Biochemical evidence for a new benzodiazepine receptor antagonist

✍ Scribed by Dr. B. Kenneth Koe; Elena Kondratas; Lorraine A. Lebel; Katherine W. Minor

• Publisher: John Wiley and Sons
• Year: 1985
• Tongue: English
• Weight: 342 KB
• Volume: 6
• Category: Article
• ISSN: 0272-4391
• DOI: 10.1002/ddr.430060410

✦ Synopsis

1-(3-Chlorophenyl)-3-diethylcarbamoyl-l H-l,2,4-triazole (CP-32,961) inhibited [3H]diazepam binding to rat cortical membranes and [3H]flunitrazepam binding to mouse brain in vivo. Its inhibition of the binding of [3H]Ro 15-1788 (benzodiazepine receptor antagonist) to these membranes was not facilitated by added GABA; CP-32,961 exhibited a GABA ratio of 0.84 compared to 2.44 for diazepam. Cerebellar cyclic GMP content in rats was raised by CP-32,961, which also further elevated the increased cyclic GMP levels induced by isoniazid. These neurochemical actions are similar to those shown by ethyl P-carboline-3carboxylate (@-CCE) and suggest that CP-32,961 is a benzodiazepine receptor antagonist with inverse agonist activity.