Diazepam stimulates the binding of GABA and muscimol but not THIP to rat brain membranes.
Diazepam (10-1000 nM) enhanced the binding of [3H]GABA and of the monocyclic GABA agonist [3H]muscimol, but failed to alter binding of the bicyclic GABA agonist [3H]THIP to fresh, well washed rat brain membranes incubated at 2 degrees C. Although stimulation of [3H]diazepam binding by THIP was observed at higher incubation temperatures and in the presence of chloride ions, these measures did not induce a corresponding enhancement of [3H]THIP binding by diazepam. These results extend earlier observations of the unusual behavior of THIP as a selective GABA agonist, and emphasize that enhancement of benzodiazepine binding by GABA agonists is not necessarily reflected in a complementary manner by any action of benzodiazepines on the binding of GABA agonists.
D000700:Analgesics / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D003975:Diazepam / Q000378:metabolism / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007555:Isoxazoles / Q000378:metabolism* / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D009118:Muscimol / Q000378:metabolism*; D010080:Oxazoles / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000378:metabolism; D011963:Receptors, GABA-A; D005680:gamma-Aminobutyric Acid / Q000378:metabolism* / Q000494:pharmacology
D000700:Analgesics; D007555:Isoxazoles; D010080:Oxazoles; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; D009118:Muscimol; D005680:gamma-Aminobutyric Acid; C015542:gaboxadol; D003975:Diazepam