Pretreatment with GABA and modulatory ligands enhances GABA receptor binding.
GABA pretreatment at 37 degrees C but not at 4 degrees C enhanced subsequent [3H]GABA binding in a concentration-dependent manner (EC50 = 440 nM) by increasing the number of high and low affinity sites. The effect mediated by GABAA receptors was attenuated by bicuculline methiodide and picrotoxinin and potentiated by pentobarbital, flurazepam and Triton X-100. These results can be interpreted by the facilitated removal of endogenous substances and/or by a temperature-restricted conversion of the GABA receptor populations.
D000818:Animals; D001418:Baclofen / Q000494:pharmacology; D001665:Binding Sites; D002540:Cerebral Cortex / Q000378:metabolism; D004347:Drug Interactions; D066298:In Vitro Techniques; D007555:Isoxazoles / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000378:metabolism*; D013570:Synaptic Membranes / Q000378:metabolism; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology*
D007555:Isoxazoles; D011963:Receptors, GABA-A; D005680:gamma-Aminobutyric Acid; D001418:Baclofen; C015542:gaboxadol