Synthesis of new cardioselective M2 muscarinic receptor antagonists.

GR Mandelli, S Maiorana, P Terni, G Lamperti…

Index: Mandelli, Giacomina R.; Maiorana, Stefano; Terni, Patrizia; Lamperti, Giuseppina; Colibretti, Maria Luisa; Imbimbo, Bruno P. Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 11 p. 1611 - 1622

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Citation Number: 8

Abstract

A series of 5H-dibenz [b, f] azepine derivatives was prepared and evaluated for binding affinities to muscarinic receptors in vitro. Among them, compound 8 showed a high affinity for human recombinant M 2 receptors (K i= 2.6 nM), a low affinity for M 4 receptors (39-fold less than for M 2 receptors) and a very low affinity for M 1 and M 3 receptors (119-and 112-fold less than for M 2 receptors, respectively). The high M 2 selectivity of 8 may be attributed to ...