Comparison of discriminative stimuli produced by full and partial benzodiazepine agonists: pharmacological...

Benzodiazepines produce discriminative stimuli that are stereospecific and antagonized by specific benzodiazepine receptor antagonists. The potency of these stimuli correlate with the ability of these compounds to bind to the benzodiazepine receptor complex. These data indicate that benzodiazepine stimuli are transduced via the benzodiazepine receptor. The underlying basis of these stimuli is unclear. Results with novel compounds that produce preclinical anxiolytic effects without the sedation and muscle relaxation of the classical benzodiazepines suggest that muscle relaxation may contribute to these stimuli. A direct comparison of discriminative stimuli established on a classical benzodiazepine agonist with the stimuli established on a partial benzodiazepine agonist supports the possibility that the classical benzodiazepine cue is mediated by a muscle relaxant effect, while the partial agonist cue is related to the anxioselectivity of the compound.