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Structural Requirements for Histamine H2 Agonists and H2 Antagonists
1991This chapter reviews the structural requirements for H2 agonists and antagonists. Section B discusses the agonists, which are divided into three classes: the non-selective histamine analogues, showing H2 activity as well as H1 and H3 activity; dimaprit, a selective, but moderately active agonist which allows no substitution without a dramatic fall in ...
H. van der Goot, A. Bast, H. Timmerman
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Recent developments in histamine H2-antagonists
Trends in Pharmacological Sciences, 1981R.T. Brittain, D. Jack, B.J. Price
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Histamine H2-receptor antagonists
Baillière's Clinical Gastroenterology, 1988The first histamine H2-receptor antagonists were developed in the early 1970s, and they have a dominant role in today's management of peptic ulceration. The original regimens using either cimetidine or ranitidine attempted to control acidity across the 24 hours, but more 'modern' regimens use a large single dose of the H2-blocker in the evening, which ...
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Histamine H2-Receptor Antagonists
Nursing Clinics of North America, 1991In summary, histamine initiates acid secretion by stimulating the H2 subtype histamine receptor on parietal cells. Cimetidine, rantidine, famotidine, and nizantidine are histamine H2-receptor antagonists that block this action of histamine, reducing gastric acid output and concentration under both basal and stimulated conditions.
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Prolactin responses to histamine H2 receptor antagonists
Acta Endocrinologica, 1980Abstract. We have compared the effects of cimetidine and SK&F 92994, a new more potent histamine H2 receptor antagonist, on serum prolactin, and also assessed the effect of the H2 receptor agonist impromidine on the response to cimetidine. As previously reported, cimetidine 200 mg given as an iv bolus dose produced a marked rise in serum prolactin,
P C, Sharpe +4 more
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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.
H D, Höltje, A, Batzenschlager
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Potential histamine H2-receptor antagonists. 4. Benzylhistamines
Journal of Medicinal Chemistry, 1982As 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 +4 more
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Metiamide—An orally active histamine H2-receptor antagonist
Agents and Actions, 1973Metiamide 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 +6 more
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Histamine H2-receptor antagonists.
Advances in internal medicine, 1978Development 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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