Synthesis and evaluation of imidazo [1, 5-a][1, 4] benzodiazepine esters with high affinities and selectivities at" diazepam-insensitive" benzodiazepine receptors

…, G Wong, C Dominguez, BR de Costa…

Index: Gu, Zi-Qiang; Wong, Garry; Dominguez, Celia; Costa, Brian R. de; Rice, Kenner C.; Skolnick, Phil Journal of Medicinal Chemistry, 1993 , vol. 36, # 8 p. 1001 - 1006

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Citation Number: 71

Abstract

A series of imidazo [1, 5-a][1, 4] benzodiazepine esters have been synthesized with varying ester side chains and 8-position substituents. The affinities of these compounds were evaluated at both" diazepam-insensitive"(DI) and diazepam-sensitive (DS) subtypes of the benzodiazepine receptor (BZR). A profound steric effect of the 3-position ester side chain moiety was observed on ligand affinity at DI. In contrast, ester size had a less robust effect ...