Ethanol inhibits the function of 5-hydroxytryptamine type 1c and muscarinic M1 G protein-linked receptors in Xenopus oocytes expressing brain mRNA: role of protein kinase C.

abstract：:Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (CNS) disorders, such as schizophrenia and Alzheimer's disease. Furthermore, mGlu5 has been shown to play an important role in hippocampal synaptic plasticity, specifically in long-term depression (LTD) and long-term pote...

journal_title：Molecular pharmacology

authors： Noetzel MJ,Gregory KJ,Vinson PN,Manka JT,Stauffer SR,Lindsley CW,Niswender CM,Xiang Z,Conn PJ

更新日期：2013-04-01 00:00:00

abstract：:The heart is richly endowed with K(ATP) channels, which function as biological sensors, regulating membrane potentials and electrical excitability in response to metabolic alterations. We recently reported that the cytochrome P450 metabolites of arachidonic acid, epoxyeicosatrienoic acids (EETs), potently activate car...

journal_title：Molecular pharmacology

authors： Lu T,VanRollins M,Lee HC

更新日期：2002-11-01 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：:Regulator of G protein signaling (RGS) proteins accelerate the endogenous GTPase activity of Galpha(i/o) proteins to increase the rate of deactivation of active Galpha-GTP and Gbetagamma signaling molecules. Previous studies have suggested that RGS proteins are more effective on less efficiently coupled systems such a...

journal_title：Molecular pharmacology

authors： Clark MJ,Linderman JJ,Traynor JR

更新日期：2008-05-01 00:00:00

abstract：:The aryl hydrocarbon receptor (AHR) binds planar aromatic compounds and up-regulates the transcription of a battery of xenobiotic-metabolizing enzymes. To identify proteins involved in the biosynthesis of endogenous AHR ligands, we screened extracts of various mouse tissues for AHR signaling activity. We found heart e...

journal_title：Molecular pharmacology

authors： Bittinger MA,Nguyen LP,Bradfield CA

更新日期：2003-09-01 00:00:00

abstract：:The effects of 5-hydroxytryptamine (5-HT)2A receptor activation on cAMP formation were studied in a cell line derived from embryonic rat cortex (A1A1). 5-HT (EC50 = 0.87 microM) amplified the amount of cAMP formed in response to 5'-N-ethylcarboxamidoadenosine (an adenosine A2 receptor agonist), cholera toxin, and fors...

journal_title：Molecular pharmacology

authors： Berg KA,Clarke WP,Chen Y,Ebersole BJ,McKay RD,Maayani S

更新日期：1994-05-01 00:00:00

abstract：:Targeted inhibition of oncogenes in tumor cells is a rational approach toward the development of cancer therapies based on RNA interference (RNAi). Tumors caused by human papillomavirus (HPV) infection are an ideal model system for RNAi-based cancer therapies because the oncogenes that cause cervical cancer, E6 and E7...

journal_title：Molecular pharmacology

authors： Putral LN,Bywater MJ,Gu W,Saunders NA,Gabrielli BG,Leggatt GR,McMillan NA

更新日期：2005-11-01 00:00:00

abstract：:ATM and NBS1, mutation of which lead to the human autosomal recessive diseases ataxia telangiectasia and Nijmegen breakage syndrome (NBS), respectively, are essential elements in the cellular response to DNA damage induced by ionizing radiation (IR). ATM is a member of the phosphatidylinositol 3-kinase family and is a...

journal_title：Molecular pharmacology

authors： Cariveau MJ,Tang X,Cui XL,Xu B

更新日期：2007-08-01 00:00:00

abstract：:Thiourea, phenylthiourea, and methimazole perfused into rat liver stimulated the biliary efflux of GSSG without affecting the excretion of GSH into either the bile or the caval perfusate. The thiocarbamide moiety appears essential, since perfusion with urea, phenylurea, or N-methylimidazole did not stimulate GSSG rele...

journal_title：Molecular pharmacology

authors： Krieter PA,Ziegler DM,Hill KE,Burk RF

更新日期：1984-07-01 00:00:00

abstract：:The binding of [3H]Hspiroperidol to D2 dopaminergic receptors in rat striatum was compared to the binding of [3H]dopamine to its binding sites. Both radioligands labeled apparently homogeneous populations of high affinity, stereoselective, saturable sites, determined from analysis of saturation isotherms. [3H]Spiroper...

journal_title：Molecular pharmacology

authors： Hancock AA,Marsh CL

更新日期：1984-11-01 00:00:00

abstract：:Smooth muscle preparations of human aorta or pig coronary arteries contain nearly equal amounts of cGMP-dependent protein kinase isozymes (cGMP kinase I alpha and I beta). In order to understand the roles of these isozymes in relaxing vascular smooth muscle, several new cGMP analogs were synthesized and tested for pot...

journal_title：Molecular pharmacology

authors： Sekhar KR,Hatchett RJ,Shabb JB,Wolfe L,Francis SH,Wells JN,Jastorff B,Butt E,Chakinala MM,Corbin JD

更新日期：1992-07-01 00:00:00

abstract：:We have investigated various nitric oxide (NO) synthase inhibitors for their affinity and selectivity toward the three human isoenzymes in radioligand binding experiments. Therefore, we developed the new radioligand [(3)H]2-amino-4-picoline to measure binding of these compounds to the three human NO synthase (NOS) iso...

journal_title：Molecular pharmacology

authors： Boer R,Ulrich WR,Klein T,Mirau B,Haas S,Baur I

更新日期：2000-11-01 00:00:00

abstract：:The binding of agonists and antagonists to alpha 2-adrenergic receptors of human platelets was studied. The receptors showed homogeneous affinities for antagonists but two affinity states for the agonist (-)-epinephrine, which were modulated by guanine nucleotides. Van't Hoff plots of antagonist binding had a break po...

journal_title：Molecular pharmacology

authors： Lohse MJ,Klotz KN,Schwabe U

更新日期：1986-03-01 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 clinical abuse of methamphetamine (METH) is a major concern because it can cause long-lasting neurodegenerative effects in humans. Current concepts of the molecular mechanisms underlying these complications have centered on the formation of reactive oxygen species. Herein, we provide cDNA microarray evidence that ...

journal_title：Molecular pharmacology

authors： Jayanthi S,McCoy MT,Ladenheim B,Cadet JL

更新日期：2002-05-01 00:00:00

abstract：:Capsaicin (vanilloid) sensitivity has long served as the functional signature of a subset of nociceptive sensory neurons. Mutagenesis studies have revealed seemingly distinct regions involved in mediating ligand binding and channel activation at the capsaicin binding site. Residue 547 (transmembrane region 4) mediates...

journal_title：Molecular pharmacology

authors： Johnson DM,Garrett EM,Rutter R,Bonnert TP,Gao YD,Middleton RE,Sutton KG

更新日期：2006-09-01 00:00:00

abstract：:The initial event upon binding of insulin-like growth factor 1 to the insulin-like growth factor type-I receptor (IGF-1R) is auto-phosphorylation of tyrosine residues within the activation loop of the kinase domain followed by phosphorylation of other receptor tyrosine residues and the subsequent activation of the int...

journal_title：Molecular pharmacology

authors： Vasilcanu R,Vasilcanu D,Sehat B,Yin S,Girnita A,Axelson M,Girnita L

更新日期：2008-03-01 00:00:00

abstract：:The 5'-flanking region of the mouse mu opioid receptor (MOR) gene has two promoters, referred to as distal and proximal. MOR mRNA is predominantly initiated by the proximal promoter. Previously, several important cis-elements and trans-factors have been shown to play a functional role in the proximal promoter of the M...

journal_title：Molecular pharmacology

authors： Choi HS,Hwang CK,Kim CS,Song KY,Law PY,Wei LN,Loh HH

更新日期：2005-05-01 00:00:00

abstract：:The powerful analgesic effects of opioid drugs have captivated the interest of physicians and scientists for millennia, and the ability of opioid drugs to produce serious undesired effects has been recognized for a similar period of time (Kieffer and Evans, 2009). Many of these develop progressively with prolonged or ...

journal_title：Molecular pharmacology

authors： Jullié D,Gondin AB,von Zastrow M,Canals M

更新日期：2020-10-01 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：:Structural changes in the macromolecular targets of pharmacological agents can result in alterations in the efficacy of these agents. In previous studies, we identified a variant structural form of thymidylate synthase (TS) that is associated with relative resistance to 5-fluoro-2'-deoxyuridine, in a human colonic tum...

journal_title：Molecular pharmacology

authors： Barbour KW,Hoganson DK,Berger SH,Berger FG

更新日期：1992-08-01 00:00:00

abstract：:The response of myeloid leukemia cells to treatment with 1-beta-D-arabinofuranosylcytosine (ara-C) includes activation of the c-Abl protein tyrosine kinase and the stress-activated protein kinase (SAPK). The present studies demonstrate that treatment of human U-937 leukemia cells with ara-C is associated with transloc...

journal_title：Molecular pharmacology

authors： Raina D,Mishra N,Kumar S,Kharbanda S,Saxena S,Kufe D

更新日期：2002-06-01 00:00:00

abstract：:The aliphatic adenine analogues, D-eritadenine, L-eritadenine, L-threoeritadenine, and 9-(S)-(2,3-dihydroxypropyl)adenine [(S)DHPA] function as inhibitors/inactivators of purified S-adenosylhomocysteine (AdoHcy) hydrolase, but these compounds did not induce reduction of enzyme-bound NAD+. D-Eritadenine, L-eritadenine,...

journal_title：Molecular pharmacology

authors： Schanche JS,Schanche T,Ueland PM,Holý A,Votruba I

更新日期：1984-11-01 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：: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：:(6R)-5,6,7,8-Tetrahydrobiopterin (BH4), which is synthesized intracellularly from GTP, caused a concentration-dependent increase in rat pheochromocytoma (PC12) cell proliferation when added exogenously. Incubation with sepiapterin, which is converted enzymatically to BH4 within cells, also increased PC12 cell prolifer...

journal_title：Molecular pharmacology

authors： Anastasiadis PZ,States JC,Imerman BA,Louie MC,Kuhn DM,Levine RA

更新日期：1996-01-01 00:00:00

abstract：:The X-ray structure of the bacterial sodium channel NavAb provides a new template for the study of sodium and calcium channels. Unlike potassium channels, NavAb contains P2 helices in the outer-pore region. Because the sequence similarity between eukaryotic and prokaryotic sodium channels in this region is poor, the s...

journal_title：Molecular pharmacology

authors： Tikhonov DB,Zhorov BS

更新日期：2012-07-01 00:00:00

abstract：:2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) was found to activate protein kinases under cell- and nucleus-free conditions in isolated C57 mouse liver cytosol (100,000 x g supernatant). This action of TCDD was found to be aryl hydrocarbon receptor (AHR) dependent, concentration dependent, and inhibited by genistein, a t...

journal_title：Molecular pharmacology

authors： Blankenship A,Matsumura F

更新日期：1997-10-01 00:00:00

abstract：:Modulation of neuronal ion channels by the cloned rat brain CB1 cannabinoid receptor was investigated with the use of a heterologous neuronal expression system. Transient expression of the rat brain CB1 cannabinoid receptor was accomplished through microinjection of in vitro transcribed cRNA into the cytoplasm of enzy...

journal_title：Molecular pharmacology

authors： Pan X,Ikeda SR,Lewis DL

更新日期：1996-04-01 00:00:00

abstract：:The pharmacological preservation of bone in the ovariectomized rat by estrogen, selective estrogen receptor modulators (SERMs), and bisphosphonates has been well described. However, comprehensive molecular analysis of the effects of these pharmacologically diverse antiresorptive agents on gene expression in bone has n...

journal_title：Molecular pharmacology

authors： Helvering LM,Liu R,Kulkarni NH,Wei T,Chen P,Huang S,Lawrence F,Halladay DL,Miles RR,Ambrose EM,Sato M,Ma YL,Frolik CA,Dow ER,Bryant HU,Onyia JE

更新日期：2005-11-01 00:00:00