Effects of WIN 64338, a nonpeptide bradykinin B2 receptor antagonist, on guinea-pig trachea.

Date publication

août 1995

Journal

British journal of pharmacology

Auteurs

Membres identifiés du Cancéropôle Est :
Dr DAEFFLER Laurent

Tous les auteurs :
Scherrer D, Daeffler L, Trifilieff A, Gies JP

Lien Pubmed

https://www.ncbi.nlm.nih.gov/pubmed/7582533

Résumé

We investigated the effect of the nonpeptide bradykinin receptor antagonist, [[4-[[2-[[bis(cyclohexylamino)methylene] amino]-3-(2-naphthalenyl) 1-oxopropyl]amino]-phenyl]-tributyl, chloride, monohydrochloride (WIN 64338), on [3H]-bradykinin binding and on bradykinin-induced contraction of the guinea-pig trachea. This non peptide bradykinin receptor antagonist inhibited [3H]-bradykinin binding with a nanomolar range of affinity, Ki = 50.9 +/- 19 nM and inhibited bradykinin-induced contraction in a non-competitive manner with a KB value of 6.43 10(-8) +/- 2.34 10(-8) M.

Mots clés

Animals, Binding, Competitive, Bradykinin Receptor Antagonists, Guinea Pigs, In Vitro Techniques, Muscle Contraction, drug effects, Naphthalenes, metabolism, Organophosphorus Compounds, metabolism, Receptor, Bradykinin B2, Trachea, drug effects

Référence

Br. J. Pharmacol.. 1995 Aug;115(7):1127-8