Literature DB >> 2891046

Kinetic analysis of the interaction of mifentidine with gastric H2-receptors in the conscious dog.

F Pagani1, M Zecca, A Giachetti.   

Abstract

The H2-receptor antagonists mifentidine and cimetidine were compared for their ability to antagonize the activation of H2-receptors in the conscious dog. Dose-response curves to dimaprit in stimulating gastric secretion were displaced to the right in a dose-related fashion by both drugs. Schild and Eadie-Hofstee analysis of these data indicated that mifentidine and cimetidine inhibited in vivo activation of H2-receptors in a manner compatible with competitive surmountable antagonism. Mifentidine displayed a 24fold greater potency than cimetidine as H2 antagonist in the conscious dog.

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Year:  1987        PMID： 2891046     DOI： 10.1007/bf00172689

Source DB:  PubMed          Journal:  Naunyn Schmiedebergs Arch Pharmacol        ISSN： 0028-1298            Impact factor:   3.000


  13 in total

1.  Theoretical considerations concerning gastric inhibition.

Authors:  K J Obrink
Journal:  Scand J Gastroenterol Suppl       Date:  1976

2.  Tautomerism and the receptor action of histamine: a mechanistic model.

Authors:  H Weinstein; D Chou; C L Johnson; S Kang; J P Green
Journal:  Mol Pharmacol       Date:  1976-09       Impact factor: 4.436

3.  Pharmacological evaluation of cimetidine, a new histamine H2-receptor antagonist, in healthy man.

Authors:  W L Burland; W A Duncan; T Hesselbo; J G Mills; P C Sharpe; S J Haggie; J H Wyllie
Journal:  Br J Clin Pharmacol       Date:  1975-12       Impact factor: 4.335

4.  Evaluation of novel compounds interacting with H2-histamine receptors: effect on histamine-sensitive adenylate cyclase activity in guinea-pig gastric mucosa.

Authors:  R Micheletti; D Oliva; P Belfiore; A Giachetti; S Nicosia
Journal:  Agents Actions       Date:  1985-07

5.  Effect of the new H2-receptor antagonist mifentidine on gastric acid secretion in the cat: comparison with cimetidine and ranitidine.

Authors:  C Scarpignato; R Tramacere; M Tangwa; G Bertaccini
Journal:  Arch Int Pharmacodyn Ther       Date:  1985-07

6.  Pharmacological profile of mifentidine: a novel H2-receptor antagonist.

Authors:  A Giachetti; F Pagani; R Micheletti; A Brambilla; E Cereda; A Donetti
Journal:  Agents Actions       Date:  1985-04

7.  Pharmacokinetics of the H2- receptor antagonist ranitidine in man.

Authors:  J J McNeil; G W Mihaly; A Anderson; A W Marshall; R A Smallwood; W J Louis
Journal:  Br J Clin Pharmacol       Date:  1981-09       Impact factor: 4.335

8.  Some quantitative uses of drug antagonists.

Authors:  O ARUNLAKSHANA; H O SCHILD
Journal:  Br J Pharmacol Chemother       Date:  1959-03

9.  (Imidazolylphenyl)formamidines. A structurally novel class of potent histamine H2 receptor antagonists.

Authors:  A Donetti; E Cereda; E Bellora; A Gallazzi; C Bazzano; P Vanoni; P Del Soldato; R Micheletti; F Pagani; A Giachetti
Journal:  J Med Chem       Date:  1984-03       Impact factor: 7.446

10.  Pharmacology of mifentidine, a novel H2-receptor antagonist.

Authors:  F Pagani; R Micheletti; A Brambilla; A Schiavone; E Montagna; C Ciprandi; A Giachetti
Journal:  Arzneimittelforschung       Date:  1985
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