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Type: Journal article
Title: CGP 36216 is a selective antagonist at GABAB presynaptic receptors in rat brain
Author: Ong, J.
Bexis, S.
Marino, V.
Parker, D.
Kerr, D.
Froestl, W.
Citation: European Journal of Pharmacology, 2001; 415(2-3):191-195
Publisher: Elsevier Science BV
Issue Date: 2001
ISSN: 0014-2999
Statement of
Jennifer Ong, Sotiria Bexis, Victor Marino, David A. S. Parker, David I. B. Kerr and Wolfgang Froestl
Abstract: In rat neocortical preparations maintained in Mg(2+)-free Krebs medium, baclofen depressed the frequency of spontaneous discharges in a concentration-dependent manner (EC(50) = 6 microM), sensitive to (3-aminopropyl)ethylphosphinic acid (CGP 36216) (100, 300 and 500 microM) (pA(2) = 3.9 +/- 0.1). By contrast, CGP 36216, up to 1 mM, was ineffective in antagonising baclofen-induced hyperpolarisations, mediated through gamma-aminobutyric acid(B) (GABA(B)) postsynaptic receptors. In electrically stimulated brain slices preloaded with [3H]GABA, CGP 36216 increased [3H]GABA release (IC(50) = 43 microM), which was reversed by baclofen (20 microM). While CGP 36216 is ineffective at GABA(B) postsynaptic receptors, it is appreciably more active at presynaptic receptors.
Keywords: Neocortex; Animals; Rats; Rats, Sprague-Dawley; Phosphinic Acids; gamma-Aminobutyric Acid; Baclofen; Organophosphorus Compounds; Autoreceptors; Receptors, GABA-B; GABA Agonists; GABA Antagonists; Dose-Response Relationship, Drug; Male
Description: Copyright © 2001 Elsevier Science B.V. All rights reserved.
RMID: 0020010727
DOI: 10.1016/S0014-2999(01)00842-1
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Appears in Collections:Anaesthesia and Intensive Care publications

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