GABAB receptor-positive modulators: enhancement of GABAB receptor agonist effects in vivo.

The Journal of Pharmacology and Experimental Therapeutics
Wouter KoekKenner C Rice

Abstract

In vivo effects of GABA(B) receptor-positive modulators suggest that they have therapeutic potential for treating central nervous system disorders such as anxiety, depression, and drug abuse. Although these effects generally are thought to be mediated by positive modulation of GABA(B) receptors, such modulation has been examined primarily in vitro. The present study was aimed at further examining the in vivo positive modulatory properties of the GABA(B) receptor-positive modulators, 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl) phenol (CGP7930) and (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one (rac-BHFF). Both compounds enhanced loss of righting induced by baclofen in mice. However, CGP7930 was less effective and rac-BHFF was less potent for enhancing loss of righting induced by γ-hydroxybutyrate (GHB), which, like baclofen, has GABA(B) receptor agonist properties. In contrast with baclofen- and GHB-induced loss of righting, the hypothermic effects of baclofen and GHB were not enhanced by rac-BHFF but were enhanced by CGP7930 only at doses that produced hypothermia when given alone. CGP7930-induced hypothermia was not attenuated by the GABA(B) receptor antagonist 3-aminopropyl(diethoxymethyl)phosp...Continue Reading

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Citations

Aug 2, 2012·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Alejandro Aparisi ReyBeat Lutz
Sep 29, 2011·The Journal of Pharmacology and Experimental Therapeutics·Julie G HenslerWouter Koek
Feb 10, 2012·The Journal of Pharmacology and Experimental Therapeutics·Wouter KoekKenner C Rice
Jan 1, 2013·The Journal of Pharmacology and Experimental Therapeutics·Wouter KoekKenner C Rice
Apr 8, 2014·CNS Neuroscience & Therapeutics·Roberto FrauMarco Bortolato
Jul 23, 2013·Pharmacology, Biochemistry, and Behavior·Kushal KumarRahul Deshmukh
Oct 30, 2016·European Journal of Pharmacology·Alessandra PorcuM Paola Castelli
Apr 21, 2017·Molecular Pharmacology·Shuai XiaJianfeng Liu
Dec 2, 2011·The Journal of Pharmacology and Experimental Therapeutics·M Paola CastelliFederico Corelli
Apr 3, 2021·Neuropharmacology·Alessandra PorcuM Paola Castelli

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