Effect of 2-hydroxy-saclofen, an antagonist of GABAB action, upon the binding of baclofen and other receptor ligands in rat cerebrum

Brain Res. 1990 Sep 3;526(2):308-12. doi: 10.1016/0006-8993(90)91237-b.

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

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • Animals
  • Baclofen / analogs & derivatives*
  • Baclofen / metabolism*
  • Baclofen / pharmacology
  • Brain / drug effects*
  • Brain / metabolism
  • GABA Antagonists*
  • Radioligand Assay
  • Rats
  • Receptors, GABA-A / drug effects*
  • Receptors, GABA-B
  • Receptors, Serotonin / drug effects
  • Serotonin Antagonists / metabolism
  • Tetrahydronaphthalenes / metabolism

Substances

  • GABA Antagonists
  • Receptors, GABA-A
  • Receptors, GABA-B
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Tetrahydronaphthalenes
  • phaclofen
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • Baclofen
  • 2-hydroxysaclofen