Progress in the proxifan class: heterocyclic congeners as novel potent and selective histamine H 3-receptor antagonists

…, JM Arrang, JC Schwartz, H Stark, W Schunack

Index: Grassmann, Sven; Sadek, Bassem; Ligneau, Xavier; Elz, Sigurd; Ganellin, C. Robin; Arrang, Jean-Michel; Schwartz, Jean-Charles; Stark, Holger; Schunack, Walter European Journal of Pharmaceutical Sciences, 2002 , vol. 15, # 4 p. 367 - 378

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Citation Number: 41

Abstract

Histamine H3 receptors are critically involved in the pathophysiology of several disorders of the central nervous system (CNS). Among other families of H3-receptor ligands, the proxifan class has recently been described to contain numerous potent histamine H3-receptor antagonists, eg ciproxifan or imoproxifan. In the present study, we report on the design of novel heterocyclic proxifan analogues and their antagonist potencies at histamine H3 ...