The GABA agonist THIP a muscimol analogue, does not interfere with the benzodiazepine binding site on rats cortical membranes.
THIP, a cyclic analogue of muscimol, is a powerful GABA agonist. It is as active as GABA in displacing [3H]muscimol from its binding site to cerebellar membranes (IC50 = 31.5 +/- 2.5 mM). However, unlike muscimol or GABA, it is devoid of any modulatory interaction with the benzodiazepine binding site on rat's cortical membranes. Homotaurine, isoguvacine and imidazole acetic acid are less active than muscimol and GABA for increasing the affinity of [3H]diazepam to cortical membrane preparations.
D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism*; D007093:Imidazoles / Q000494:pharmacology; D066298:In Vitro Techniques; D007539:Isonicotinic Acids / Q000494:pharmacology; D008297:Male; D009118:Muscimol / Q000031:analogs & derivatives / Q000494:pharmacology*; D010080:Oxazoles / Q000494:pharmacology*; D051381:Rats; D011955:Receptors, Drug / Q000187:drug effects*; D013654:Taurine / Q000031:analogs & derivatives / Q000494:pharmacology; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
D007093:Imidazoles; D007539:Isonicotinic Acids; D010080:Oxazoles; D011955:Receptors, Drug; D013654:Taurine; D009118:Muscimol; D005680:gamma-Aminobutyric Acid; D003975:Diazepam