Results 141 to 150 of about 18,066 (161)
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Analysis of the histamine H2-receptor in human monocytes
Biochemical Pharmacology, 2014Histamine receptors are G-protein-coupled receptors (GPCRs). Canonically, the histamine H2-receptor (H2R) couples to Gs-proteins and activates adenylyl cyclases (ACs) with subsequent adenosine-3',5'-cyclic monophosphate (cAMP) generation. Recently, the classic two-state model describing GPCR activation has been extended to a multiple-state model ...
Roland Seifert+2 more
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Histamine H2-Receptors and Gastric Secretion
1978In 1966 Ash and Schild1 pointed out for the first time the existence of different types of histamine receptors. They defined as H1 receptors those which could be blocked by the classical antihistaminics and non-H1 receptors those which could not be blocked.
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Histamine H2 receptors in rat renal glomeruli
Biochemical Pharmacology, 1982The aim of this study was to demonstrate histamine-H2 receptors in glomeruli isolated from rat renal cortex and to correlate binding to stimulation by histamine of glomerular cyclic AMP concentration. Binding studies were performed at 10-12 degrees C using [3H]cimetidine as a tracer.
Jean-Paul Oudinet+3 more
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Nephrotoxicity and Hepatotoxicity of Histamine H2 Receptor Antagonists
Drug Safety, 2001The extensive use of selective histamine H2 receptor antagonists provides a unique opportunity to describe very rare adverse drug reactions. Although mild elevation of serum creatinine level following the administration of cimetidine is relatively common, acute interstitial nephritis (AIN) is a rare hypersensitivity reaction.
Alexander A. Fisher, David G. Le Couteur
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Conformational analyses on histamine H2-receptor antagonists
Journal of Computer-Aided Molecular Design, 1990In a series of compounds with H2-antihistaminic activity, a conformational analysis was performed based on force field calculations. The drugs studied were cimetidine, ranitidine, famotidine, roxatidine and the conformationally more restricted ICI127032.
Hans-Dieter Höltje+1 more
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Histamin-H2-Receptor-Antagonismus
1978Receptoren sind als hypothetische Orte an der Zelloberflache aufzufassen, deren Verbindung mit einem Agonisten (physiologischer Wirkstoff oder Pharmakon) von einer spezifischen Leistung der Zelle gefolgt ist. Antagonisten besitzen ebenfalls eine Affinitat zum Receptor, konnen aber die spezifische Wirkung in der Zelle nicht hervorrufen. Sie konkurrieren
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Characterization of an accessory binding area in the histamine H2 receptor
European Journal of Pharmacology: Molecular Pharmacology, 1991The histamine H2 receptor-blocking activity of ranitidine and lamtidine analogues has been investigated to gain information on the structure of the receptor area adjacent to the site fitted by the polar group. The introduction of differently shaped alkyl moieties on the polar group is always accompanied by maintenance or by an increase of H2 receptor ...
ORSETTI, Marco Riccardo Lilio, SORBA G.
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Multiple Signaling Pathways of Histamine H2 Receptors
1991Histamine H2 receptor (H2R) has been shown to be coupled to adenylate cyclase. However, we have previously demonstrated that H2R-specific stimulation also activated phospholipase C in human HL-60 promyelocytic leukemia cells (Mitsuhashi M. et al. J. Biol. Chem. 264:18356, 1989).
D G Payan, M Mitsuhashi
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Journal of Molecular Structure: THEOCHEM, 1985
Abstract The conformational energy maps and charge distributions of histamine and six H2-receptor agonists of histamine were determined in the CNDO/2 approach. When several tautomeric forms were possible only the NτH was considered. A judicious analysis of the conformational results, as a function of the H2-receptor activity, allows us to propose ...
F.J. Romero-Sánchez+2 more
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Abstract The conformational energy maps and charge distributions of histamine and six H2-receptor agonists of histamine were determined in the CNDO/2 approach. When several tautomeric forms were possible only the NτH was considered. A judicious analysis of the conformational results, as a function of the H2-receptor activity, allows us to propose ...
F.J. Romero-Sánchez+2 more
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H2 histaminic receptors in rat cerebral cortex. 3. Inhibition of [3H]histamine by H2 agonists
Biochemistry, 1985The binding of [3H]histamine to H2 receptors in homogenates of rat cerebral cortex is inhibited by 11 H2 agonists in a characteristic and unique manner. At low concentrations of the radioligand (less than 1.5 nM), the inhibitory profiles of individual agonists (A) are distinctly biphasic; specific binding is well described in most cases by the ...
Marianne Kandel+3 more
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