Altered striatal function and muscarinic cholinergic receptors in acetylcholinesterase knockout mice.

abstract：:The highly conserved aspartate residue in the second transmembrane domain of G protein-coupled receptors is present in position 113 in the type 1 neurotensin receptor (NTR1) but is replaced by an Ala residue in position 79 in the type 2 neurotensin receptor (NTR2). NTR1 couples to Galphaq to stimulate phospholipase C ...

journal_title：Molecular pharmacology

authors： Martin S,Botto JM,Vincent JP,Mazella J

更新日期：1999-02-01 00:00:00

abstract：:Neuromedin U (NmU) is a 25 amino acid peptide prominently expressed in the upper gastrointestinal (GI) tract and central nervous system. It is highly conserved throughout evolution and induces smooth muscle contraction in a variety of species. Our understanding of NmU biology has been limited because the identity of i...

journal_title：Molecular pharmacology

authors： Hedrick JA,Morse K,Shan L,Qiao X,Pang L,Wang S,Laz T,Gustafson EL,Bayne M,Monsma FJ Jr

更新日期：2000-10-01 00:00:00

abstract：:The present study characterizes the methanethiosulfonate (MTS) inhibition profiles of 26 consecutive cysteine-substituted mutants comprising transmembrane (TM) helix 6 of the human apical Na(+)-dependent bile acid transporter (SLC10A2). TM6 is linked exofacially to TM7 via extracellular loop 3. TM7 was identified prev...

journal_title：Molecular pharmacology

authors： Hussainzada N,Khandewal A,Swaan PW

更新日期：2008-02-01 00:00:00

abstract：:The aim of this study was to create and characterize constitutively active mutant (CAM) histamine H(1) receptors (H(1)R) using random mutagenesis methods to further investigate the activation process of the rhodopsin-like family of G protein-coupled receptors (GPCRs). This approach identified position 6.40 in TM 6 as ...

journal_title：Molecular pharmacology

authors： Bakker RA,Jongejan A,Sansuk K,Hacksell U,Timmerman H,Brann MR,Weiner DM,Pardo L,Leurs R

更新日期：2008-01-01 00:00:00

abstract：:Ca2-dependent protein phosphorylations activated by calmodulin or phospholipid were studied using selective inhibitors. Both protein phosphorylations were inhibited by N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7) and its derivatives. Kinetic analysis indicated that the primary effect of these agents was me...

journal_title：Molecular pharmacology

authors： Tanaka T,Ohmura T,Yamakado T,Hidaka H

更新日期：1982-09-01 00:00:00

abstract：:The pharmacological effects of angiotensin II (AII) are potently inhibited by several peptide and recently synthesized nonpeptide AII receptor antagonists. The interaction of sarcosine1, isoleucine8-AII (sarile), sarcosine1,O-methyltyrosine4-AII (sarmesin), and the nonpeptide AII antagonists 2-n-butyl-4-chloro-5- hydr...

journal_title：Molecular pharmacology

authors： Wienen W,Mauz AB,Van Meel JC,Entzeroth M

更新日期：1992-06-01 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：:We demonstrate that gastrin-releasing peptide (GRP) can inhibit the proliferation of human immortal nontumorigenic (184-B5) mammary epithelial cells ectopically expressing the human GRP receptor. Growth of Balb 3T3 cells ectopically expressing relatively high levels of the GRP receptor was also inhibited by GRP; howev...

journal_title：Molecular pharmacology

authors： Feldman RI,Fried S,Mann E,Wu JM,Liang M

更新日期：1996-03-01 00:00:00

abstract：:Tissue plasminogen activator (tPA), a serine protease, catalyzes the conversion of plasminogen to plasmin. In the present study, we investigated the role of the tPA-plasmin system in depolarization-evoked dopamine (DA) and acetylcholine (ACh) release in the nucleus accumbens (NAc) and hippocampus, respectively, of mic...

journal_title：Molecular pharmacology

authors： Ito M,Nagai T,Kamei H,Nakamichi N,Nabeshima T,Takuma K,Yamada K

更新日期：2006-11-01 00:00:00

abstract：:In an attempt to better understand the role of the cyclohexene ring (ring A) in the biochemical and pharmacological properties of anthracyclines related to doxorubicin and daunorubicin, we investigated the effects of introduction of a fluorine atom at position 8 of idarubicin (4-demethoxydaunorubicin) on drug molecula...

journal_title：Molecular pharmacology

authors： Animati F,Arcamone F,Bigioni M,Capranico G,Caserini C,De Cesare M,Lombardi P,Pratesi G,Salvatore C,Supino R,Zunino F

更新日期：1996-09-01 00:00:00

abstract：:Supplemental oxygen therapy is frequently used in the treatment of pulmonary insufficiency, as is encountered in premature infants, and in patients with acute respiratory distress syndrome. However, hyperoxia causes lung damage in experimental animals and may do so in humans. Cytochrome P4501A enzymes have been implic...

journal_title：Molecular pharmacology

authors： Couroucli XI,Welty SE,Geske RS,Moorthy B

更新日期：2002-03-01 00:00:00

abstract：:Previous studies have shown that the transcription factor signal transducer and activator of transcription-3 (STAT3) in podocytes plays an important role in progression of HIV nephropathy and in collapsing forms of glomerulonephritis. Here, we have observed that application of 100 nM angiotensin II (Ang II) to culture...

journal_title：Molecular pharmacology

authors： Abkhezr M,Dryer SE

更新日期：2014-08-01 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：:Avermectins are a family of potent broad-spectrum anthelmintic compounds, which bind with high affinity to membranes isolated from the free-living nematode Caenorhabditis elegans. Binding of avermectins is thought to modulate chloride channel activity, but the exact mechanism for anthelmintic activity remains to be de...

journal_title：Molecular pharmacology

authors： Arena JP,Liu KK,Paress PS,Cully DF

更新日期：1991-09-01 00:00:00

abstract：:Tetradecyl 2,3-dihydroxybenzoate (ABG-001) is a lead compound derived from neuritogenic gentisides. In the present study, we investigated the mechanism by which ABG-001 induces neurite outgrowth in a rat adrenal pheochromocytoma cell line (PC12). Inhibitors of insulin-like growth factor 1 (IGF-1) receptor, phosphatidy...

journal_title：Molecular pharmacology

authors： Tang R,Gao L,Kawatani M,Chen J,Cao X,Osada H,Xiang L,Qi J

更新日期：2015-08-01 00:00:00

abstract：:The CB1 cannabinoid receptor has been implicated in the regulation of bone remodeling and bone mass. A high bone mass (HBM) phenotype was reported in CB1-null mice generated on a CD1 background (CD1(CB1-/-) mice). By contrast, our preliminary studies in cb1-/- mice, backcrossed to C57BL/6J mice (C57(CB1-/-) mice), rev...

journal_title：Molecular pharmacology

authors： Tam J,Ofek O,Fride E,Ledent C,Gabet Y,Müller R,Zimmer A,Mackie K,Mechoulam R,Shohami E,Bab I

更新日期：2006-09-01 00:00:00

abstract：:Acute cannabidiol treatment of mice inactivated hepatic microsomal cytochrome P-450IIIA (P-450IIIA) and markedly inhibited in vitro cannabinoid metabolism. Antibodies raised against purified P-450IIIA inhibited the microsomal formation of quantitatively minor cannabinoid metabolites but had no effect on the major meta...

journal_title：Molecular pharmacology

authors： Bornheim LM,Correia MA

更新日期：1991-08-01 00:00:00

abstract：:Recently, several classes of compounds have been shown to be potent, selective, and specific inhibitors of human immunodeficiency virus type 1 replication in vitro. These include the tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione (TIBO) and the 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (H...

journal_title：Molecular pharmacology

authors： Debyser Z,Pauwels R,Baba M,Desmyter J,De Clercq E

更新日期：1992-05-01 00:00:00

abstract：:Atropine, the classic muscarinic receptor antagonist, inhibits ion currents mediated by neuronal nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes. At the holding potential of -80 mV, 1 microM atropine inhibits 1 mM acetylcholine-induced inward currents mediated by rat alpha2beta2, alpha2beta4, alp...

journal_title：Molecular pharmacology

authors： Zwart R,Vijverberg HP

更新日期：1997-11-01 00:00:00

abstract：:The L-type amino acid transporter 1 (LAT1) is an Na(+)-independent neutral amino acid transporter subserving the amino acid transport system L. Because of its broad substrate selectivity, system L has been proposed to be responsible for the permeation of amino acid-related drugs through the plasma membrane. To underst...

journal_title：Molecular pharmacology

authors： Uchino H,Kanai Y,Kim DK,Wempe MF,Chairoungdua A,Morimoto E,Anders MW,Endou H

更新日期：2002-04-01 00:00:00

abstract：:delta-Opioid receptor (DOR) promoter exhibited a cell-type-specific expression pattern. Protein-DNA interactions in this promoter were identified by dimethyl sulfate in vivo footprinting analysis of NG108-15 cells, expressing endogenous DOR. Complete protection of the putative Sp1 cis-element and partial protection of...

journal_title：Molecular pharmacology

authors： Smirnov D,Im HJ,Loh HH

更新日期：2001-08-01 00:00:00

abstract：:Styrylquinoline derivatives (SQ) efficiently inhibit the 3'-processing activity of integrase (IN) with IC50 values of between 0.5 and 5 microM. We studied the mechanism of action of these compounds in vitro. First, we used steady-state fluorescence anisotropy to assay the effects of the SQ derivatives on the formation...

journal_title：Molecular pharmacology

authors： Deprez E,Barbe S,Kolaski M,Leh H,Zouhiri F,Auclair C,Brochon JC,Le Bret M,Mouscadet JF

更新日期：2004-01-01 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：:The involvement of mitogen-activated protein (MAP) kinases in the mitogenic effect of thyrotropin (TSH) is not fully elucidated. In FRTL-5 cells, we found that the MAP kinase kinase (MEK) inhibitors UO126 and PD98059 substantially decreased TSH-induced DNA synthesis, indicating that MAP kinases are involved in the TSH...

journal_title：Molecular pharmacology

authors： Iacovelli L,Capobianco L,Salvatore L,Sallese M,D'Ancona GM,De Blasi A

更新日期：2001-11-01 00:00:00

abstract：:The beta 3-adrenergic receptor (beta 3AR) is a member of the super-family of G protein-coupled receptors that are characterized by seven putative transmembrane helices connected by hydrophilic loops. The mechanism by which the activated beta ARs transmit the signals across the plasma membrane involves the stimulation ...

journal_title：Molecular pharmacology

authors： Guan XM,Amend A,Strader CD

更新日期：1995-09-01 00:00:00

abstract：:2-Hydroxy-4(-2,2,3,3,3-pentafluoropropoxy)-benzoic acid (UR-1505), a new molecule chemically related to salicylic acid, has immunomodulator properties and is currently under clinical development for treatment of atopic dermatitis. The present work describes the immunomodulatory profile of UR-1505. UR-1505 targets T ce...

journal_title：Molecular pharmacology

authors： Román J,de Arriba AF,Barrón S,Michelena P,Giral M,Merlos M,Bailón E,Comalada M,Gálvez J,Zarzuelo A,Ramis I

更新日期：2007-08-01 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：:Studies were carried out to elucidate the mechanism whereby thyroid hormone (T3) induces NADPH:cytochrome P450 oxidoreductase (P450R) mRNA in rat liver in vivo. Northern blot analysis revealed that T3 treatment increases unspliced liver nuclear P450R RNA 4-fold within 8 h and that this induction precedes the induction...

journal_title：Molecular pharmacology

authors： Li HC,Liu D,Waxman DJ

更新日期：2001-05-01 00:00:00

abstract：:In this study, we investigated the effects of single alanine substitutions of amino acid residues in the supposed ATP binding site of the human P2X3 receptor on the agonistic effect of nucleotide analogs. The wild-type and mutant receptors were expressed in HEK293 cells, and the nucleotide effects were measured by mea...

journal_title：Molecular pharmacology

authors： Riedel T,Wiese S,Leichsenring A,Illes P

更新日期：2012-07-01 00:00:00

abstract：:Glutathione-liganded binuclear dinitrosyl iron complex (glut-BDNIC) has been proposed to be a donor of nitric oxide (NO). This study was undertaken to investigate the mechanisms of vasoactivity, systemic hemodynamic effects, and pharmacokinetics of glut-BDNIC. To test the hypothesis that glut-BDNICs vasodilate by rele...

journal_title：Molecular pharmacology

authors： Liu T,Zhang M,Terry MH,Schroeder H,Wilson SM,Power GG,Li Q,Tipple TE,Borchardt D,Blood AB

更新日期：2018-05-01 00:00:00