Article date: 1979/10/15
PubMed ID: 510380
Journal name: European journal of pharmacology (ISSN: 0014-2999)
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.
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;