Dipole moment in relation to hydrogen receptor histamine antagonist activity for cimetidine analogs

…, JC Emmett, CR Ganellin, MJ Graham…

Index: Young; Durant; Emmett; Ganellin; Graham; Mitchell; Prain; Roantree Journal of Medicinal Chemistry, 1986 , vol. 29, # 1 p. 44 - 49

Full Text: HTML

Citation Number: 40

Abstract

The activities of a series of H2 receptor histamine antagonists structurally related to cimetidine (1) have been compared to investigate the effect of replacing the cyanoguanidine moiety by other neutral, dipolar groups. Antagonist activity, as measured in vitro on the histamine-stimulated guinea pig right atrium, was found to be very sensitive to relatively minor structural changes. Differences in H2 antagonist activity are accounted for by dipole ...