Attaining in vivo selectivity of positive modulation of α3βγ2 GABAA receptors in rats: A hard task!

It is unclear whether GABAA receptors (GABAARs) that contain the α3-subunit are substantially involved in the anxiolytic effects of benzodiazepines (BDZs). In the present study, we tested YT-III-31, a newer BDZ ligand with functional preference for α3βγ2 GABAARs, in two paradigms of unconditioned anxiety, the open field and elevated plus maze in rats. The eff ective dose of YT-III-31 (2 mg/kg) displayed a clear anxiolytic-like profile, unhampered by sedative action, in both tests. At a higher dose (10 mg/kg), YT-III-31 induced ataxia in the rotarod and sedation in spontaneous locomotor activity test.

Source: European Neuropsychopharmacology - June 8, 2018 Category: Psychiatry & Psychology Authors: Bojan Batini ć, Tamara Stanković, Michael Rajesh Stephen, Revathi Kodali, Veera V. Tiruveedhula, Guanguan Li, Petra Scholze, Bojan D. Marković, Aleksandar Lj. Obradović, Margot Ernst, James M. Cook, Miroslav M. Savić Source Type: research