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CGS 9896, a chloro‐derivative of the diazepam antagonist CGS 8216, exhibits anxiolytic activity in the pentylenetetrazol‐saline discrimination test
Author(s) -
Spencer David G.,
Lal Harbans
Publication year - 1983
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430030409
Subject(s) - pentylenetetrazol , diazepam , anxiolytic , anxiogenic , antagonist , pharmacology , saline , anxiety , anesthesia , psychology , medicine , neuroscience , anticonvulsant , psychiatry , epilepsy , receptor
Abstract The effects of CGS 8216, a diazepam antagonist, and CGS 9896, a chloro‐derivative of CGS 8216, were assessed in an animal model of anxiety: discrimination of interoceptive discriminable stimuli (IDS) induced by pentylenetetrazol (PTZ). Rats were trained to discriminate the effects of an anxiogenic drug, PTZ, from those of saline by pressing one of two levers in an operant chamber. When given saline followed by PTZ (20 mg/kg), all subjects reliably selected the PTZ‐appropriate lever. When either diazepam or CGS 9896 (5, 20, or 80 mg/kg) injection preceded PTZ treatment, fewer subjects selected the PTZ‐appropriate lever. When given before either diazepam or CGS 9896, however, CGS 8216 (40 mg/kg) reversed their blockade of PTZ‐appropriate lever selection. These findings support the characterization of CGS 8216 as an effective diazepam antagonist, in vivo, with respect to an anxiolytic effect. CGS 9896 was effective in blocking the PTZ‐induced IDS, establishing anxiolytic action in this animal model of anxiety.