Effect of 2-hydroxy-saclofen, an antagonist of GABAB 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 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.
al-Dahan
M I
MI
Department of Cell Biology, Baylor College of Medicine, Houston, TX 77030.
Tehrani
M H
MH
Thalmann
R H
RH
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
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