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Benzodiazepine recognition sites on GABA receptors

Abstract

A role of γ-amino butyric acid (GABA) in benzodiazepine actions1–3 is supported by the GABA stimulation of membrane-bound4–8 and soluble9,10 benzodiazepine receptors and preliminary evidence that GABA protects benzodiazepine receptors from heat inactivation11. We show here that the GABA receptors labelled by 3H-muscimol possess a benzodiazepine recognition site, as benzodiazepines, in proportion to their pharmacological activity, protect 3H-muscimol binding from inactivation by heat and the protein modifying reagent iodoacetamide. We also show that benzodiazepines and GABA act at apparently distinct sites to protect benzodiazepine receptors from heat and iodoacetamide.

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