EFFECT OF 2-HYDROXY-SACLOFEN, AN ANTAGONIST OF GABA-B ACTION, UPON THE BINDING OF BACLOFEN AND OTHER RECEPTOR LIGANDS IN RAT CEREBRUM

2-Hydroxysaclofen (2-OH-saclofen), a newly available compound which blocks certain physiological actions of the γ-aminobutyric acidB (GABAB) agonist, baclofen, was found to displace [3H]baclofen at least 10-fold more potently than did phaclofen, a previously available antagonist of GABAB action. 2-OH-Saclofen reduced both the affinity and apparent density of baclofen binding sites and displaced baclofen binding at least 60-fold more potently than it displaced the binding of ligands for 3 other transmitters present in the rat cerebral cortex. © 1990.