123811-36-9Relevant articles and documents
Benzodiazepine Receptor Binding Activity of 8-Substituted-9-(3-substituted-benzyl)-6-(dimethylamino)9H-purines
Kelley, James L.,McLean, Ed W.,Linn, James A.,Krochmal, Mark P.,Ferris, Robert M.,Howard, James L.
, p. 196 - 202 (2007/10/02)
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 (IC50 = 0.011 μM), 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 a m-formamido group and an 8-bromo substituent on 1 imparted potent BZR binding activity, neither 16 nor 17 analogues exhibited significant anxiolytic activity on a modified Geller-Seifter conflict schedule.