Pharmacological profile of a novel series of NK 1 antagonists. In vitro and in vivo potency of benzimidazolone derivatives

G Rémond, B Portevin, J Bonnet, E Canet…

Index: Remond; Portevin; Bonnet; Canet; Regoli; De Nanteuil European Journal of Medicinal Chemistry, 1997 , vol. 32, # 11 p. 843 - 868

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Citation Number: 15

Abstract

By low throughput examination of our chemical library, compound 7 was selected as a lead NK1 antagonist with a Ki of 7.1 nM. Modifications of its structure led to the finding that the in vitro potency could be markedly enhanced by disubstituting the anilino phenyl ring as in compounds 13 or 22. Human binding data correlated rather well with results obtained with in vitro animal smooth muscle preparations. Several agents proved to possess ...