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Type: Journal article
Title: Comparative activities of the enantiomeric GABAB receptor agonists CGP 44532 and 44533 in central and peripheral tissues
Author: Ong, J.
Bexis, S.
Marino, V.
Parker, D.
Kerr, D.
Froestl, W.
Citation: European Journal of Pharmacology, 2001; 412(1):27-37
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 neocortical slices maintained in Mg(2+)-free Krebs medium, the gamma-aminobutyric acid (GABA(B)) receptor agonists baclofen, (3-amino-2(S)-hydroxypropyl)methylphosphinic acid (CGP 44532), and its (R)-enantiomer CGP 44533 depressed the frequency of spontaneous discharges in a concentration-dependent manner (EC(50)=10, 6.5, and 50 microM, respectively). These effects were reversibly antagonised by the GABA(B) receptor antagonist (+)-(S)-5,5 dimethylmorpholinyl-2-acetic acid (Sch 50911) (3, 10, and 30 microM) (average pA(2) value=6.0+/-0.2). In neocortical wedges, baclofen, CGP 44532 and CGP 44533 elicited concentration-dependent hyperpolarisations (the EC(50)s were 14, 7.5 and 16 microM, respectively) sensitive to Sch 50911 (1, 5, 10 microM) (average pA(2) value=6.0+/-0.1), whilst they also depressed ileal electrically elicited cholinergic twitch contractions (EC(50)=11, 7, and 50 microM) that were antagonised by Sch 50911 (average pA(2) value=6.0+/-0.1). In electrically stimulated brain slices preloaded with [3H]GABA, baclofen, CGP 44532 and CGP 44533 decreased [3H]GABA release (IC(50)=5, 0.45, and 10 microM); this effect was reversed by Sch 50911 (50 microM). It is concluded that CGP 44532 is a far more potent agonist at GABA(B) autoreceptors than at central or peripheral heteroreceptors.
Keywords: Ileum
Guinea Pigs
Rats, Sprague-Dawley
Phosphinic Acids
gamma-Aminobutyric Acid
Receptors, GABA-B
Dose-Response Relationship, Drug
GABA-B Receptor Agonists
Description: Copyright © 2001 Published by Elsevier Science B.V. All rights reserved.
DOI: 10.1016/S0014-2999(00)00945-6
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