Pharmacology of vanilloid transient receptor potential cation channels.

abstract：:Ro 11-2465 is a cyanide derivative of imipramine. In cerebral cortex homogenates, [3H] Ro 11-2465 displays a binding profile similar to that of [3H]imipramine. Agents compete with binding of [3H]Ro 11-2465 in an order of potency similar to their ability to block serotonin uptake, and raphe lesions greatly decrease the...

journal_title：Molecular pharmacology

authors： Dumbrille-Ross A,Tang SW

更新日期：1983-05-01 00:00:00

abstract：:Ubiquitination of the human kappa opioid receptor (hKOR) expressed in Chinese hamster ovary (CHO) cells was observed in the presence of the proteasomal inhibitor N-benzoyloxycarbonyl (Z)-Leu-Leu-leucinal (MG132) and enhanced by the agonists (-)(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidiny) cyclohexyl] benzeneaceta...

journal_title：Molecular pharmacology

authors： Li JG,Haines DS,Liu-Chen LY

更新日期：2008-04-01 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：:Heart cells in culture need no external stimulation to contract; they beat rhythmically at a rate and intensity dependent on culture conditions. These cells respond to the general anesthetic 2-bromo-2-chloro-1,1,1-trifluorethane (halothane), with a loss of beating intensity and a lessening of beating rate. Increased c...

journal_title：Molecular pharmacology

authors： Malinconico SM,Hartzell CR,McCarl RL

更新日期：1983-03-01 00:00:00

abstract：:The D2 dopamine receptor (D2R) was examined for its ability to mediate nuclear factor-kappaB (NF-kappaB) activation through G proteins. Stimulation of D2R-transfected HeLa cells with its agonist quinpirole induced the expression of a NF-kappaB luciferase reporter and formation of NF-kappaB-DNA complex. This response w...

journal_title：Molecular pharmacology

authors： Yang M,Zhang H,Voyno-Yasenetskaya T,Ye RD

更新日期：2003-08-01 00:00:00

abstract：:Ethanol-inducible CYP2E1 is an enzyme of major toxicological interest because it metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. CYP2E1 has also been implicated in alcohol liver disease because of its contribution to oxidative stress. Previously, polymorphic alleles with mutations in i...

journal_title：Molecular pharmacology

authors： Hu Y,Oscarson M,Johansson I,Yue QY,Dahl ML,Tabone M,Arincò S,Albano E,Ingelman-Sundberg M

更新日期：1997-03-01 00:00:00

abstract：:Catecholamine transporters constitute the biological targets for several important drugs, including antidepressants, cocaine, and related compounds. Some information exists about discrete domains of these transporters that are involved in substrate translocation and uptake blockade, but delineation of domains mediatin...

journal_title：Molecular pharmacology

authors： Syringas M,Janin F,Mezghanni S,Giros B,Costentin J,Bonnet JJ

更新日期：2000-12-01 00:00:00

abstract：:Although the thiopurine drugs 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) are well established agents for the treatment of leukemia, controversies remain regarding their main mode of action. Previous evidence has suggested that although 6-TG exerts a cytotoxic effect through incorporation of 6-thioguanine nucleot...

journal_title：Molecular pharmacology

authors： Coulthard SA,Hogarth LA,Little M,Matheson EC,Redfern CP,Minto L,Hall AG

更新日期：2002-07-01 00:00:00

abstract：:It has been demonstrated previously that cannabinol (CBN) differentially modulates interleukin-2 (IL-2) protein secretion by T cells with a corresponding change in extracellular signal-regulated kinase activity. The objective of the present studies was to further investigate the molecular mechanism by which CBN enhanc...

journal_title：Molecular pharmacology

authors： Jan TR,Rao GK,Kaminski NE

更新日期：2002-02-01 00:00:00

abstract：:We examined the effects on allosteric modulation and ligand binding of the mutation of amino acid residues of the human A(3) adenosine receptor (A(3)AR) that are hypothesized to be near one of three loci: the putative sodium binding site, the putative ligand binding site, and the DRY motif in transmembrane helical dom...

journal_title：Molecular pharmacology

authors： Gao ZG,Kim SK,Gross AS,Chen A,Blaustein JB,Jacobson KA

更新日期：2003-05-01 00:00:00

abstract：:Extracellular protons inhibit N-methyl-D-aspartate (NMDA) receptors with an IC50 value in the physiological pH range. To identify the molecular determinants of proton sensitivity, we used scanning mutagenesis of the NR1 subunit to search for residues that control proton inhibition of NMDA receptors. Homology modeling ...

journal_title：Molecular pharmacology

authors： Low CM,Lyuboslavsky P,French A,Le P,Wyatte K,Thiel WH,Marchan EM,Igarashi K,Kashiwagi K,Gernert K,Williams K,Traynelis SF,Zheng F

更新日期：2003-06-01 00:00:00

abstract：:Adefovir dipivoxil [9-(2-(bispivaloyloxymethyl)phosphonylmethoxyethyl)adenine (bis-POM PMEA)], an oral prodrug of adefovir (PMEA), is currently in phase III clinical testing for the treatment of human immunodeficiency virus-1 (HIV-1) infection. Previous in vitro experiments have shown that HIV-1 recombinant viruses ex...

journal_title：Molecular pharmacology

authors： Miller MD,Lamy PD,Fuller MD,Mulato AS,Margot NA,Cihlar T,Cherrington JM

更新日期：1998-08-01 00:00:00

abstract：:Combining chemotherapeutics to treat malignant tumors has been shown to be effective in preventing drug resistance, tumor recurrence, and reducing tumor size. We modeled combination drug therapy in PC-3 human prostate cancer cells using mixture design response surface methodology (MDRSM), a statistical technique desig...

journal_title：Molecular pharmacology

authors： Oblad R,Doughty H,Lawson J,Christensen M,Kenealey J

更新日期：2018-08-01 00:00:00

abstract：:The regulation of the cellular distribution and intracellular signaling properties of the alpha(1B)- and alpha(1D)- adrenoceptor (alpha(1)-AR) subtypes was examined in stably transfected Rat 1 fibroblasts. In unstimulated cells, alpha(1B)-AR expression was noted primarily on the cell surface. Treatment with phenylephr...

journal_title：Molecular pharmacology

authors： McCune DF,Edelmann SE,Olges JR,Post GR,Waldrop BA,Waugh DJ,Perez DM,Piascik MT

更新日期：2000-04-01 00:00:00

abstract：:The ligand-binding sites of many G protein-coupled receptors (GPCRs) are situated around and deeply embedded within the central pocket formed by their seven transmembrane-spanning α-helical domains. Generally, these binding sites are assumed accessible to endogenous ligands from the aqueous phase. Recent advances in t...

journal_title：Molecular pharmacology

authors： Szlenk CT,Gc JB,Natesan S

更新日期：2019-11-01 00:00:00

abstract：:Poly(ADP-ribose) polymerase-1 (PARP-1) is a NAD-consuming enzyme with an emerging key role in epigenetic regulation of gene transcription. Although PARP-1 expression is characteristically restricted to the nucleus, a few studies report the mitochondrial localization of the enzyme and its ability to regulate organelle ...

journal_title：Molecular pharmacology

authors： Lapucci A,Pittelli M,Rapizzi E,Felici R,Moroni F,Chiarugi A

更新日期：2011-06-01 00:00:00

abstract：:The rat mu-opioid receptor clone in which novel exon 5 was found in the place of exon 4 (MOR-1B) was one of the first MOR-1 variants described. We now have identified the mouse homolog of the rat MOR-1B as well as four additional variants derived from splicing from exon 3 into different sites within exon 5. The sequen...

journal_title：Molecular pharmacology

authors： Pan YX,Xu J,Bolan E,Moskowitz HS,Xu M,Pasternak GW

更新日期：2005-09-01 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：:The MUC1 C-terminal transmembrane subunit (MUC1-C) oncoprotein is a direct activator of the canonical nuclear factor-kappaB (NF-kappaB) RelA/p65 pathway and is aberrantly expressed in human multiple myeloma cells. However, it is not known whether multiple myeloma cells are sensitive to the disruption of MUC1-C functio...

journal_title：Molecular pharmacology

authors： Yin L,Ahmad R,Kosugi M,Kufe T,Vasir B,Avigan D,Kharbanda S,Kufe D

更新日期：2010-08-01 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：:Very few antagonists have been identified for the human pregnane X receptor (PXR). These molecules may be of use for modulating the effects of therapeutic drugs, which are potent agonists for this receptor (e.g., some anticancer compounds and macrolide antibiotics), with subsequent effects on transcriptional regulatio...

journal_title：Molecular pharmacology

authors： Ekins S,Kholodovych V,Ai N,Sinz M,Gal J,Gera L,Welsh WJ,Bachmann K,Mani S

更新日期：2008-09-01 00:00:00

abstract：:The ubiquitously expressed nitric oxide (NO) receptor soluble guanylate cyclase (sGC) plays a key role in signal transduction. Binding of NO to the N-terminal prosthetic heme moiety of sGC results in approximately 200-fold activation of the enzyme and an increased conversion of GTP into the second messenger cGMP. sGC ...

journal_title：Molecular pharmacology

authors： Rothkegel C,Schmidt PM,Atkins DJ,Hoffmann LS,Schmidt HH,Schröder H,Stasch JP

更新日期：2007-11-01 00:00:00

abstract：:We cloned and expressed a human metabotropic glutamate receptor 1 alpha (HmGluR1 alpha) in a novel cell line. The human mGluR1 alpha cDNA was found to be 86% identical to rat mGluR1 alpha, and the predicted protein sequence was found to be 93% identical to rat mGluR1 alpha. We expressed HmGluR1 alpha in AV12-664, an a...

journal_title：Molecular pharmacology

authors： Desai MA,Burnett JP,Mayne NG,Schoepp DD

更新日期：1995-10-01 00:00:00

abstract：:alpha4beta2 nicotinic acetylcholine receptors (nAChRs) are recognized as the principal nicotine binding site in brain. Recombinant alpha4beta2 nAChR demonstrate biphasic concentration-response relationships with low- and high-EC50 components. This study shows that untranslated regions (UTR) can influence expression of...

journal_title：Molecular pharmacology

authors： Briggs CA,Gubbins EJ,Marks MJ,Putman CB,Thimmapaya R,Meyer MD,Surowy CS

更新日期：2006-07-01 00:00:00

abstract：:The P2Y(1) receptor is responsible for the initiation of platelet aggregation in response to ADP and plays a key role in thrombosis. Although this receptor is expressed early in the platelet lineage, the regulation of its expression during megakaryocyte differentiation is unknown. In the mouse megakaryocytic cell line...

journal_title：Molecular pharmacology

authors： Hechler B,Toselli P,Ravanat C,Gachet C,Ravid K

更新日期：2001-11-01 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：:Rat and human lung microsomal cytochrome P-450 (P-450) enzymes have been characterized with regard to their catalytic activities towards several xenobiotic chemicals, including procarcinogens, in different microsomal preparations. Rat lung microsomal P-450s were more active than the human P-450s in catalyzing most of ...

journal_title：Molecular pharmacology

authors： Shimada T,Yun CH,Yamazaki H,Gautier JC,Beaune PH,Guengerich FP

更新日期：1992-05-01 00:00:00

abstract：:Maurotoxin (MTX) is a potent blocker of human voltage-activated Kv1.2 and intermediate-conductance calcium-activated potassium channels, hIKCa1. Because its blocking affinity on both channels is similar, although the pore region of these channels show only few conserved amino acids, we aimed to characterize the bindin...

journal_title：Molecular pharmacology

authors： Visan V,Fajloun Z,Sabatier JM,Grissmer S

更新日期：2004-11-01 00:00:00

abstract：:We studied the mechanism by which the peptide omega-grammotoxin-SIA inhibits voltage-dependent calcium channels. Grammotoxin at concentrations of > 50 nM completely inhibited inward current carried by 2 mM barium through P-type channels in rat cerebellar Purkinje neurons when current was elicited by depolarizations up...

journal_title：Molecular pharmacology

authors： McDonough SI,Lampe RA,Keith RA,Bean BP

更新日期：1997-12-01 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