Immortalized hypothalamic GT1-7 neurons express functional gamma-aminobutyric acid type A receptors.

abstract：:We examined the subtype-selective binding site of the beta-adrenergic receptors (betaARs). The beta(1)/beta(2)-chimeric receptors showed the importance of the second and seventh transmembrane domains (TM2 and TM7) of the beta(2)AR for the binding of the beta(2)-selective agonists such as formoterol and procaterol. Ala...

journal_title：Molecular pharmacology

authors： Isogaya M,Sugimoto Y,Tanimura R,Tanaka R,Kikkawa H,Nagao T,Kurose H

更新日期：1999-11-01 00:00:00

abstract：:Ligands that selectively inhibit human α3β2 and α6β2 nicotinic acetylcholine receptor (nAChRs) and not the closely related α3β4 and α6β4 subtypes are lacking. Current α-conotoxins (α-Ctxs) that discriminate among these nAChR subtypes in rat fail to discriminate among the human receptor homologs. In this study, we desc...

journal_title：Molecular pharmacology

authors： Hone AJ,McIntosh JM,Azam L,Lindstrom J,Lucero L,Whiteaker P,Passas J,Blázquez J,Albillos A

更新日期：2015-11-01 00:00:00

abstract：:UDP-glucuronosyltransferase (UGT) 1A1 glucuronidates endogenous metabolites, such as bilirubin, and exogenous substances, and plays a critical role in their detoxification and excretion. In a previous article, we described the phenobarbital response activity to a 290-base pair (bp) distal enhancer sequence (-3499/-321...

journal_title：Molecular pharmacology

authors： Sugatani J,Nishitani S,Yamakawa K,Yoshinari K,Sueyoshi T,Negishi M,Miwa M

更新日期：2005-03-01 00:00:00

abstract：:Olanzapine was shown to be oxidized to a reactive intermediate by HOCl, which is the major oxidant produced by activated neutrophils. A mass spectrum obtained using a flow system in which the reactants were fed into a mixing chamber and the products flowed directly into a mass spectrometer revealed a reactive intermed...

journal_title：Molecular pharmacology

authors： Gardner I,Zahid N,MacCrimmon D,Uetrecht JP

更新日期：1998-06-01 00:00:00

abstract：:In ND8-47 cells, a neuroblastoma x dorsal root ganglion hybrid cell line, activation of delta-opioid receptors induced an increase in the intracellular free calcium concentration ([Ca2+]i) through dihydropyridine-sensitive calcium channels. This effect was mediated by pertussis toxin-sensitive G proteins. The G protei...

journal_title：Molecular pharmacology

authors： Tang T,Kiang JG,Côté TE,Cox BM

更新日期：1995-08-01 00:00:00

abstract：:Folate receptor-targeted cancer therapies constitute a promising treatment for the approximately one third of human cancers that overexpress the folate receptor (FR). However, the potencies of all folate-receptor targeted therapies depend on 1) the rate of folate-linked drug conjugate binding to the cancer cell surfac...

journal_title：Molecular pharmacology

authors： Paulos CM,Reddy JA,Leamon CP,Turk MJ,Low PS

更新日期：2004-12-01 00:00:00

abstract：:We have identified four new mu-opiod receptor (MOR)-1 exons, indicating that the gene now contains at least nine exons spanning more than 200 kilobases. Replacement of exon 4 by combinations of the new exons yields three new receptors. When expressed in Chinese hamster ovary cells, all three variants displayed high af...

journal_title：Molecular pharmacology

authors： Pan YX,Xu J,Bolan E,Abbadie C,Chang A,Zuckerman A,Rossi G,Pasternak GW

更新日期：1999-08-01 00:00:00

abstract：:We determined the effect of flufenamic acid (FFA) and related derivatives on gap junction channel currents, applying the dual whole-cell patch-clamp technique to pairs of N2A neuroblastoma cells transfected with various connexins. FFA reduced gap junction channel currents in a reversible and concentration-dependent ma...

journal_title：Molecular pharmacology

authors： Srinivas M,Spray DC

更新日期：2003-06-01 00:00:00

abstract：:Homopentameric complexes of either the A or As subunit of the 5-hydroxytryptamine3 receptor form Ca(2+)-permeable channels that can be activated by the selective agonist 1-(m-chlorophenyl)-biguanide (mCPBG). In both N1E-115 neuroblastoma cells and human embryonic kidney 293 cells stably expressing the 5-HT3 receptor A...

journal_title：Molecular pharmacology

authors： Hargreaves AC,Gunthorpe MJ,Taylor CW,Lummis SC

更新日期：1996-11-01 00:00:00

abstract：:[3H]Dihydroalprenolol ([3H]DHA) has been used extensively in receptor binding studies to measure beta-adrenergic receptors in the central nervous system. Usually, nonspecific binding has been defined by high concentrations of the beta-adrenergic receptor agonist isoproterenol or antagonists such as alprenolol or propr...

journal_title：Molecular pharmacology

authors： Riva MA,Creese I

更新日期：1989-07-01 00:00:00

abstract：:The retinoid (visual) cycle consists of a series of biochemical reactions needed to regenerate the visual chromophore 11-cis-retinal and sustain vision. Genetic or environmental factors affecting chromophore production can lead to blindness. Using animal models that mimic human retinal diseases, we previously demonstr...

journal_title：Molecular pharmacology

authors： Gao S,Kahremany S,Zhang J,Jastrzebska B,Querubin J,Petersen-Jones SM,Palczewski K

更新日期：2018-05-01 00:00:00

abstract：:Previous studies suggest that selective antagonists of specific subtypes of muscarinic acetylcholine receptors (mAChRs) may provide a novel approach for the treatment of certain central nervous system (CNS) disorders, including epileptic disorders, Parkinson's disease, and dystonia. Unfortunately, previously reported ...

journal_title：Molecular pharmacology

authors： Sheffler DJ,Williams R,Bridges TM,Xiang Z,Kane AS,Byun NE,Jadhav S,Mock MM,Zheng F,Lewis LM,Jones CK,Niswender CM,Weaver CD,Lindsley CW,Conn PJ

更新日期：2009-08-01 00:00:00

abstract：:Ryanodine receptors (RyRs) are intracellular membrane channels playing key roles in many Ca(2+) signaling pathways and, as such, are emerging novel therapeutic and insecticidal targets. RyRs are so named because they bind the plant alkaloid ryanodine with high affinity and although it is established that ryanodine pro...

journal_title：Molecular pharmacology

authors： Mukherjee S,Thomas NL,Williams AJ

更新日期：2014-09-01 00:00:00

abstract：:Bufuralol 1'-hydroxylation is a prototypical reaction catalyzed by cytochrome P450 (P450) 2D6, an enzyme known to show debrisoquine/sparteine-type genetic polymorphism in humans. In the present study we further examined the roles of several human P450 enzymes, as well as P450 2D6, in the hydroxylation of (+/-)-bufural...

journal_title：Molecular pharmacology

authors： Yamazaki H,Guo Z,Persmark M,Mimura M,Inoue K,Guengerich FP,Shimada T

更新日期：1994-09-01 00:00:00

abstract：:A cDNA encoding the human liver phenol-sulfating form of phenol sulfotransferase (P-PST) has been isolated and characterized from a lambda Uni-Zap XR human liver cDNA library. P-PST is the major form of phenol sulfotransferase involved in drug and xenobiotic metabolism in human liver. P-PST is also responsible for the...

journal_title：Molecular pharmacology

authors： Wilborn TW,Comer KA,Dooley TP,Reardon IM,Heinrikson RL,Falany CN

更新日期：1993-01-01 00:00:00

abstract：:We investigated the interactions of the anticancer drug vinorelbine with drug efflux transporters and cytochrome P450 3A drug-metabolizing enzymes. Vinorelbine was transported by human multidrug-resistance associated protein (MRP) 2, and Mrp2 knockout mice displayed increased vinorelbine plasma exposure after oral adm...

journal_title：Molecular pharmacology

authors： Lagas JS,Damen CW,van Waterschoot RA,Iusuf D,Beijnen JH,Schinkel AH

更新日期：2012-10-01 00:00:00

abstract：:The bile salt export pump (BSEP/ABCB11) transports bile salts from hepatocytes into bile canaliculi. Its malfunction is associated with severe liver disease. One reason for functional impairment of BSEP is systemic administration of drugs, which as a side effect inhibit the transporter. Therefore, drug candidates are ...

journal_title：Molecular pharmacology

authors： Sohail MI,Schmid D,Wlcek K,Spork M,Szakács G,Trauner M,Stockner T,Chiba P

更新日期：2017-10-01 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：:Airway smooth muscle (ASM) cells can act as effector cells in the initiation and/or perpetuation of airway inflammation in asthma by producing various inflammatory chemokines or cytokines. Previous studies from our laboratory and others showed that the combination of tumor necrosis factor-alpha (TNFalpha) and interfer...

journal_title：Molecular pharmacology

authors： Keslacy S,Tliba O,Baidouri H,Amrani Y

更新日期：2007-02-01 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：:Activation of N-methyl-D-aspartate (NMDA) receptors is required for induction of some lasting changes in nervous system structure and function. The cellular mechanisms involved in transducing receptor stimulation into long-lasting changes in cellular activity are unknown. Immediate-early genes (IEGs) have been implica...

journal_title：Molecular pharmacology

authors： Lerea LS,Carlson NG,McNamara JO

更新日期：1995-06-01 00:00:00

abstract：:We have previously identified allosteric modulators of the cannabinoid CB(1) receptor (Org 27569, PSNCBAM-1) that display a contradictory pharmacological profile: increasing the specific binding of the CB(1) receptor agonist [(3)H]CP55940 but producing a decrease in CB(1) receptor agonist efficacy. Here we investigate...

journal_title：Molecular pharmacology

authors： Baillie GL,Horswill JG,Anavi-Goffer S,Reggio PH,Bolognini D,Abood ME,McAllister S,Strange PG,Stephens GJ,Pertwee RG,Ross RA

更新日期：2013-02-01 00:00:00

abstract：:At the vertebrate neuromuscular junction (nmj), ATP is known to be coreleased with acetylcholine from the synaptic vesicles. We have previously shown that the P2Y1 receptor is localized at the nmj. Here, we extend the findings to show that another nucleotide receptor, P2Y2, is also localized there and with P2Y1 jointl...

journal_title：Molecular pharmacology

authors： Tung EK,Choi RC,Siow NL,Jiang JX,Ling KK,Simon J,Barnard EA,Tsim KW

更新日期：2004-10-01 00:00:00

abstract：:Chimeric receptors of the beta2-adrenergic receptor in which the extracellular loops were replaced with the corresponding amino acids of the alpha1a-adrenergic receptor were generated to measure changes in alpha1-antagonist affinity. Although no changes in alpha1-antagonist affinity were measured in the beta2/alpha1a ...

journal_title：Molecular pharmacology

authors： Zhao MM,Gaivin RJ,Perez DM

更新日期：1998-03-01 00:00:00

abstract：:CYP3A4 is one of the major drug-metabolizing enzymes in human and is responsible for the metabolism of 60% of clinically used drugs. Many drugs are able to induce the expression of CYP3A4, which usually causes drug-drug interactions and adverse drug reactions. This study aims to explore the role of histone modificatio...

journal_title：Molecular pharmacology

authors： Yan L,Wang Y,Liu J,Nie Y,Zhong XB,Kan Q,Zhang L

更新日期：2017-08-01 00:00:00

abstract：:Typical equilibrium binding experiments cannot be quantitatively analyzed on the basis of classical mathematical equations when the receptor concentration is so high that a significant fraction of the added radioligand concentration is in the bound form. In this paper, the appropriate equations are derived and used in...

journal_title：Molecular pharmacology

authors： Swillens S

更新日期：1995-06-01 00:00:00

abstract：:In cervical cancer, the p53 and retinoblastoma (pRb) tumor suppressor pathways are disrupted by the human papilloma virus (HPV) E6 and E7 oncoproteins, because E6 targets p53 and E7 targets pRb for rapid proteasome-mediated degradation. We have investigated whether E6 suppression with small interfering RNA (siRNA) res...

journal_title：Molecular pharmacology

authors： Tan S,Hougardy BM,Meersma GJ,Schaap B,de Vries EG,van der Zee AG,de Jong S

更新日期：2012-05-01 00:00:00

abstract：:We demonstrated previously that the nucleoside of fludarabine (F-ara-A), a clinically effective agent against chronic lymphocytic leukemia and low-grade lymphoma, produces synergistic cytotoxicity against cisplatin-resistant CP2.0 human colon tumor cells when administered in combination with cisplatin. The purpose of ...

journal_title：Molecular pharmacology

authors： Li L,Keating MJ,Plunkett W,Yang LY

更新日期：1997-11-01 00:00:00

abstract：:The spatiotemporal dynamics of opioid signaling in the brain remain poorly defined. Photoactivatable opioid ligands provide a means to quantitatively measure these dynamics and their underlying mechanisms in brain tissue. Although activation kinetics can be assessed using caged agonists, deactivation kinetics are obsc...

journal_title：Molecular pharmacology

authors： Banghart MR,Williams JT,Shah RC,Lavis LD,Sabatini BL

更新日期：2013-11-01 00:00:00

abstract：:Poly(A)+ RNA from mammalian retina expresses bicuculline/baclofen-insensitive gamma-aminobutyric acid (GABA) receptors in Xenopus oocytes with properties similar to those of homooligomeric GABA rho 1 receptors. The pharmacological profile of these rho-like receptors was extended by measuring sensitivities to various G...

journal_title：Molecular pharmacology

authors： Woodward RM,Polenzani L,Miledi R

更新日期：1993-04-01 00:00:00