Stimulation of GABA receptor binding by barbiturates.

Barbiturates increase Na+-independent GABA binding to bovine cerebral cortex membranes. The relative activity of a series of compounds to enhance GABA binding correlates significantly with their anesthetic activity and with their ability to reverse bicuculline antagonism of GABA responses. There are regional differences in the maximal percent stimulation of GABA binding by pentobarbital; a low stimulation in cerebellum.