title: Effect of 2-hydroxy-saclofen, an antagonist of GABAB action, upon the binding of baclofen and other receptor ligands in rat cerebrum.
abstract: 2-Hydroxysaclofen (2-OH-saclofen), a newly available compound which blocks certain physiological actions of the gamma-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.
authors.affiliation: Department of Cell Biology, Baylor College of Medicine, Houston, TX 77030.
authors.forename: M I
authors.initials: MI
authors.lastname: al-Dahan
authors.forename: M H
authors.initials: MH
authors.lastname: Tehrani
authors.forename: R H
authors.initials: RH
authors.lastname: Thalmann
mesh_terms: D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000818:Animals; D001418:Baclofen / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000494:pharmacology; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D018756:GABA Antagonists; D011869:Radioligand Assay; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects*; D018080:Receptors, GABA-B; D011985:Receptors, Serotonin / Q000187:drug effects; D012702:Serotonin Antagonists / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000378:metabolism
chemical_list: D018756:GABA Antagonists; D011963:Receptors, GABA-A; D018080:Receptors, GABA-B; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D013764:Tetrahydronaphthalenes; C052329:phaclofen; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D001418:Baclofen; C057491:2-hydroxysaclofen