GABA Autoreceptors Are Not Coupled to Benzodiazepine Receptors in Rat Cerebral Cortex

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Abstract
Depolarization-induced release of [3H]-GABA from preloaded slices of rat cerebral cortex was inhibited by muscimol and THIP [4,5,6,7-tetrahydroisoxazolo(5-4-c)pyridin-3-ol] in a dose-dependent fashion. This inhibition of release was prevented by the GABA antagonists bicuculline and picrotoxin. The results confirm the existence of GABA autoreceptors on GABAergic terminals. Since benzodiazepines facilitate postsynaptic GABA actions, the effect of flunitrazepam on the inhibition of GABA release mediated through the autoreceptors was examined. At a concentration of 1 .mu.M or 10 .mu.M, flunitrazepam had no effect on the IC50 [median inhibitory concentration] values for muscimol or THIP in inhibiting stimulated GABA release. GABA autoreceptors are apparently not functionally coupled to benzodiazepine receptors in rat cerebral cortex.

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