Pharmacological profile of mifentidine: a novel H2-receptor antagonist

Mifentidine, a representative compound of a novel class of H2-antagonists, has been investigated for its ability to interact with H2-receptors and to inhibit gastric acid secretion. Affinity estimates (KB) of mifentidine obtained from in vitro studies on cardiac and gastric mucosal histamine (H2) re...

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Bibliographic Details
Published inAgents and actions Vol. 16; no. 3-4; p. 173
Main Authors Giachetti, A, Pagani, F, Micheletti, R, Brambilla, A, Cereda, E, Donetti, A
Format Journal Article
LanguageEnglish
Published Switzerland 01.04.1985
Subjects
Animals
Dogs
Female
Gastric Acid - metabolism
Guinea Pigs
Heart - drug effects
Histamine H2 Antagonists - pharmacology
Imidazoles - pharmacology
In Vitro Techniques
Rats
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Summary:Mifentidine, a representative compound of a novel class of H2-antagonists, has been investigated for its ability to interact with H2-receptors and to inhibit gastric acid secretion. Affinity estimates (KB) of mifentidine obtained from in vitro studies on cardiac and gastric mucosal histamine (H2) receptors were in the 20-50 nM range. Mifentidine appeared to be endowed with strong anti-secretory properties against histamine-stimulated secretion in the anaesthetized rat and in the conscious dog. Distinct features of mifentidine were considerable bioavailability and duration of anti-secretory effect.
ISSN:0065-4299
DOI:10.1007/BF01983131