Results 191 to 200 of about 42,892 (256)

Conformational analyses on histamine H2-receptor antagonists

Journal of Computer-Aided Molecular Design, 1990
In 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.
H D, Höltje, A, Batzenschlager
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Novel qualitative structure-activity relationships for the antinociceptive actions of H2 antagonists, H3 antagonists and derivatives.

Journal of Pharmacology and Experimental Therapeutics, 1997
Recent studies have shown that cimetidine, burimamide and improgan (also known as SKF92374, a cimetidine congener lacking H2 antagonist activity) induce antinociception after intracerebroventricular administration in rodents.
Lindsay B. Hough, J. Nalwalk, B. Y. Li, R. Leurs, W. Menge, H. Timmerman, M. Carlile, C. Cioffi, M. Wentland   +8 more
semanticscholar   +1 more source

Potential histamine H2-receptor antagonists. 4. Benzylhistamines

Journal of Medicinal Chemistry, 1982
As part of our studies aimed at designing histamine H2-receptor antagonists, the effect on histaminergic activity of introducing benzyl substituents at various positions in the histamine molecule is described. New synthetic methods are reported for the novel 4-benzyl-, beta-benzyl- and 4,N tau-dibenylhistamines and the reported 2-benzylhistamine.
J C, Emmett, G J, Durant, C R, Ganellin, A M, Roe, J L, Turner   +4 more
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Metiamide—An orally active histamine H2-receptor antagonist

Agents and Actions, 1973
Metiamide has been found to be about 10 times more active than burimamide in vitro in antagonizing histamine H2-receptors and nearly 5 times more active in vivo as an antagonist of histamine or pentagastrin-stimulated secretion. Effective oral ED50 doses for inhibition have been estimated as 25 μmole kg−1 against basal secretion in rats and 16 μmole kg−
J W, Black, W A, Duncan, J C, Emmett, C R, Ganellin, T, Hesselbo, M E, Parsons, J H, Wyllie   +6 more
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Histamine H2-receptor antagonists.

Advances in internal medicine, 1978
Development of histamine H2-receptor antagonists has enhanced the understanding of histamine physiology and pharmacology. The effect of H2-receptor antagonists on gastrointestinal physiology has been studied extensively. These compounds inhibit gastric acid secretion in response to all known secretagogues and, in contrast to anticholinergic drugs ...
M, Feldman, C T, Richardson
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Carrier-mediated active transport of histamine H2 receptor antagonists, cimetidine and nizatidine, into isolated rat hepatocytes: contribution of type I system.

Journal of Pharmacology and Experimental Therapeutics, 1994
The uptake rates of [3H]cimetidine and [14C]nizatidine into isolated rat hepatocytes were studied in order to identify the transport mechanism of histamine H2 receptor antagonists into the liver.
H. Nakamura, H. Sano, M. Yamazaki, Yuichi Sugiyama   +3 more
semanticscholar   +1 more source

Haematological Adverse Effects of Histamine H2-Receptor Antagonists

Medical Toxicology, 1988
Histamine H2-receptor antagonists are widely used in the treatment of gastrointestinal diseases related to gastric acid hypersecretion. Cimetidine was introduced into medical practice in 1976 and ranitidine, famotidine and nizatidine in 1981, 1985 and 1987, respectively. Haematological adverse effects are relatively uncommon and most have been reported
J P, Aymard, B, Aymard, P, Netter, B, Bannwarth, P, Trechot, F, Streiff   +5 more
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Studies on histamine H2 receptors coupled to cardiac adenylate cyclase. Blockade by H2 and H1 receptor antagonists.

Molecular Pharmacology, 1979
In particulate preparations from guinea pig ventricle, histamine caused a three to five-fold stimulation of basal adenylate cyclase activity. The H2 antagonist, cimetidine, displaced the dose-response curve of histamine to the right in a parallel fashion
Carl L. Johnson, Harel Weinstein, J. Green   +2 more
semanticscholar   +1 more source

A radioimmunoassay for the histamine H2-antagonist, tiotidine

Agents and Actions, 1984
A specific and sensitive radioimmunoassay (RIA) for the histamine H2-antagonist, tiotidine, has been developed. The assay is based upon competition of tiotidine with [3H]-tiotidine for antibody (Ab) obtained from immunized rabbits. The immunogen used was a glutaraldehyde coupled conjugate of the tiotidine derivative (ICI 147,655) and bovine serum ...
P, Dobson, T O, Yellin
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Nephrotoxicity and Hepatotoxicity of Histamine H2 Receptor Antagonists

Drug Safety, 2001
The 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.
A A, Fisher, D G, Le Couteur
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