A growing number of studies suggest that the development of compulsive drug seeking and taking depends on dorsostriatal mechanisms. We previously observed that ex vivo acute...Full Text Available

2010-07-28

415

Lnk controls mouse hematopoietic stem cell self-renewal and quiescence through direct interactions with JAK2  

UK PubMed Central (United Kingdom)

In addition to its role in megakaryocyte production, signaling initiated by thrombopoietin (TPO) activation of its receptor, myeloproliferative leukemia virus protooncogene (c-Mpl, or Mpl), controls...Full Text Available

2008-08-01

416

Listeria monocytogenes Infection Induces Prosurvival Metabolic Signaling in Macrophages?  

UK PubMed Central (United Kingdom)

Host cells use metabolic signaling through the LXRα nuclear receptor to defend against Listeria monocytogenes infection. 25-Hydroxycholesterol is a natural ligand of LXRs that...Full Text Available

2011-04-01

417

Lack of Association Between Prokineticin 2 Gene and Japanese Methamphetamine Dependence  

UK PubMed Central (United Kingdom)

Disruption of circadian rhythms may be involved in the pathophysiology of psychiatric disorders, including drug addiction. Recently, we detected the significant association between prokineticin 2 receptor...Full Text Available

2011-03-01

418

JAK/STAT Pathways in Cytokine Signaling and Myeloproliferative Disorders  

UK PubMed Central (United Kingdom)

Hematopoiesis is the cumulative result of intricately regulated signaling pathways that are mediated by cytokines and their receptors. Studies conducted over the past 10 to 15 years have revealed that...Full Text Available

2010-10-01

419

Interaction of Platelet Membrane Receptors with von Willebrand Factor, Ristocetin, and the Fc Region of Immunoglobulin G  

UK PubMed Central (United Kingdom)

The agglutination of human platelets by ristocetin and von Willebrand factor was inhibited by aggregated immunoglobulin (Ig)G and by Fc fragments of IgG, but not by Fab, F(ab′)2 or...Full Text Available

1978-11-01

420

Interaction between Bluetongue virus outer capsid protein VP2 and vimentin is necessary for virus egress  

UK PubMed Central (United Kingdom)

BackgroundThe VP2 outer capsid protein Bluetongue Virus (BTV) is responsible for receptor binding, haemagglutination and eliciting host-specific immunity. However, the assembly of...Full Text Available

421

Insulin receptor signaling in the development of neuronal structure and function  

UK PubMed Central (United Kingdom)

Sensory experience plays a crucial role in regulating neuronal shape and in developing synaptic contacts during brain formation. These features are required for a neuron to receive, integrate, and transmit...Full Text Available

422

Inactivating cholecystokinin-2 receptor inhibits progastrin-dependent colonic crypt fission, proliferation, and colorectal cancer in mice  

UK PubMed Central (United Kingdom)

Hyperproliferation of the colonic epithelium, leading to expansion of colonic crypt progenitors, is a recognized risk factor for colorectal cancer. Overexpression of progastrin, a nonamidated and incompletely...Full Text Available

2009-09-01

423

Immunolocalization of endothelin-B receptor in mouse intestinal tract.  

Science.gov (United States)

The endothelin-B (ETB) receptor is a G-protein-coupled receptor that binds endothelin ligands and is essential for the development of epidermal melanocytes and enteric neurons. Recent reports indicate that ETB is localized to nuclei in cardiac ventricular myocytes, although it has been thought that ETB is localized mainly on the plasma membrane. It remains unknown, however, whether this unique distribution of ETB occurs in other tissues. To elucidate the subcellular distribution of ETB in the intestine, we performed immunofluorescence of ETB in mouse intestine using a specific antibody. ETB-like immunoreactivity was detected in both the mucosal and muscle layers. In the mucosal layer, villous epithelial cells, stromal cells of the lamina propria, and cryptic cells were immunostained. Subcellularly, ETB is localized mainly to the nuclei of villous epithelial cells. In the muscle layer, immunoreactivity of ETB was localized to the myenteric ...

2004-11-01

424

Identification of circulating neuropilin-1 and dose-dependent elevation following anti-neuropilin-1 antibody administration  

UK PubMed Central (United Kingdom)

Neuropilin-1 (NRP1) acts as a co-receptor for class 3 semaphorins and vascular endothelial growth factor and is an attractive angiogenesis target for cancer therapy. In addition to the transmembrane...Full Text Available

2009-07-01

425

Identification and characterization of Aedes aegypti aminopeptidase N as a putative receptor of Bacillus thuringiensis Cry11A toxin  

UK PubMed Central (United Kingdom)

Bacillus thuringiensis subsp. israelensis, which is used worldwide to control Aedes aegypti larvae, produces Cry11Aa and other toxins during...Full Text Available

2009-10-01

426

Histamine Regulation in Glucose and Lipid Metabolism via Histamine Receptors  

UK PubMed Central (United Kingdom)

Histamine has been proposed to be an important regulator of energy intake and expenditure. The aim of this study was to evaluate histamine regulation of glucose and lipid metabolism and development...Full Text Available

2010-08-01

427

Glutamatergic regulation of ghrelin-induced activation of the mesolimbic dopamine system  

UK PubMed Central (United Kingdom)

Recently, we demonstrated that the central ghrelin signalling system, involving the ghrelin receptor (GHS-R1A), is important for alcohol reinforcement. Ghrelin targets a key mesolimbic circuit involved...Full Text Available

2011-01-01

428

Glutamate Receptor-Mediated Restoration of Experience-Dependent Place Field Expansion Plasticity in Aged Rats  

UK PubMed Central (United Kingdom)

Place fields of hippocampal pyramidal cells expand asymmetrically when adult rats repeatedly follow the same route. This behaviorally-induced expression of neuronal plasticity utilizes an NMDAR-dependent,...Full Text Available

2008-06-01

429

Genetic Elucidation of Human Hyperosmia to Isovaleric Acid  

UK PubMed Central (United Kingdom)

The genetic basis of odorant-specific variations in human olfactory thresholds, and in particular of enhanced odorant sensitivity (hyperosmia), remains largely unknown. Olfactory receptor (OR) segregating...Full Text Available

2007-11-01

430

Gene-silencing reveals the functional significance of pheromone biosynthesis activating neuropeptide receptor (PBAN-R) in a male moth  

UK PubMed Central (United Kingdom)

The role of pheromone biosynthesis activating neuropeptide (PBAN) in the regulation of pheromone biosynthesis of several female moth species is well elucidated, but its role in the males has been a...Full Text Available

2010-09-28

431

Gadolinium-containing phosphatidylserine liposomes for molecular imaging of atherosclerosis  

UK PubMed Central (United Kingdom)

Exteriorized phosphatidylserine (PS) residues in apoptotic cells trigger rapid phagocytosis by macrophage scavenger receptor pathways. Mimicking apoptosis with liposomes containing PS may represent...Full Text Available

2009-11-01

432

Fungal recognition is mediated by the association of dectin-1 and galectin-3 in macrophages  

UK PubMed Central (United Kingdom)

Dectin-1, the major β-glucan receptor in leukocytes, triggers an effective immune response upon fungal recognition. Here we use sortase-mediated transpeptidation, a technique that allows placement...Full Text Available

2011-08-23

433

Functional significance of UDP-glucuronosyltransferase (UGT) variants in the metabolism of active tamoxifen metabolites  

UK PubMed Central (United Kingdom)

Tamoxifen (TAM) is a selective estrogen receptor modulator widely used in the prevention and treatment of breast cancer. A major mode of metabolism of the major active metabolites of TAM, 4-OH-TAM...Full Text Available

2009-03-01

434

FGF18 is required for normal cell proliferation and differentiation during osteogenesis and chondrogenesis  

UK PubMed Central (United Kingdom)

Fibroblast growth factor (FGF) signaling is involved in skeletal development of the vertebrate. Gain-of-function mutations of FGF receptors (FGFR) cause craniosynostosis, premature fusion of the skull,...Full Text Available

2002-04-01

435

Expression of leukotriene receptors in the rat dorsal root ganglion and the effects on pain behaviors  

UK PubMed Central (United Kingdom)

BackgroundLeukotrienes (LTs) belong to the large family of lipid mediators implicated in various inflammatory conditions such as asthma and rheumatoid arthritis. Four distinct types...Full Text Available

436

EphB Receptors Couple Dendritic Filopodia Motility to Synapse Formation  

UK PubMed Central (United Kingdom)

SUMMARYMotile dendritic filopodial processes are thought to be precursors of spine synapses, but how motility relates to cell-surface cues required for axon-dendrite recognition...Full Text Available

2008-07-10

437

Eosinophils Utilize Multiple Chemokine Receptors for Chemotaxis to the Parasitic Nematode Strongyloides stercoralis  

UK PubMed Central (United Kingdom)

Protective innate immunity to the nematode Strongyloides stercoralis requires eosinophils in the parasite killing process. Experiments were performed to determine if an extract of S....Full Text Available

2009-10-01

438

Effects of Long-Term Pioglitazone Treatment on Peripheral and Central Markers of Aging  

UK PubMed Central (United Kingdom)

BackgroundThiazolidinediones (TZDs) activate peroxisome proliferator-activated receptor gamma (PPARγ) and are used clinically to help restore peripheral insulin sensitivity...Full Text Available

439

Effective In Vitro Clearance of Porphyromonas gingivalis by Fc? Receptor I (CD89) on Gingival Crevicular Neutrophils  

UK PubMed Central (United Kingdom)

Porphyromonas gingivalis has been implicated as a causative pathogen in periodontitis. Immunotherapeutic approaches have recently been suggested to aid in the clearance of P....Full Text Available

2001-05-01

440

Effect of differentiation on specific receptor sites and endocytosis of transferrin in a cell (HT-29) derived from human colic adenocarcinoma  

International Nuclear Information System (INIS)

The specific receptor sites and the endocytosis of transferrin (Tf) are evidenced in a cell line (HT-29) derived from a human colic adenocarcinoma by means of "1"2"5I radiolabeled Tf. The receptor density is studied in undifferentiated (UD) or differentiated (D) cells with respective doubling times of about 24 hours and 46 hours. The number of binding sites for Tf is 162,000 (K_d = 7.8 nmol/l in ND cells and 68,000 (K_d = 7.40 nmol/l) in D cells. The distribution between the Tf bound to the cell surface and the internalized Tf is investigated by elimination of Tf bound to the surface by an acid wash method. The intracellular cycle of Tf seems to be characterized by a slower kinetics in UD cells. The high density of Tf receptor sites in HT-29 UD cells should allow the detection or the treatment of highly evolutive colic adenocarcinoma by means of Tf.

441

Effect of Peroxisome Proliferator-Activated Receptor Gamma Agonist (Pioglitazone) and Methotrexate on Disease Activity in Rheumatoid Arthritis (Experimental and Clinical Study)  

UK PubMed Central (United Kingdom)

Objective:To investigate the combined effect of both pioglitazone and methotrexate on disease activity of rheumatoid arthritis in a biphasic study; experimental and clinical.Methods:Experimentally:...Full Text Available

442

Editing Antigen Presentation: Antigen Transfer between Human B Lymphocytes and Macrophages Mediated by Class A Scavenger Receptors1  

UK PubMed Central (United Kingdom)

B lymphocytes can function independently as efficient APCs. However, our previous studies demonstrate that both dendritic cells and macrophages are necessary to propagate immune responses initiated...Full Text Available

2008-09-15

443

EGFR Signaling Through an Akt-SREBP-1-Dependent, Rapamycin-Resistant Pathway Sensitizes Glioblastomas to Anti-Lipogenic Therapy  

UK PubMed Central (United Kingdom)

Glioblastoma, the most common malignant brain tumor, is among the most lethal and difficult cancers to treat. Although epidermal growth factor receptor (EGFR) mutations are frequent in glioblastoma,...Full Text Available

444

Dynamin-dependent NMDAR endocytosis during LTD and its dependence on synaptic state  

UK PubMed Central (United Kingdom)

BackgroundThe N-methyl-D-aspartate (NMDA)-type glutamate receptor expressed at excitatory glutamatergic synapses is required for learning and memory and is critical for normal brain...Full Text Available

445

Differential recognition of viral RNA by RIG-I  

UK PubMed Central (United Kingdom)

Retinoic acid inducible gene I (RIG-I) is a pattern recognition receptor (PRR) responsible for detection of nucleic acids from pathogens in the cytoplasm of infected cells and induction of type I interferon...Full Text Available

2011-03-01

446

DIFFERENTIAL EXPRESSION OF HPA AXIS HOMOLOG IN THE SKIN  

UK PubMed Central (United Kingdom)

SummaryHuman skin expresses elements of the hypothalamo-pituitary-adrenal (HPA) axis including pro-opiomelanocortin (POMC), corticotropin releasing hormone (CRH), the CRH receptor-1...Full Text Available

2007-02-01

447

Cytokinin-Dependent Photorespiration and the Protection of Photosynthesis during Water Deficit1[W][OA  

UK PubMed Central (United Kingdom)

We investigated the effects of PSARK∷IPT (for Senescence-Associated Receptor Kinase∷Isopentenyltransferase) expression and cytokinin production...Full Text Available

2009-07-01

448

Cyclophilin B Interacts with Sodium-Potassium ATPase and Is Required for Pump Activity in Proximal Tubule Cells of the Kidney  

UK PubMed Central (United Kingdom)

Cyclophilins (Cyps), the intracellular receptors for Cyclosporine A (CsA), are responsible for peptidyl-prolyl cis-trans isomerisation and for chaperoning several membrane proteins. Those functions...Full Text Available

449

Coevolution of activating and inhibitory receptors within mammalian carcinoembryonic antigen families  

UK PubMed Central (United Kingdom)

BackgroundMost rapidly evolving gene families are involved in immune responses and reproduction, two biological functions which have been assigned to the carcinoembryonic antigen...Full Text Available

450

Co-localization of Sorting Nexin 2 and Androgen Receptor in the Song System of Juvenile Zebra Finches  

UK PubMed Central (United Kingdom)

Mechanisms regulating sexual differentiation of the zebra finch song system appear to include both genetic and hormonal factors. Sorting Nexin 2 (SNX2), which is involved in trafficking proteins...Full Text Available

2010-07-09

451

Chimeric Antigen Receptor Therapy for B-cell Malignancies  

UK PubMed Central (United Kingdom)

We presented data showing that the CART-19 cells expressing the 4-1BB signaling domain can have unprecedented and massive in-vivo expansion, traffic to tumor sites, persist long term in vivo, and induce...Full Text Available

452

Characterization of Cytokinin and Adenine Transport in Arabidopsis Cell Cultures1[OA  

UK PubMed Central (United Kingdom)

Cytokinins are distributed through the vascular system and trigger responses of target cells via receptor-mediated signal transduction. Perception and transduction of the signal can occur at the plasma...Full Text Available

2008-12-01

453

Cd36, a class B scavenger receptor, functions as a monomer to bind acetylated and oxidized low-density lipoproteins  

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

2007-11-01

454

Catabolite Repression of the Citrate Fermentation Genes in Klebsiella pneumoniae: Evidence for Involvement of the Cyclic AMP Receptor Protein  

UK PubMed Central (United Kingdom)

Klebsiella pneumoniae is able to grow anaerobically with citrate as a sole carbon and energy source by a fermentative pathway involving the Na+-dependent citrate...Full Text Available

2001-09-01

455

Calcium/Calmodulin-Dependent Protein Kinase II Mediates Hippocampal Glutamatergic Plasticity During Benzodiazepine Withdrawal  

UK PubMed Central (United Kingdom)

Benzodiazepine withdrawal anxiety is associated with potentiation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor (AMPAR) currents in hippocampal CA1 pyramidal...Full Text Available

2010-08-01

456

Calcium, Vitamin D, VDR Genotypes, and Epigenetic and Genetic Changes in Rectal Tumors  

UK PubMed Central (United Kingdom)

Calcium, vitamin D, exposure to sunshine, and vitamin D receptor (VDR) genotypes have been associated rectal cancer. We used data from 750 rectal tumors and 1,205 population-based...Full Text Available

2010-05-01

457

CRF receptors in the nucleus accumbens modulate partner preference in prairie voles  

UK PubMed Central (United Kingdom)

Recent evidence suggests a role for corticotropin-releasing factor (CRF) in the regulation of pair bonding in prairie voles. We have previously shown that monogamous and non-monogamous vole...Full Text Available

2007-04-01

458

CD44 as a receptor for colonization of the pharynx by group A Streptococcus  

UK PubMed Central (United Kingdom)

The pharynx is the primary reservoir for strains of group A Streptococcus (GAS) associated both with pharyngitis (streptococcal sore throat) and with invasive or “flesh-eating”...Full Text Available

2000-10-15

459

Breast Cancer Stem-Like Cells Are Inhibited by a Non-Toxic Aryl Hydrocarbon Receptor Agonist  

UK PubMed Central (United Kingdom)

BackgroundCancer stem cells (CSCs) have increased resistance to cancer chemotherapy. They can be enriched as drug-surviving CSCs (D-CSCs) by growth with chemotherapeutic drugs, and/or...Full Text Available

460

Bacterial Particle Endocytosis by Epithelial Cells Is Selective and Enhanced by Tumor Necrosis Factor Receptor Ligands?  

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

2009-03-01

461

Atrial natriuretic peptide signal pathway upregulated in stomach of streptozotocin-induced diabetic mice  

UK PubMed Central (United Kingdom)

AIM: To investigate atrial natriuretic peptide (ANP) secretion from gastric mucosa and the relationship between the ANP/natriuretic peptide receptor type A (NPR-A) pathway and diabetic gastroparesis.METHODS:...Full Text Available

2010-01-07

462

Association Study of Serine Racemase Gene with Methamphetamine Psychosis  

UK PubMed Central (United Kingdom)

Experimental studies have demonstrated that not only dopaminergic signaling but also glutamatergic/NMDA receptor signaling play indispensable roles in the development of methamphetamine psychosis. Our...Full Text Available

2011-03-01

463

Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand  

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

2004-08-01

464

Angiotensin II Promotes Development of the Renal Microcirculation through AT1 Receptors  

UK PubMed Central (United Kingdom)

Pharmacologic or genetic deletion of components of the renin-angiotensin system leads to postnatal kidney injury, but the roles of these components in kidney development are unknown. To test the hypothesis...Full Text Available

2010-03-01

465

Analysis of Protein Covalent Modification by Xenobiotics using a Covert Oxidatively Activated Tag  

UK PubMed Central (United Kingdom)

Numerous xenobiotics, including therapeutics agents, are substrates for bioactivation to electrophilic reactive intermediates that may covalently modify biomolecules. Selective estrogen receptor...Full Text Available

2005-09-01

466

Alterations in the steroid hormone receptor co-chaperone FKBPL are associated with male infertility: a case-control study  

UK PubMed Central (United Kingdom)

BackgroundMale infertility is a common cause of reproductive failure in humans. In mice, targeted deletions of the genes coding for FKBP6 or FKBP52, members of the FK506 binding...Full Text Available

467

Activation of PPAR? induces profound multilocularization of adipocytes in adult mouse white adipose tissues  

UK PubMed Central (United Kingdom)

We sought to determine the effects of activation of peroxisome proliferator-activated receptor-γ (PPAR-γ) on multilocularization of adipocytes in adult white adipose tissue (WAT). Male...Full Text Available

2009-12-31

468

Ability of complement to release systemic lupus erythematosus immune complexes from cell receptors.  

UK PubMed Central (United Kingdom)

Endogenous immune complexes present in sera from 10 different patients with systemic lupus erythematosus (SLE) in an active phase were allowed to bind to Raji cells; the ability of intact complement...Full Text Available

1981-05-01

469

A novel role of the aryl hydrocarbon receptor (AhR) in centrosome amplification - implications for chemoprevention  

UK PubMed Central (United Kingdom)

BackgroundCentrosome aberrations can cause genomic instability and correlate with malignant progression in common human malignancies such as breast and prostate cancer. Deregulation...Full Text Available

470

A membrane-associated progesterone-binding protein, 25-Dx, is regulated by progesterone in brain regions involved in female reproductive behaviors  

UK PubMed Central (United Kingdom)

The ventromedial hypothalamus (VMH) plays a central role in the regulation of the female reproductive behavior lordosis, a behavior dependent upon the sequential activation of receptors for the ovarian...Full Text Available

2000-11-07

471

A homozygous P86S mutation of the human glucagon receptor is associated with hyperglucagonemia, ? cell hyperplasia, and islet cell tumor  

UK PubMed Central (United Kingdom)

ObjectiveThe goal of the study was to investigate the genetic and molecular basis of a novel syndrome of marked hyperglucagonemia and pancreatic α cell hyperplasia...Full Text Available

2009-11-01

472

A Comparison of intra-oral digital imaging modalities: Charged Couple Device versus Storage Phosphor Plate  

UK PubMed Central (United Kingdom)

BackgroundThis in vitro study was conducted to compare the accuracy of two digital image receptors in identifying the location of tip of a fine endodontic file and radiographic apex...Full Text Available

2010-11-01

473

PPAR action in insulin resistance unraveled by metabolomics: potential clinical implications.  

Science.gov (United States)

ABSTRACT: Metabolomic analysis will provide the next large set of clues to further our understanding of human health and disease. A recent study has elucidated the significant differences in the metabolomes of adipocytes, serum and an adipocyte cell line after activation of two nuclear receptors, peroxisome proliferator activated receptor ?/? (PPAR?/?) and PPAR?. These findings hold great promise for explaining fundamental differences in the mechanisms of PPAR agonists and for identifying targets for the treatment of diabetes.See related research article: http://genomebiology.com/2011/12/8/R75. PMID:21861850

2011-08-23

474

Immunity and tolerance to infections in experimental hematopoietic transplantation  

British Library Electronic Table of Contents (United Kingdom)

Resistance and tolerance are two types of host defense mechanisms that increase fitness in response to fungi. Several genetic polymorphisms in pattern recognition receptors, most remarkably Toll-like receptors (TLRs), have been described to influence resistance and tolerance to aspergillosis in distinct clinical settings. TLRs on dendritic cells pivotally contribute in determining the balance between immunopathology and protective immunity to the fungus. Epithelial cells also contribute to this balance via selected TLRs converging on indoleamine-2,3-dioxygenase (IDO). Studies in experimental hematopoietic transplantation confirmed the dichotomy of pathways leading to resistance and tolerance to the fungus providing new insights on the relative contribution of the hematopoietic/nonhematopoi...

2011-01-01

475

A case study of trastuzumab treatment for metastatic breast cancer in pregnancy: fetal risks and management of cerebral metastases  

British Library Electronic Table of Contents (United Kingdom)

Trastuzumab increases survival amongst women with human epidermal growth factor receptor (HER)-2 receptor positive metastatic breast cancer, but maternal and fetal risks are associated with advanced disease and its treatment in pregnancy. We present a case of a primigravid with HER-2 positive metastatic breast cancer who received trastuzumab throughout pregnancy. She presented with cerebral metastases, requiring surgical decompression and resection. Reversible oligohydramnios developed during pregnancy. Fetal safety data on trastuzumab in pregnancy is limited, but case reports suggest a recurring pattern of (mostly reversible) oligohydramnios.

2011-01-01

476

[New cardiotonic agents].  

Science.gov (United States)

The possibilities for therapy in the field of severe cardiac insufficiency have been extended in recent years by the introduction of novel agents endowed with a positive inotropic action. These substances may be arranged in two large classes: sympathomimetic agents and "non sympathomimetic--non digitalis-like" inotropic agents. The stimulant action of noradrenaline, adrenaline and isoproterenol on beta-adrenergic myocardial receptors has been clearly demonstrated but the usefulness of these medicines is limited by their positive chronotropic and arrhythmogenic actions. Dopamine and dobutamine have proved to be very useful in the treatment of patients in intensive care units. However, the exclusively intravenous route of administration limits their importance to the medium or long term. Several compounds, which are active by the oral route, have been the subject of therapeutic trials for the short or medium term. The problems posed by their use result, in the first ...

1985-12-01

477

Localisation of the neuropeptide PACAP and its receptors in the rat parathyroid and thyroid glands.  

Science.gov (United States)

PACAP (pituitary adenylate cyclase activating polypeptide) is widely distributed neuropeptide acting via three subtypes of receptors, PAC(1), VPAC(1) and VPAC(2). Here we examined the localisation and nature of PACAP-immunoreactive nerves in the rat thyroid and parathyroid glands and defined the distribution of PAC(1), VPAC(1) and VPAC(2) receptor mRNA's. In the parathyroid gland a large number of nerve fibres displaying PACAP-immunoreactivity were distributed beneath the capsule, around blood vessels and close to glandular cells. Most of the PACAP-nerves were sensory, since they co-stored CGRP (calcitonin-gene-related peptide) and were sensitive to capsaicin-treatment. mRNA's for PAC(1) and VPAC(2) receptors occurred in the parathyroid gland, mainly located in the glandular cells. In the thyroid gland PACAP-immunoreactive nerve fibres were associated with blood vessels, thyroid follicles and parafollicular C-cells. A high ...

2010-12-19

478

Cloning of the cDNA for the human. beta. /sub 1/-adrenergic receptor  

Energy Technology Data Exchange (ETDEWEB)

Screening of a human placenta lambdagt11 library has led to the isolation of the cDNA for the human ..beta../sub 1/-adrenergic receptor (..beta../sub 1/AR). Used as the probe was the human genomic clone termed G-21. This clone, which contains an intronless gene for a putative receptor, was previously isolated by virtue of its cross hybridization with the human ..beta../sub 2/-adrenergic receptor (..beta../sub 2/AR). The 2.4-kilobase cDNA for the human ..beta../sub 1/AR encodes a protein of 477 amino acid residues that is 69% homologous with the avian ..beta..AR but only 54% homologous with the human ..beta../sub 2/AR. This suggests that the avian gene encoding ..beta..AR and the human gene encoding ..beta../sub 1/AR evolved from a common ancestral gene. RNA blot analysis indicates a message of 2.5 kilobases in rat tissues, with a pattern of tissue distribution consistent with ..beta../sub 1/AR binding. This pattern is quite ...

1987-11-01

479

Thorium different-ligand complexes with morin as analytic form for extraction-photometric determination of thorium microamounts  

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.

1989-01-01

480

Theoretical studies of metal-phosphate interactions: interaction of Li+, Na+, K+, Be++, Mg++, and Ca++ with H2PO4- and (CH3O)2PO2-: implications for nucleic acid solvation.  

UK PubMed Central (United Kingdom)

Model phosphate-metal solvation complexes have been studied by ab-initio self-consistent-field techniques. The complexes studied include (RO)2PO2-(R = H or CH3) with Li+, Na+, K+, Be++, Mg++, Ca++,...Full Text Available

1975-10-01

481

The application of virtual instruments technique in U-H_2 experimental system  

International Nuclear Information System (INIS)

The concept of the modern data acquisition system and some functional specialties of the programming software--Visual Basic 6.0 are introduced. The construction and theory of the hardware and the designing principle of the software are described. Experimental results showed that the real-time data acquisition rate was as high as 10 times per second in the system. And the relative standard uncertainty of the measurement was less than 0.5%. (authors)

2004-11-01

482

The Fenton oxidation mechanism: reactivities of biologically relevant substrates with two oxidizing intermediates differ from those predicted for the hydroxyl radical.  

UK PubMed Central (United Kingdom)

The application of kinetic probes that allow one to determine relative reactivities of biologically relevant substrates with oxidizing intermediates in the Fenton reagent (H2O2 plus Fe2+ in acidic aqueous...Full Text Available

1994-07-05

483

Study of nanocrystallization in FINEMET alloy by active screen plasma nitriding  

International Nuclear Information System (INIS)

The nanocrystallization process of amorphous Fe_7_3_._5Si_1_3_._5B_9Nb_3Cu_1 was investigated by active screen plasma nitriding (ASPN) treatment at temperatures ranging from 410 "oC to 560 "oC for 3 h in two gas mixtures of 75% N_2-25% H_2 and 25% N_2-75% H_2 at 5 mbar atmosphere. The amorphous ribbons were then annealed under vacuum at the same time and temperatures mentioned above. The structure of the samples was analyzed using various techniques such as X-ray diffraction (XRD), atomic force microscopy (AFM) and differential scanning calorimetry (DSC). Microhardness measurements, electrical resistivity and Vibrating Sample Magnetometer (VSM) were used to study mechanical, electrical and magnetic properties of the samples, respectively. It was observed that the ASPN treatment leads to finer grain size and higher crystalline volume fraction and modifies the structural features of Fe(Si) phase. The ...

2010-02-18

484

Shuttle Showcase: STS-124  

National Aeronautics and Space Administration (NASA)

The second in a series of flights to assemble the Japanese segment of the International Space Station saw the mammoth Kibo module delivered to the complex complements of Discovery and its crew on the STS-124 mission. Kibo, the Japanese word for u201chopeu201d would house dozens of experiments and serve as a platform for external payloads brought to the complex on subsequent Shuttle flights and the Japanese u201cKounotoriu201d H-2 Transfer Vehicle cargo ship.

2011-07-10

485

Neutrophil-endothelial cell interaction. Evidence for and mechanisms of the self-protection of bovine microvascular endothelial cells from hydrogen peroxide-induced oxidative stress.  

UK PubMed Central (United Kingdom)

Bovine microvascular endothelial cells (MEC) were able to degrade the H2O2 generated by phorbol myristate acetate-activated bovine neutrophils or by glucose oxidase with a maximal capacity of 4.0 +/-...Full Text Available

1986-08-01

486

Mechanism of denting corrosion  

International Nuclear Information System (INIS)

The rapid corrosion of carbon steels in high temperature, acid chloride solutions is shown to be rate limited by the anodic reaction, 3Fe + 4H_2O = Fe_3O_4 + 8H"+ + 8e"-, based on experiments which find that the corrosion rate in 0.1M NiCl_2 solution has an activation energy of 60 kJ/ mole and is unaffected by adding NaCl or by replacing NiCl_2 with PtCl_4. (author).

487

MOS device chemical response reversal with temperature  

British Library Electronic Table of Contents (United Kingdom)

Biased above threshold (VT), pulsed photocurrent (u) measurements on windowed silicon Pd gate MOS capacitors are shifted (DV) negatively by H2/N2, whereas Au gates shift positively under NO2/air. Below VT, the shifts are reversed by adjustments of interface state population. Minor temperature increases may coax the device from inversion to depletion, inducing sign reversal of the chemical response.

2010-01-01

488

Light emission from grazing incidence interaction of light ions with clean Cu(110)  

International Nuclear Information System (INIS)

Photon yields were measured from Cu(110) bombarded by H"+, H_2"+ and He"+ with different energies. The energy dependence is different from previous studies at perpendicular incidence. A calculation of the energy dependence of resonant charge capture into the n=3 state of H is compared with experiment. (G.Q.).

1983-02-04

489

Detection of Shiga Toxin-Producing Escherichia coli Serotypes O26:H11, O103:H2, O111:H8, O145:H28, and O157:H7 in Raw-Milk Cheeses by Using Multiplex Real-Time PCR ?  

UK PubMed Central (United Kingdom)

Shiga toxin (Stx)-producing Escherichia coli (STEC) strains are a diverse group of food-borne pathogens with various levels of virulence for humans. In this study, we describe the use...Full Text Available

2011-03-01

490

Amino acid sequences that determine the nuclear localization of yeast histone 2B.  

UK PubMed Central (United Kingdom)

Histone-beta-galactosidase protein fusions were used to identify the domain of yeast histone 2B, which targets this protein to the nucleus. Amino acids 28 to 33 in H2B were required for nuclear localization...Full Text Available

1987-11-01

491

A new type of scorpion Na+-channel-toxin-like polypeptide active on K+ channels  

UK PubMed Central (United Kingdom)

We have purified and characterized two peptides, named KAaH1 and KAaH2 (AaH polypeptides 1 and 2 active on K+ channels, where AaH stands for Androctonus australis Hector),...Full Text Available

2005-06-01

492

Further evidence for particle nucleation in clear air adjacent to marine cumulus clouds  

Science.gov (United States)

Observational evidence is presented for the nucleation of condensation nuclei (CN) in the clear air adjacent to an isolated, marine, cumulus cloud. Two separate regions of particle nucleation are identified: one located above the cloud top, and the second located downwind of the cloud near the level of the anvil outflow. The regions of high CN concentrations were located in extremely clean marine air, with unactivated aerosol surface area (excluding the nucleation mode) less than 2 sq micrometers/cu cm, air temperature -31 C, and higher relative humidities than the undisturbed environment. Vertical profile measurements downwind of the cloud showed that CN concentrations at the level of the anvil outflow (4.9 km) were 8 times greater than at any other level between the surface and 5.3 km. A conceptual model is formulated in which aerosol particles, sulfur dioxide (SO2), sulfuric acid vapor (H2SO4), dimethyl sulfide (DMS), and ozone (O3) from the ...

1994-11-01

493

A single amino acid substitution (R441A) in the receptor-binding domain of SARS coronavirus spike protein disrupts the antigenic structure and binding activity  

International Nuclear Information System (INIS)

The spike (S) protein of severe acute respiratory syndrome coronavirus (SARS-CoV) has two major functions: interacting with the receptor to mediate virus entry and inducing protective immunity. Coincidently, the receptor-binding domain (RBD, residues 318-510) of SAR-CoV S protein is a major antigenic site to induce neutralizing antibodies. Here, we used RBD-Fc, a fusion protein containing the RBD and human IgG1 Fc, as a model in the studies and found that a single amino acid substitution in the RBD (R441A) could abolish the immunogenicity of RBD to induce neutralizing antibodies in immunized mice and rabbits. With a panel of anti-RBD mAbs as probes, we observed that R441A substitution was able to disrupt the majority of neutralizing epitopes in the RBD, suggesting that this residue is critical for the antigenic structure responsible for inducing protective immune responses. We also demonstrated that the RBD-Fc bearing R441A mutation could not ...

2006-05-26

494

A Phase III Extension Trial With a 1-Arm Crossover From Leuprolide to Degarelix: Comparison of Gonadotropin-Releasing Hormone Agonist and Antagonist Effect on Prostate Cancer  

British Library Electronic Table of Contents (United Kingdom)

PurposeWe investigated the efficacy and safety of degarelix treatment and the effects of switching from leuprolide to degarelix in an ongoing extension study with a median 27.5-month followup of a pivotal 1-year prostate cancer trial. Materials and MethodsPatients who completed a 1-year pivotal phase III trial continued on the same monthly degarelix maintenance dose (160 or 80 mg in 125 each), or were re-randomized from leuprolide 7.5 mg to degarelix 240/80 mg (69) or 240/160 mg (65). Data are shown on the approved degarelix 240/80 mg dose. The primary end point was safety/tolerability and the secondary end points were testosterone, prostate specific antigen, luteinizing hormone and follicle-stimulating hormone responses, and prostate specific antigen failure and progression-free survival....

2011-01-01

495

Inflammatory spine disease as a cause of back pain; Entzuendliche Wirbelsaeulenerkrankungen als Ursache fuer Rueckenschmerzen  

Energy Technology Data Exchange (ETDEWEB)

The aim of this review is to evaluate the role of inflammatory spine disease in patients with chronic back pain. The contribution of imaging modalities for the diagnostic evaluation of back pain is discussed. A systematic literature search based on the classification of seronegative spondyloarthropathies and rheumatoid arthritis was performed. The results of this search and the experiences in a large collective of rheumatological patients are analyzed. The prevalence of rheumatoid arthritis (1-2%) is comparable to that of spondyloarthropathies (1.9%). The etiology of these entities is not fully elucidated. Magnetic resonance imaging is increasingly used for early detection and surveillance of therapy with TNF-{alpha} antagonists. Bone marrow edema, which is only detectable with MRI, represents an early sign of inflammation. Therapy with TNF-{alpha} antagonists is based on clinical and laboratory criteria, and signs of inflammation in MRI. MRI ...

2006-06-15

496

The synthesis of (1',3'- sup 3 H)4-(4'-azido-5',6',7',8'-tetrahydro-5',5',8',8'-tetramethyl -2'-anthracenyl)benzoic acid as a probe of the retinoic acid receptor  

Energy Technology Data Exchange (ETDEWEB)

The synthesis of (1',3'-{sup 3}H)4-(4'-azido-5',6',7',8'-tetrahydro-5'5'8',8'-tetramethyl-2'-anthracenyl)benzoic acid is described. This retinoid was designed as a photoaffinity probe of the receptor sites of cellular retinoic acid-binding protein and the nuclear retinoic acid receptor protein. The ({sup 3}H)azidoretinoid was prepared from 1,2,3,4-tetrahydro-1,1,4,4-tetra-methyl-7-(4-methylphenyl)-5-nitroanthracene in five steps in 15% yield (89% radiochemical purity by HPLC). {sup 1}H and {sup 3}H NMR was used to confirm the sites of {sup 3}H substitution on the ring. (author).

1990-01-01

497

Natriuretic peptides in the pathophysiology of congestive heart failure.  

Science.gov (United States)

A hallmark of congestive heart failure (CHF) is the activation of the cardiac endocrine system, in particular atrial natriuretic peptide (ANP) and brain natriuretic peptide (BNP). The natriuretic peptides are a group of structurally similar but genetically distinct peptides that have diverse actions in cardiovascular, renal, and endocrine homeostasis. ANP and BNP are of myocardial cell origin and C-type natriuretic peptide (CNP) is of endothelial origin. ANP and BNP bind to the natriuretic peptide-A receptor (NPR-A), which, via 3',5'-cyclic guanosine monophosphate (cGMP), mediates natriuresis, vasodilatation, renin inhibition, antimitogenesis, and lusitropic properties. CNP lacks natriuretic actions but possesses vasodilating and growth inhibiting actions via the guanylyl cyclase-linked natriuretic peptide-B receptor. All three peptides are cleared by the natriuretic peptide-C receptor and degraded by the ectoenzyme neutral ...

2000-05-01

498

Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor  

Energy Technology Data Exchange (ETDEWEB)

Crystallography and computer modeling have been used to exploit a previously unexplored channel in the glucocorticoid receptor (GR). Highly potent, nonsteroidal indazole amides showing excellent complementarity to the channel were designed with the assistance of the computational technique AlleGrow. The accuracy of the design process was demonstrated through crystallographic structural determination of the GR ligand-binding domain-agonist complex of the D-prolinamide derivative 11. The utility of the channel was further exemplified through the design of a potent phenylindazole in which structural motifs, seen to interact with the traditional GR ligand pocket, were abandoned and replaced by interactions within the new channel. Occupation of the channel was confirmed with a second GR crystal structure of this truncated D-alaninamide derivative 13. Compound 11 displays properties compatible with development as an intranasal solution formulation, whereas oral ...

2010-09-17

499

Cloning and mapping of the mouse {alpha}7-neuronal nicotinic acetylcholine receptor  

Energy Technology Data Exchange (ETDEWEB)

We report the isolation of cDNA clones for the mouse {alpha}7 neuronal nicotinic acetylcholine receptor subunit (gene symbol Acra7), the only nicotinic receptor subunit known to bind a-bungarotoxin in mammalian brain. This gene may have relevance to nicotine sensitivity and to some electrophysiologic findings in schizophrenia. The mouse {alpha}7 subunit gene encodes a protein of 502 amino acids with substantial identity to the rat (99.6%), human (92.8%), and chicken (87.5%) amino acid sequences. The {alpha}7 gene was mapped to mouse chromosome 7 near the p locus with the following gene order from proximal to distal: Myod1-3.5 {+-}1.7 cM-Gas2-0.9 cM {+-} 0.9 cM-D7Mit70-1.8 {+-} 1.2 cM- Acra7-4.4 {+-}1.0 cM-Hras1-ps11/Igf1r/Snrp2a. The human gene was confirmed to map to the homologous region of human chromosome 15q13-q14. 26 refs., 3 figs.

1995-03-20

500

Assessment of epidermal growth factor receptor (EGFR, ErbB1) and HER2 (ErbB2) protein expression levels and response to lapatinib (Tykerb, GW572016) in an expanded panel of human normal and tumour cell lines  

British Library Electronic Table of Contents (United Kingdom)

Abstract. Objective: Lapatinib (Tykerb, GW572016), a potent inhibitor of the catalytic activities of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) (ErbB2), inhibits population growth of selected EGFR and HER2 overexpressing cell lines. Previous studies with a small number of cell lines suggest a correlation between overexpression of EGFR and/or HER2 and sensitivity to growth inhibition by lapatinib; however, the precise determinants of lapatinib selectivity for tumour and/or other cells remain unclear. Materials and methods: To clarify the determinants of its selectivity in cultured cells, lapatinib-induced cell population growth inhibition and relative EGFR and HER2 protein expression were quantified in 61 different human tumour cell lines fro...

2007-01-01