An efficacy-dependent effect of cardiac overexpression of beta2-adrenoceptor on ligand affinity in transgenic mice.

abstract：:Activators of G protein signaling (AGS), initially discovered in the search for receptor-independent activators of G protein signaling, define a broad panel of biologic regulators that influence signal transfer from receptor to G-protein, guanine nucleotide binding and hydrolysis, G protein subunit interactions, and/o...

journal_title：Molecular pharmacology

authors： Blumer JB,Lanier SM

更新日期：2014-03-01 00:00:00

abstract：:Multidrug and toxin extrusion 1 (MATE1/SLC47A1) is important for excretion of organic cations in the kidney and liver, where it is located on the luminal side. Although its functional and regulatory characteristics have been clarified, its pharmacokinetic roles in vivo have yet to be elucidated. In the present study, ...

journal_title：Molecular pharmacology

authors： Tsuda M,Terada T,Mizuno T,Katsura T,Shimakura J,Inui K

更新日期：2009-06-01 00:00:00

abstract：:Glucose utilization in isolated islets of Langerhans of the rat was determined by measuring the conversion of [5-3H]glucose (10 mM) to 3H2O. The alpha 2-adrenoceptor agonists clonidine, epinephrine, and norepinephrine in the presence of the alpha 1-adrenoceptor antagonist prazosin and the beta-adrenoceptor antagonist ...

journal_title：Molecular pharmacology

authors： Laychock SG

更新日期：1987-08-01 00:00:00

abstract：:The effect of endocytosis inhibitors on 5-hydroxytryptamine(2A) (5-HT(2A)) receptor desensitization and resensitization was examined in transiently transfected human embryonic kidney (HEK) 293 cells and in C6 glioma cells that endogenously express 5-HT(2A) receptors. In HEK-293 cells, 5-HT(2A) receptor desensitization...

journal_title：Molecular pharmacology

authors： Gray JA,Sheffler DJ,Bhatnagar A,Woods JA,Hufeisen SJ,Benovic JL,Roth BL

更新日期：2001-11-01 00:00:00

abstract：:Recent years have witnessed the discovery of novel selective agonists of the M(1) muscarinic acetylcholine (ACh) receptor (mAChR). One mechanism invoked to account for the selectivity of such agents is that they interact with allosteric sites. We investigated the molecular pharmacology of two such agonists, 1-[3-(4-bu...

journal_title：Molecular pharmacology

authors： Avlani VA,Langmead CJ,Guida E,Wood MD,Tehan BG,Herdon HJ,Watson JM,Sexton PM,Christopoulos A

更新日期：2010-07-01 00:00:00

abstract：:Tumor suppressor gene BRCA1 is frequently mutated in familial breast and ovarian cancer. BRCA1 plays pivotal roles in maintaining genomic stability by interacting with numerous proteins in cell cycle control and DNA repair. Irofulven (6-hydroxymethylacylfulvene, HMAF, MGI 114, NSC 683863) is one of a new class of anti...

journal_title：Molecular pharmacology

authors： Wiltshire T,Senft J,Wang Y,Konat GW,Wenger SL,Reed E,Wang W

更新日期：2007-04-01 00:00:00

abstract：:To study the molecular pharmacology of low-voltage-activated calcium channels in biophysical detail, human medullary thyroid carcinoma (hMTC) cells were investigated using the single-channel technique. These cells had been reported to express T-type whole-cell currents and a Ca(v)3.2 (or alpha 1H) channel subunit. We ...

journal_title：Molecular pharmacology

authors： Michels G,Matthes J,Handrock R,Kuchinke U,Groner F,Cribbs LL,Pereverzev A,Schneider T,Perez-Reyes E,Herzig S

更新日期：2002-03-01 00:00:00

abstract：:In the human lymphocyte, desensitization of the beta-adrenergic receptor-adenylate cyclase complex is associated with sequestration of the receptor as well as a change in photolabeling of beta-receptor proteins. Thus, desensitization of the lymphocyte beta-adrenergic receptor-adenylate cyclase system is associated wit...

journal_title：Molecular pharmacology

authors： Feldman RD,McArdle W,Lai C

更新日期：1986-11-01 00:00:00

abstract：:The catestatin fragment of chromogranin A is an endogenous inhibitor of nicotinic cholinergic transmission, functioning in negative feedback control of catecholamine secretion. We explored naturally occurring polymorphisms in the amino acid sequence of catestatin. Three human variants were identified: Gly364Ser, Pro37...

journal_title：Molecular pharmacology

authors： Mahata SK,Mahata M,Wen G,Wong WB,Mahapatra NR,Hamilton BA,O'Connor DT

更新日期：2004-11-01 00:00:00

abstract：:Peroxisome proliferator-activated receptors (PPARs) are a family of nuclear receptors that are involved in lipid metabolism, differentiation, proliferation, cell death, and inflammation. Three subtypes have been identified: PPAR-alpha, -delta, and -gamma. We have previously shown presence of PPAR-gamma mRNA in the amn...

journal_title：Molecular pharmacology

authors： Berry EB,Eykholt R,Helliwell RJ,Gilmour RS,Mitchell MD,Marvin KW

更新日期：2003-12-01 00:00:00

abstract：:Acute desensitization of mu opioid receptors is thought to be an initial step in the development of tolerance to opioids. Given the resistance of the respiratory system to develop tolerance, desensitization of neurons in the Kölliker-Fuse (KF), a key area in the respiratory circuit, was examined. The activation of G p...

journal_title：Molecular pharmacology

authors： Levitt ES,Williams JT

更新日期：2018-01-01 00:00:00

abstract：:1-Deoxynojirimycin (DNM) is a saccharide decoy that inhibits cellular alpha-glucosidase I-II activity. Treatment by DNM of human immunodeficiency virus (HIV)-infected lymphocyte cultures inhibits virus spread. The functional properties of the membrane-associated Env glycoprotein (Env) modified in the presence of DNM r...

journal_title：Molecular pharmacology

authors： Papandréou MJ,Barbouche R,Guieu R,Kieny MP,Fenouillet E

更新日期：2002-01-01 00:00:00

abstract：:Electrical recordings were made in Xenopus oocytes to study the modulatory effects of steroids on gamma-aminobutyric acid (GABA) receptors expressed by RNA from mammalian brain and retina. GABA responses expressed by rat cerebral cortex poly(A)+ RNA were bicuculline-sensitive Cl- currents mediated by GABAA receptors. ...

journal_title：Molecular pharmacology

authors： Woodward RM,Polenzani L,Miledi R

更新日期：1992-01-01 00:00:00

abstract：:This article describes the expected phenotypic behavior of all types of ligands in constitutively active receptor systems and, in particular, the molecular mechanisms of inverse agonism. The possible physiological relevance of inverse agonism also is discussed. Competitive antagonists with the molecular property of ne...

journal_title：Molecular pharmacology

authors： Kenakin T

更新日期：2004-01-01 00:00:00

abstract：:The effect of ethanol on intracellular ionized calcium concentrations (Cai) was studied in synaptosomes isolated from mouse whole brain and in hepatocytes isolated from rat liver. The fluorescent calcium chelator, fura-2, was used to quantitate Cai. Incubation of synaptosomes with ethanol (350-700 mM) increased restin...

journal_title：Molecular pharmacology

authors： Daniell LC,Brass EP,Harris RA

更新日期：1987-12-01 00:00:00

abstract：:Lack of high potency agonists has restricted analysis of the G protein-coupled receptor GPR35. Moreover, marked variation in potency and/or affinity of current ligands between human and rodent orthologs of GPR35 has limited their productive use in rodent models of physiology. Based on the reported modest potency of th...

journal_title：Molecular pharmacology

authors： MacKenzie AE,Caltabiano G,Kent TC,Jenkins L,McCallum JE,Hudson BD,Nicklin SA,Fawcett L,Markwick R,Charlton SJ,Milligan G

更新日期：2014-01-01 00:00:00

abstract：:The ADP-sensitive and K+ -sensitive phosphorylated forms of Na,K-ATPase (E1P and E2P, respectively) are believed to be the main phosphorylated intermediates of Na,K-ATPase. In the presence of 100 mM Na+, E2P is the major component of the phosphorylated form in all native Na,K-ATPase preparations known, including the m...

journal_title：Molecular pharmacology

authors： Yoda A,Yoda S

更新日期：1982-11-01 00:00:00

abstract：:Two forms of the multisubunit gamma-aminobutyric acid (GABA)A receptor were expressed in Xenopus oocytes by injecting mRNA encoding the bovine GABAA receptor subunit cDNAs for alpha 1 beta 1 gamma 2L and alpha 3 beta 1 gamma 2L. The properties of these two combinations were examined by electrophysiological recording o...

journal_title：Molecular pharmacology

authors： Wafford KA,Whiting PJ,Kemp JA

更新日期：1993-02-01 00:00:00

abstract：:Metabolism of [3H]-(+/-)-trans-1,2-dihydroxy-1,2-dihydrobenz[a] anthracene by liver microsomes isolated from control, phenobarbital-treated, and 3-methylcholanthrene-treated Long-Evans rats and from 3-methylcholanthrene-treated Sprague-Dawley rats was examined. Liver microsomes from both control and phenobarbital-trea...

journal_title：Molecular pharmacology

authors： Vyas KP,van Bladeren PJ,Thakker DR,Yagi H,Sayer JM,Levin W,Jerina DM

更新日期：1983-07-01 00:00:00

abstract：:The nuclear receptor peroxisome proliferator-activated receptor (PPAR) is activated by a diverse group of acidic ligands, including many peroxisome proliferator chemicals present in the environment. Janus tyrosine kinase-signal transducer and activator of transcription (JAK-STAT) signaling is activated by multiple cyt...

journal_title：Molecular pharmacology

authors： Shipley JM,Waxman DJ

更新日期：2003-08-01 00:00:00

abstract：:Glyceryl trinitrate (GTN) is used in the treatment of angina pectoris and cardiac failure, but the rapid onset of GTN tolerance limits its clinical utility. Research suggests that a principal cause of tolerance is inhibition of an enzyme responsible for the production of physiologically active concentrations of NO fro...

journal_title：Molecular pharmacology

authors： DiFabio J,Ji Y,Vasiliou V,Thatcher GR,Bennett BM

更新日期：2003-11-01 00:00:00

abstract：:(+/-)-6' beta-Fluoroaristeromycin (F-C-Ado) is a potent and competitive inhibitor of purified S-adenosylhomocysteine (AdoHcy) hydrolase isolated from murine L929 cells (Ki = 3.1 nM). It also inhibits vaccinia virus and vesicular stomatitis virus replication in L929 cells, at a 90% inhibitory dose (ID90) of 3.5 and 13 ...

journal_title：Molecular pharmacology

authors： Cools M,Balzarini J,De Clercq E

更新日期：1991-06-01 00:00:00

abstract：:We have investigated the effect of chronic flurazepam HCl treatment on the gamma-aminobutyric acid (GABA)A receptor complex in cultured mammalian cortical neurons. Chronic flurazepam (1-5 microM, for 1-10 days) treatment did not produce any changes in the morphological appearance or the cell protein content of cortica...

journal_title：Molecular pharmacology

authors： Hu XJ,Ticku MK

更新日期：1994-04-01 00:00:00

abstract：:In the rat isolated optic nerve, nitric oxide (NO) activates soluble guanylyl cyclase (sGC), resulting in a selective accumulation of cGMP in the axons. The axons are also selectively vulnerable to NO toxicity. The experiments initially aimed to determine any causative link between these two effects. It was shown, usi...

journal_title：Molecular pharmacology

authors： Garthwaite G,Goodwin DA,Neale S,Riddall D,Garthwaite J

更新日期：2002-01-01 00:00:00

abstract：:Several novel phenylaminotetralins (PATs) cause functional changes in brain that are associated with binding to saturable, high affinity sites that are not identical to any known central nervous system receptor. These PATs were tested for their ability to cause receptor-mediated functional effects on tyrosine hydroxyl...

journal_title：Molecular pharmacology

authors： Booth RG,Wyrick SD,Baldessarini RJ,Kula NS,Myers AM,Mailman RB

更新日期：1993-12-01 00:00:00

abstract：:ATP-gated purinergic receptors (P2XRs) are a family of cation-permeable channels that conduct Ca(2+) and facilitate voltage-sensitive Ca(2+) entry in excitable cells. To study Ca(2+) signaling by P2XRs and its dependence on voltage-sensitive Ca(2+) influx, we expressed eight cloned P2XR subtypes individually in gonado...

journal_title：Molecular pharmacology

authors： Koshimizu TA,Van Goor F,Tomić M,Wong AO,Tanoue A,Tsujimoto G,Stojilkovic SS

更新日期：2000-11-01 00:00:00

abstract：:Reversible binding of warfarin to defatted serum albumin was studied by equilibrium dialysis at pH 7.4, in a 66 mM sodium phosphate buffer at 37 degrees. The binding isotherm could be described by two stoichiometric binding constants, K1 in the range 141,000 to 192,000 M-1 and K2 at 39,000 to 57,000 M-1. At least two ...

journal_title：Molecular pharmacology

authors： Larsen FG,Larsen CG,Jakobsen P,Brodersen R

更新日期：1985-02-01 00:00:00

abstract：:Arrestins mediate G protein-coupled receptor desensitization, internalization, and signaling. Dopamine D(2) and D(3) receptors have similar structures but distinct characteristics of interaction with arrestins. The goals of this study were to compare arrestin-binding determinants in D(2) and D(3) receptors other than ...

journal_title：Molecular pharmacology

authors： Lan H,Liu Y,Bell MI,Gurevich VV,Neve KA

更新日期：2009-01-01 00:00:00

abstract：:We recently reported the cloning of a novel alpha 1-adrenergic receptor (AR), the alpha 1CAR. By transient and stable expression of the alpha 1CAR and the previously cloned alpha 1BAR in COS-7 and HeLa cells, respectively, we have now compared their ability to interact with major signal-transduction pathways (includin...

journal_title：Molecular pharmacology

authors： Schwinn DA,Page SO,Middleton JP,Lorenz W,Liggett SB,Yamamoto K,Lapetina EG,Caron MG,Lefkowitz RJ,Cotecchia S

更新日期：1991-11-01 00:00:00

abstract：:Accumulated evidence suggests that dopamine and dopamine D1 agonists can activate phospholipase C in both brain and peripheral tissue. The receptor that mediates the hydrolysis of phosphoinositides has not been identified. The cloned dopamine D1A receptor that is generally thought to be linked to adenylyl cyclase, has...

journal_title：Molecular pharmacology

authors： Friedman E,Jin LQ,Cai GP,Hollon TR,Drago J,Sibley DR,Wang HY

更新日期：1997-01-01 00:00:00