Recent developments in the behavioral pharmacology of benzodiazepine (ω) receptors: Evidence for the functional significance of receptor subtypes

摘要: Recent research in molecular biology has demonstrated the complexity of GABAA receptors and shown that benzodiazepine (BZ-ω) receptor subtypes have a structural reality. It is therefore appropriate to ask whether different pharmacological effects produced by benzodiazepines (anticonvulsant activity, anxiety reduction, motor incoordination, learning deficits, characteristic discriminative stimulus effects, tolerance dependence) are associated with activity at subtypes. The present paper reviews literature dealing behavioral novel BZ (ω) ligands relevant question functional significance BZ1 (ω1) BZ2 (ω2) only drugs currently available considerable degree selectivity alpidem zolpidem. These compounds relatively high affinity for containing α1 subunit (corresponding subtype) very low α5 one type receptor). Pharmacological observed these, other, less selective allow several tentative conclusions be drawn: (a) Little known role subtype anxiolytic or amnestic but intrinsic may reduce without giving rise sedation incoordination appear disrupt memory sedative doses; (b) Selectivity sleep-inducing not suggesting particular importance mechanisms muscle relaxation; (c) identical differences related selectivity; (d) Compounds produce little no dependence. A wider range will necessary investigate these factors detail many profiles can expected from levels activity.