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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Animals
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Baclofen / analogs & derivatives*
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Baclofen / metabolism*
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Baclofen / pharmacology
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Brain / drug effects*
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Brain / metabolism
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GABA Antagonists*
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Radioligand Assay
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Rats
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Receptors, GABA-A / drug effects*
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Receptors, GABA-B
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Receptors, Serotonin / drug effects
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Serotonin Antagonists / metabolism
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Tetrahydronaphthalenes / metabolism
Substances
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GABA Antagonists
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Receptors, GABA-A
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Receptors, GABA-B
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Receptors, Serotonin
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Serotonin Antagonists
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Tetrahydronaphthalenes
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phaclofen
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Baclofen
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2-hydroxysaclofen