510380

THIP and isoguvacine are partial agonists of GABA-stimulated benzodiazepine receptor binding.

Article date: 1979/10/15

PubMed ID: 510380

Journal name: European journal of pharmacology (ISSN: 0014-2999)

ABSTRACT

The effects of THIP and isoguvacine on 3H-flunitrazepam binding to washed membranes prepared from the cerebral cortex of adult rats have been examined. THIP, which has only minimal stimulatory effects on benzodiazepine (BZ) receptor binding, has been found to inhibit the stimulation induced by small concentrations (2 microM) of exogenous GABA. While isoguvacine stimulates BZ receptor binding, although to a smaller extent than GABA, it also antagonizes the stimulation of BZ receptor binding induced by GABA. Thus THIP and isoguvacine exhibit the properties of a partial agonist of GABA-stimulated BZ receptor binding.

This document is available from: http://directlinks.cc/files/muscimol/510380.pdf

Author List: Karobath M, Lippitsch M

Publication Types: Journal Article

Substances mentioned in the article: Isonicotinic Acids; Isoxazoles; Oxazoles; Receptors, Drug; Benzodiazepines; Muscimol; gamma-Aminobutyric Acid; Flunitrazepam;

Mesh terms: Animals; Benzodiazepines/metabolism; Cerebral Cortex/metabolism; Drug Synergism; Flunitrazepam/metabolism; In Vitro Techniques; Isonicotinic Acids/pharmacology; Isoxazoles/pharmacology; Muscimol/pharmacology; Oxazoles/pharmacology; Rats; Receptors, Drug/drug effects; gamma-Aminobutyric Acid/pharmacology;

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