Epinephrine activates both Gs and Gi pathways, but norepinephrine activates only the Gs pathway through human beta2-adrenoceptors overexpressed in mouse heart.

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：:Organic anion transporter-1 (OAT1) mediates the body disposition of a diverse array of clinically important drugs, including anti-HIV therapeutics, antitumor drugs, antibiotics, antihypertensives, and anti-inflammatories. Therefore, understanding the regulation of OAT1 has profound clinical significance. We previously...

journal_title：Molecular pharmacology

authors： Li S,Zhang Q,You G

更新日期：2013-07-01 00:00:00

abstract：:Previous studies have shown that at least two subtypes of somatostatin (SRIF) receptors (SRIF1 and SRIF2) are expressed in mammalian cells. SRIF1 receptors have high affinity for MK 678, whereas SRIF2 receptors have no affinity for MK 678 but selectively bind peptides with structures similar to that of CGP 23996. Rece...

journal_title：Molecular pharmacology

authors： Rens-Domiano S,Law SF,Yamada Y,Seino S,Bell GI,Reisine T

更新日期：1992-07-01 00:00:00

abstract：:A functional interaction between peroxisome proliferator-activated receptor alpha (PPARalpha) and components of the circadian clock has been suggested, but whether these transcriptional factors interact to regulate the expression of their target genes remains obscure. Here we used a PPARalpha ligand, bezafibrate, to s...

journal_title：Molecular pharmacology

authors： Oishi K,Koyanagi S,Matsunaga N,Kadota K,Ikeda E,Hayashida S,Kuramoto Y,Shimeno H,Soeda S,Ohdo S

更新日期：2010-07-01 00:00:00

abstract：:The effects of the non-tumor-promoting protein kinase C (PKC) activator bryostatin 1 and the PKC inhibitors staurosporine and UCN-01 were examined with respect to modulation of 1-[beta-D-arabinofuranosyl]cytosine (ara-C)-induced apoptosis in human myeloid leukemia cells (HL-60) overexpressing the antiapoptotic protein...

journal_title：Molecular pharmacology

authors： Wang S,Vrana JA,Bartimole TM,Freemerman AJ,Jarvis WD,Kramer LB,Krystal G,Dent P,Grant S

更新日期：1997-12-01 00:00:00

abstract：:We reported earlier that delta 9-tetrahydrocannabinol (THC), the main psychoactive ingredient in marihuana, increased markedly the level of unesterified arachidonic acid (AA) in guinea pig cerebral cortex slices prelabeled with [14C]AA. The purpose of the present study was to clarify the mechanism underlying THC-enhan...

journal_title：Molecular pharmacology

authors： Reichman M,Nen W,Hokin LE

更新日期：1991-10-01 00:00:00

abstract：:Vesnarinone, a cardiotonic agent, blocks I(Kr) and, unlike other I(Kr) blockers, produces a frequency-dependent prolongation of action potential duration (APD). To elucidate the mechanisms, we studied the effects of vesnarinone on HERG, the cloned human I(Kr) channel, heterologously expressed in Xenopus laevis oocytes...

journal_title：Molecular pharmacology

authors： Kamiya K,Mitcheson JS,Yasui K,Kodama I,Sanguinetti MC

更新日期：2001-08-01 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：:Adenine-uridine rich elements (AREs) play an important role in modulating mRNA stability, being the target site of many ARE-binding proteins (AUBPs) that are involved in the decay process. Three 26-mer 2'-O-methyl oligoribonucleotides (ORNs) homologous to the core region of ARE of bcl2 mRNA have been studied for decoy...

journal_title：Molecular pharmacology

authors： Bevilacqua A,Ghisolfi L,Franzi S,Maresca G,Gherzi R,Capaccioli S,Nicolin A,Canti G

更新日期：2007-02-01 00:00:00

abstract：:The cannabinoid field is currently an active research area. Anandamide (AEA) and 2-arachidonoylglycerol (2-AG) are the most characterized endogenous cannabinoids (also known as endocannabinoids). These neuromodulators have been implicated in various physiologically relevant phenomena, including mood (Witkin et al., 20...

journal_title：Molecular pharmacology

authors： Yates ML,Barker EL

更新日期：2009-07-01 00:00:00

abstract：:The insecticide imidacloprid and structurally related neonicotinoids act selectively on insect nicotinic acetylcholine receptors (nAChRs). To investigate the mechanism of neonicotinoid selectivity, we have examined the effects of mutations to basic amino acid residues in loop D of the nAChR acetylcholine (ACh) binding...

journal_title：Molecular pharmacology

authors： Shimomura M,Yokota M,Ihara M,Akamatsu M,Sattelle DB,Matsuda K

更新日期：2006-10-01 00:00:00

abstract：:The organic anions picrate (2,4,6-trinitrophenol) and niflumate (2-[[3-(trifluoromethyl)phenyl]-amino]-3-pyridinecarboxylate) were examined for their effects on radioligand binding to the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex. Neither organic anion produced the enhancement of [35S] t-butylbicy...

journal_title：Molecular pharmacology

authors： Evoniuk G,Skolnick P

更新日期：1988-12-01 00:00:00

abstract：:Multidrug resistance-associated protein 1 (Mrp1; Abcc1) is expressed in sarcolemma of murine heart, where it probably protects the cardiomyocyte by mediating efflux of endo- and xenobiotics. We used doxorubicin (DOX), a chemotherapeutic drug known to induce oxidative stress and thereby cardiac injury, as a model cardi...

journal_title：Molecular pharmacology

authors： Jungsuwadee P,Nithipongvanitch R,Chen Y,Oberley TD,Butterfield DA,St Clair DK,Vore M

更新日期：2009-05-01 00:00:00

abstract：:The therapeutic potential of antitumor drugs is seriously limited by the manifestation of cellular drug resistance. We used the budding yeast Saccharomyces cerevisiae as a model system to identify novel mechanisms of resistance to one of the most active anticancer agents, cisplatin. We pinpointed NPR2 (nitrogen permea...

journal_title：Molecular pharmacology

authors： Schenk PW,Brok M,Boersma AW,Brandsma JA,Den Dulk H,Burger H,Stoter G,Brouwer J,Nooter K

更新日期：2003-08-01 00:00:00

abstract：:GPR139 is an orphan G-protein-coupled receptor expressed in the central nervous system. To identify its physiologic ligand, we measured GPR139 receptor activity from recombinant cells after treatment with amino acids, orphan ligands, serum, and tissue extracts. GPR139 activity was measured using guanosine 5'-O-(3-[(35...

journal_title：Molecular pharmacology

authors： Liu C,Bonaventure P,Lee G,Nepomuceno D,Kuei C,Wu J,Li Q,Joseph V,Sutton SW,Eckert W,Yao X,Yieh L,Dvorak C,Carruthers N,Coate H,Yun S,Dugovic C,Harrington A,Lovenberg TW

更新日期：2015-11-01 00:00:00

abstract：:The activities of phosphorylase kinase and myosin light-chain kinase are regulated by Ca2+ binding to calmodulin. However, differences in the activation properties of the purified enzymes are apparent, since calmodulin binds to phosphorylase kinase in the absence of Ca2+ whereas prior formation of a Ca2+ . calmodulin ...

journal_title：Molecular pharmacology

authors： Silver PJ,Stull JT

更新日期：1983-05-01 00:00:00

abstract：:Benzamide riboside (BR) and tiazofurin (TR) are converted to analogs of NAD that inhibit IMP dehydrogenase (IMPDH), resulting in cellular depletion of GTP and dGTP and inhibition of proliferation. The current work was undertaken to identify the human nucleoside transporters involved in cellular uptake of BR and TR and...

journal_title：Molecular pharmacology

authors： Damaraju VL,Visser F,Zhang J,Mowles D,Ng AM,Young JD,Jayaram HN,Cass CE

更新日期：2005-01-01 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：:Tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione (TIBO) derivatives (e.g., R82150) are potent, human immunodeficiency virus-1 (HIV-1)-specific, inhibitors of reverse transcriptase (RT) that are undergoing initial evaluation in clinical trials. Because HIV-1 has become resistant to other RT inhibitor...

journal_title：Molecular pharmacology

authors： Mellors JW,Im GJ,Tramontano E,Winkler SR,Medina DJ,Dutschman GE,Bazmi HZ,Piras G,Gonzalez CJ,Cheng YC

更新日期：1993-01-01 00:00:00

abstract：:Novel methods of detecting and quantitating cooperative interactions between an agent and both a tritiated (muscarinic) antagonist and the endogenous agonist (acetylcholine), acting at a common (muscarinic) receptor, have been devised. In a semiquantitative protocol, binding data are transformed into affinity ratios (...

journal_title：Molecular pharmacology

authors： Lazareno S,Birdsall NJ

更新日期：1995-08-01 00:00:00

abstract：:The interaction of hormones acting via the mobilization of calcium and stimulation of cAMP levels in cells was examined by determining the effects of carbachol and forskolin on cAMP and cGMP accumulation in mouse parotid gland. Treatment of isolated acini with either carbachol (0.01 to 20 microM) or forskolin (1 micro...

journal_title：Molecular pharmacology

authors： Watson EL,Singh JC,McPhee C,Beavo J,Jacobson KL

更新日期：1990-10-01 00:00:00

abstract：:The aryl hydrocarbon receptor (AHR) and its DNA binding partner, the AHR nuclear translocator (ARNT), are basic helix-loop-helix transcription factors that mediate many of the toxic and carcinogenic effects of polyhalogenated aromatic hydrocarbons. The basic regions of the AHR and ARNT contact the GCGTG recognition si...

journal_title：Molecular pharmacology

authors： Swanson HI,Yang JH

更新日期：1998-10-01 00:00:00

abstract：:Post-transcriptional protein synthesis by GH3 cloned pituitary cells, which secrete prolactin and growth hormone, is dependent on Ca2+. The effects of antagonists of prolactin secretion were examined on overall protein synthesis in GH3 cells as a function of cellular Ca2+ depletion and restoration at varying concentra...

journal_title：Molecular pharmacology

authors： Wolfe SE,Brostrom CO,Brostrom MA

更新日期：1986-04-01 00:00:00

abstract：:We reported previously that protein associated with Myc (PAM) interacts with the C2 domain of type V adenylyl cyclase (ACV-C2) and that purified PAM is a potent inhibitor of Galphas-stimulated ACV activity (J Biol Chem 276:47583-47589, 2001). The present study was conducted to identify the region in PAM that inhibits ...

journal_title：Molecular pharmacology

authors： Gao X,Patel TB

更新日期：2005-01-01 00:00:00

abstract：:N-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) induces Parkinson-like symptoms in humans, nonhuman primates, and mice. Several studies suggest that MPTP is metabolized by monoamine oxidase (MAO) type B to yield N-methyl-4-phenyl-pyridinium (MPP+), which is responsible for the neurotoxic effects of the drug. In th...

journal_title：Molecular pharmacology

authors： Itzhak Y,Mash D,Zhang SH,Stein I

更新日期：1991-03-01 00:00:00

abstract：:Voltage-gated sodium (Na(V)1) channels play a critical role in modulating the excitability of sensory neurons, and human genetic evidence points to Na(V)1.7 as an essential contributor to pain signaling. Human loss-of-function mutations in SCN9A, the gene encoding Na(V)1.7, cause channelopathy-associated indifference ...

journal_title：Molecular pharmacology

authors： Schmalhofer WA,Calhoun J,Burrows R,Bailey T,Kohler MG,Weinglass AB,Kaczorowski GJ,Garcia ML,Koltzenburg M,Priest BT

更新日期：2008-11-01 00:00:00

abstract：:Previous studies have shown that neural stimulation of brown adipose tissue (BAT) reorganizes the expression and activity of signaling proteins in the beta-adrenergic adenylyl cyclase pathway. Cold stress increases neural stimulation of BAT and increases alpha1-adrenergic receptor number; however, the alpha1 receptor ...

journal_title：Molecular pharmacology

authors： Granneman JG,Zhai Y,Lahners KN

更新日期：1997-04-01 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：:At sites of inflammation, endothelial cells play a major role in defining the types of leukocytes that are recruited to a specific area. This is accomplished, at least in part, through the cytokine induction of cell surface adhesion molecules, including vascular cell adhesion molecule 1 (VCAM-1). We investigated the r...

journal_title：Molecular pharmacology

authors： Cobb RR,Felts KA,Parry GC,Mackman N

更新日期：1996-06-01 00:00:00

abstract：:Cytosolic sulfotransferase 1C3 (SULT1C3) is the least characterized of the three human SULT1C subfamily members. Originally identified as an orphan SULT by computational analysis of the human genome, we recently reported that SULT1C3 is expressed in human intestine and LS180 colorectal adenocarcinoma cells and is upre...

journal_title：Molecular pharmacology

authors： Dubaisi S,Fang H,Kocarek TA,Runge-Morris M

更新日期：2016-11-01 00:00:00