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GABAA receptors of the mammalian central nervous system are ligand-gated Cl- ion channels and the sites of action of many pharmacologically important drugs. GABAA receptors were characterized using a potent antagonist, [3H]SR 95531, and agonists such as [3H]GABA and [3H]muscimol. Pretreatment of brain membranes with Triton X-100 or phospholipase A2 increased [3H]GABA and [3H]muscimol binding in the frontal cortex and cerebellum, whereas these treatments significantly decreased [3H]SR 95531 binding. The treatment of rats subacutely with a subconvulsive dose of bicuculline (2 mg/kg, i.p., daily for 10 days) significantly increased the apparent affinity for [3H]muscimol in the frontal cortex, cerebellum, striatum and substantia nigra. On the other hand, the apparent affinity for [3H]SR 95531 binding was significantly decreased in these regions. These results suggest that subacute bicuculline treatment in vivo and treatment in vitro of brain membranes with Triton X-100 or phospholipase A2 bring about a conformational change in the GABAA-receptor molecule, thus resulting in access increase of the GABA agonist and access decrease of the antagonist to GABAA receptors. In the cerebellum, the Bmax values of [3H]muscimol and [3H]SR 95531 binding and Vmax value of muscimol-stimulated 36Cl- uptake were significantly increased following subacute bicuculline treatment with no change in the frontal cortex, with this process involving increased de novo synthesis of GABAA receptors.

Neurochemical and pharmacological studies on brain GABA receptors.