Modulation of benzodiazepine binding site sensitivity.

Article date: 1979/5/1

PubMed ID: 40255

Journal name: Pharmacology, biochemistry, and behavior (ISSN: 0091-3057)


Recent studies on agents which alter benzodiazepine binding site sensitivity in brain are described. GABAergic agonists enhance and antagonists inhibit binding to the brain specific benzodiazepine binding site, and the binding can be correlated with effects on neuronal cell firing in the dorsal raphe nucleus. Anions such as chloride, iodide and nitrite also enhance (3H)diazepam binding and this enhancement is consistent with their role in postsynaptic inhibition. Pretreatment of animals with the anticonvulsant, diphenylhydantoin, enhances both diazepam binding and the electrophysiological response to diazepam suggesting one possible locus for the anticonvulsant action of diphenylhydantoin in brain. Taken together, these results suggest the existence of a GABA/Cl- ionophore/BZ binding complex in brain. Preliminary results on the purification of the BZ component of this complex and fluorescent probes for its study are described.

This document is available from: http://directlinks.cc/files/muscimol/40255.pdf

Author List: Tallman J F, Gallager D W

Publication Types: Journal Article; Review

Substances mentioned in the article: Anti-Anxiety Agents; Aminooxyacetic Acid; Muscimol; Phenytoin; Diazepam;

Mesh terms: Aminooxyacetic Acid/pharmacology; Animals; Anti-Anxiety Agents/metabolism; Binding Sites/drug effects; Diazepam/pharmacology; Drug Interactions; Electrophysiology; Humans; Kinetics; Muscimol/pharmacology; Phenytoin/pharmacology;

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