Benzodiazepine receptor binding activity of 8-substituted-9-(3-substituted-benzyl)-6-(dimethylamino)-9H-purines

…, MP Krochmal, RM Ferris, JL Howard

Index: Kelley, James L.; McLean, Ed W.; Linn, James A.; Krochmal, Mark P.; Ferris, Robert M.; Howard, James L. Journal of Medicinal Chemistry, 1990 , vol. 33, # 1 p. 196 - 202

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Citation Number: 23

Abstract

A series of 8-substituted analogues of 9-(3-aminobenzyl)-6-(dimethylamino)-9H-purine (8) were synthesized and tested for their ability to bind to the benzodiazepine receptor (BZR) in rat brain tissue. The most active compound was the 8-bromo-9-(3-formamidobenzyl) analogue 16 (ICw= 0.011 wM), which was 1000-fold more active than the parent 9-benzyl-6- (dimethylamino)-9H-purine (1) and nearly as active as diazepam. Although substitution of ...