Localization of P2X purinoceptor transcripts in the rat nervous system.

abstract：:Capacitative Ca2+ influx, which occurs in response to mobilization of intracellular Ca2+ stores, is a general feature of many cell types. Although the mechanism of capacitative Ca2+ entry is not known, evidence suggests the involvement of small G proteins that are prenylated on a cysteine residue near their carboxyl t...

journal_title：Molecular pharmacology

authors： Xu Y,Gilbert BA,Rando RR,Chen L,Tashjian AH Jr

更新日期：1996-12-01 00:00:00

abstract：:The binding kinetics of [3H]Ro 15-1788, a selective benzodiazepine receptor antagonist, to synaptosomal membranes of rat cerebral cortices was studied. [3H]Ro 15-1788 binds with high affinity (dissociation constant, 0.53 nM) to a single class of binding sites (maximal binding capacity, 1.97 pmoles/mg of protein). Equi...

journal_title：Molecular pharmacology

authors： Chiu TH,Rosenberg HC

更新日期：1983-03-01 00:00:00

abstract：:The constitutive androstane receptor (CAR) and the pregnane X receptor (PXR) play a major part in the control of drug metabolism and transport. We have previously shown that PXR and CAR expression is controlled by the glucocorticoid receptor (GR) and proposed the existence of a signal transmission cascade GR-(PXR/CAR)...

journal_title：Molecular pharmacology

authors： Duret C,Daujat-Chavanieu M,Pascussi JM,Pichard-Garcia L,Balaguer P,Fabre JM,Vilarem MJ,Maurel P,Gerbal-Chaloin S

更新日期：2006-07-01 00:00:00

abstract：:The interaction of [3H]acetylcholine ([3H]AcCh) with the muscarinic receptor was studied in seven distinct rat brain regions and in heart atrium by employing 10 microM atropine to define specific binding. The specific binding exhibited by the labeled neurotransmitter was found to be sensitive to muscarinic but not to ...

journal_title：Molecular pharmacology

authors： Gurwitz D,Kloog Y,Sokolovsky M

更新日期：1985-09-01 00:00:00

abstract：:In an effort to combine the benefits of fibrinolytics, such as staphylokinase, with those of thrombin inhibitors for the prevention of vessel reocclusion after vascular injury, we have produced several chimeric proteins with plasminogen-activating and thrombin-inhibiting properties. Fusion proteins were constructed co...

journal_title：Molecular pharmacology

authors： Icke C,Schlott B,Ohlenschläger O,Hartmann M,Gührs KH,Glusa E

更新日期：2002-08-01 00:00:00

abstract：:[3H]-d-cis-Diltiazem binds to canine cardiac sarcolemma in a specific, saturable, and reversible manner with a KD = 58.0 +/- 9.5 nM and a receptor site density (maximum binding) of 2.19 +/- 0.24 pmol/mg of protein. Bepridil and verapamil, Ca2+ channel inhibitors, can completely inhibit this binding at nM concentration...

journal_title：Molecular pharmacology

authors： Balwierczak JL,Johnson CL,Schwartz A

更新日期：1987-02-01 00:00:00

abstract：:Our previous studies suggested that the dNTP/dNDP transporter systems that exist in mitochondria for transporting dNTP/dNDP from the cytoplasm to the mitochondria for mitochondrial DNA (mtDNA) synthesis play a critical role in delayed cytotoxicity of anti-human immunodeficiency virus (HIV) dideoxynucleoside analogs in...

journal_title：Molecular pharmacology

authors： Lam W,Chen C,Ruan S,Leung CH,Cheng YC

更新日期：2005-02-01 00:00:00

abstract：:Prolonged ethanol exposure causes central nervous system hyperexcitability that involves a loss of GABAergic inhibition. We previously demonstrated that long-term ethanol exposure enhances the internalization of synaptic GABA(A) receptors composed of alpha1beta2/3gamma2 subunits. However, the mechanisms of ethanol-med...

journal_title：Molecular pharmacology

authors： Kumar S,Suryanarayanan A,Boyd KN,Comerford CE,Lai MA,Ren Q,Morrow AL

更新日期：2010-05-01 00:00:00

abstract：:Reuptake of glutamate in astrocytes, a critical mechanism involved in the maintenance of physiological excitatory amino acid neurotransmission, is inhibited by both arachidonic acid (AA) and reactive oxygen species (ROS), via incompletely defined molecular mechanisms. Because ROS are generated during AA metabolism and...

journal_title：Molecular pharmacology

authors： Volterra A,Trotti D,Racagni G

更新日期：1994-11-01 00:00:00

abstract：:Cadmium is a dangerous metal distributed widely in the environment. Members of our laboratory recently identified the ZIP8 transporter protein, encoded by the mouse Slc39a8 gene, to be responsible for genetic differences in response to cadmium damage of the testis. Stable retroviral infection of the ZIP8 cDNA in mouse...

journal_title：Molecular pharmacology

authors： He L,Girijashanker K,Dalton TP,Reed J,Li H,Soleimani M,Nebert DW

更新日期：2006-07-01 00:00:00

abstract：:We investigated the roles of cyclic GMP and cyclic AMP in the inhibition of rabbit platelet aggregation and degranulation by two nitrovasodilators, sodium nitroprusside (SNP) and 3-morpholinosydnonimine (SIN-1; the active metabolite of molsidomine), with particular reference to the synergistic interaction of these dru...

journal_title：Molecular pharmacology

authors： Maurice DH,Haslam RJ

更新日期：1990-05-01 00:00:00

abstract：:Melanocortins (MCs) have various physiological actions on the brain. The recent cloning of neural MC receptors opened new avenues to study the effects of these neuropeptides on the nervous system. Here we investigated the structure-activity relationships (SARs) of peptides derived from adrenocorticotropic hormone (ACT...

journal_title：Molecular pharmacology

authors： Adan RA,Cone RD,Burbach JP,Gispen WH

更新日期：1994-12-01 00:00:00

abstract：:Although ATP-sensitive K+ channels continue to be explored for their therapeutic potential, developments in high-affinity radioligands to investigate native and recombinant KATP channels have been less forthcoming. This study reports the identification and pharmacological characterization of a novel iodinated 1,4-dihy...

journal_title：Molecular pharmacology

authors： Davis-Taber R,Molinari EJ,Altenbach RJ,Whiteaker KL,Shieh CC,Rotert G,Buckner SA,Malysz J,Milicic I,McDermott JS,Gintant GA,Coghlan MJ,Carroll WA,Scott VE,Gopalakrishnan M

更新日期：2003-07-01 00:00:00

abstract：:The phosphatidylcholine-using phospholipase D (PLD) isoform PLD2 is widely expressed in mammalian cells and is activated in response to a variety of promitogenic agonists. In this study, active and inactive hemagglutinin-tagged human PLD2 (HA-PLD2) constructs were stably expressed in an EL4 cell line lacking detectabl...

journal_title：Molecular pharmacology

authors： Knoepp SM,Chahal MS,Xie Y,Zhang Z,Brauner DJ,Hallman MA,Robinson SA,Han S,Imai M,Tomlinson S,Meier KE

更新日期：2008-09-01 00:00:00

abstract：:Intermediate-conductance (KCa3.1) and small-conductance (KCa2) calcium-activated K+ channels are gated by calcium binding to calmodulin (CaM) molecules associated with the calmodulin-binding domain (CaM-BD) of these channels. The existing KCa activators, such as naphtho[1,2-d]thiazol-2-ylamine (SKA-31), 6,7-dichloro-1...

journal_title：Molecular pharmacology

authors： Brown BM,Shim H,Zhang M,Yarov-Yarovoy V,Wulff H

更新日期：2017-10-01 00:00:00

abstract：:Valproic acid (VPA) is a widely used antiepileptic agent that is undergoing clinical evaluation for anticancer therapy. We assessed the effects of VPA on angiogenesis in vitro and in vivo. In human umbilical vein endothelial cells, therapeutically relevant concentrations of VPA (0.25 to 1 mM) inhibited proliferation, ...

journal_title：Molecular pharmacology

authors： Michaelis M,Michaelis UR,Fleming I,Suhan T,Cinatl J,Blaheta RA,Hoffmann K,Kotchetkov R,Busse R,Nau H,Cinatl J Jr

更新日期：2004-03-01 00:00:00

abstract：:Allosteric modulators of G-protein-coupled receptors can regulate conformational states involved in receptor activation ( Mol Pharmacol 58: 1412-1423, 2000 ). This hypothesis was investigated for the corticotropin-releasing factor type 1 (CRF(1)) receptor using a novel series of ligands with varying allosteric effect ...

journal_title：Molecular pharmacology

authors： Hoare SR,Fleck BA,Gross RS,Crowe PD,Williams JP,Grigoriadis DE

更新日期：2008-05-01 00:00:00

abstract：:A fusion protein consisting of the endothelin B (ET(B)) receptor and the enhanced green fluorescent protein (EGFP) in conjunction with Cyanin3- or fluorescein-conjugated endothelin 1 (Cy3-ET1, Fluo-ET1) was used to investigate the ligand-mediated internalization of the ET(B) receptor. The ET(B) receptor and the ET(B)/...

journal_title：Molecular pharmacology

authors： Oksche A,Boese G,Horstmeyer A,Furkert J,Beyermann M,Bienert M,Rosenthal W

更新日期：2000-06-01 00:00:00

abstract：:The epithelial sodium channel (ENaC) is believed to represent the rate-limiting step for sodium absorption in the renal collecting duct. Consequently, ENaC is a central effector affecting systemic blood volume and pressure. Sodium and water transport are dysregulated in diabetes mellitus. Peroxisome proliferator-activ...

journal_title：Molecular pharmacology

authors： Pavlov TS,Levchenko V,Karpushev AV,Vandewalle A,Staruschenko A

更新日期：2009-12-01 00:00:00

abstract：:A number of different agonists activate G protein-coupled receptors to stimulate adenylyl cyclase (AC), increase cAMP formation, and promote relaxation in vascular smooth muscle. To more fully understand this stimulation of AC, we assessed the expression, regulation, and compartmentation of AC isoforms in rat aortic s...

journal_title：Molecular pharmacology

authors： Ostrom RS,Liu X,Head BP,Gregorian C,Seasholtz TM,Insel PA

更新日期：2002-11-01 00:00:00

abstract：:Isoproterenol increases and decreases contractile force at low and high concentrations, respectively, through beta(2)-adrenoceptors overexpressed in transgenic mouse heart (TG4), consistent with activation of both G(s) and G(i) proteins. Using TG4 hearts, we demonstrated that epinephrine behaves like isoproterenol, bu...

journal_title：Molecular pharmacology

authors： Heubach JF,Ravens U,Kaumann AJ

更新日期：2004-05-01 00:00:00

abstract：:Adaptive changes in gene expression are thought to contribute to dependence, addiction and other behavioral responses to chronic ethanol abuse. DNA array studies provide a nonbiased detection of networks of gene expression changes, allowing insight into functional consequences and mechanisms of such molecular response...

journal_title：Molecular pharmacology

authors： Thibault C,Lai C,Wilke N,Duong B,Olive MF,Rahman S,Dong H,Hodge CW,Lockhart DJ,Miles MF

更新日期：2000-12-01 00:00:00

abstract：:Human and bovine dopamine transporters (DAT) demonstrate discrete functional differences in dopamine (DA), 1-methyl-4-phenylpyridium (MPP(+)) transport, and cocaine analog binding. In a previous study, the functional analyses on the chimeras of human and bovine DAT have revealed that the region from residues 133 throu...

journal_title：Molecular pharmacology

authors： Lee SH,Chang MY,Lee KH,Park BS,Lee YS,Chin HR,Lee YS

更新日期：2000-05-01 00:00:00

abstract：:Cross-talk between G protein-coupled receptors and protein tyrosine kinases is well established, but the phenotypic consequences of these signaling interactions are not completely understood. To investigate the role of Src family kinases in mitogenic signaling by G protein-coupled receptors, we used genetic and pharma...

journal_title：Molecular pharmacology

authors： Mishra R,Wang Y,Simonson MS

更新日期：2005-06-01 00:00:00

abstract：:Lead (Pb(2+)) is a well-known inhibitor of voltage-dependent Ca(2+) channels in their native environments in several types of cells. However, its effects on discrete Ca(2+) channel phenotypes in isolation have not been well studied. We compared how specific subtypes of human neuronal high-voltage-activated Ca(2+) chan...

journal_title：Molecular pharmacology

authors： Peng S,Hajela RK,Atchison WD

更新日期：2002-12-01 00:00:00

abstract：:We showed previously that subtypes of alpha 1-adrenergic receptors can be differentiated by selective inactivation with chlorethylclonidine (CEC) [Mol. Pharmacol. 32:505-510 (1987)] or by their affinities for the competitive antagonist WB 4101 [Nature (Lond.) 329:333-335 (1987)]. Examining eight rat tissues, the propo...

journal_title：Molecular pharmacology

authors： Minneman KP,Han C,Abel PW

更新日期：1988-05-01 00:00:00

abstract：:GH3 cells show spontaneous activity characterized by bursts of action potentials and oscillations in [Ca 2+]i. This activity is modulated by the activation of exogenously expressed opioid receptors. In GH3 cells expressing only micro receptors (GH3MOR cells), the micro receptor-specific ligand [D-Ala2,N-Me-Phe4,Gly5-o...

journal_title：Molecular pharmacology

authors： Charles AC,Mostovskaya N,Asas K,Evans CJ,Dankovich ML,Hales TG

更新日期：2003-01-01 00:00:00

abstract：:Based on their relative affinities for cholecystokinin octapeptide (26-33) (CCK-8), cholecystokinin tetrapeptide (30-33) (CCK-4), desulfated CCK-8, and gastrin, cholecystokinin (CCK) receptors have been classified as CCK-A (alimentary) and CCK-B (brain). Selective nonpeptide antagonists of CCK-A and CCK-B receptors, a...

journal_title：Molecular pharmacology

authors： Lin CW,Shiosaki K,Miller TR,Witte DG,Bianchi BR,Wolfram CA,Kopecka H,Craig R,Wagenaar F,Nadzan AM

更新日期：1991-03-01 00:00:00

abstract：:Magnesium modulates hormone-sensitive adenylate cyclase activation. In the present studies, we have examined the magnesium requirement of beta-adrenergic-stimulated adenylate cyclase activity in permeabilized human lymphocytes. Following isoproterenol pretreatment, under conditions that lead to homologous beta-adrener...

journal_title：Molecular pharmacology

authors： Feldman RD

更新日期：1989-03-01 00:00:00

abstract：:The presence of DNA damage initiates signaling through the ataxia-telangiectasia mutated kinase (ATM) and the ATM- and the Rad3-related kinase (ATR), which phosphorylate, thus activating, the checkpoint kinases (Chk) 1 and 2, which leads to cell cycle arrest. The bifunctional DNA alkylator 1,3-bis(2-chloroethyl)-1-nit...

journal_title：Molecular pharmacology

authors： Cui B,Johnson SP,Bullock N,Ali-Osman F,Bigner DD,Friedman HS

更新日期：2009-06-01 00:00:00