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https://hdl.handle.net/2440/14744
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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 1879-0712 |
Statement of Responsibility: | 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. |
DOI: | 10.1016/S0014-2999(01)00842-1 |
Description (link): | http://www.elsevier.com/wps/find/journaldescription.cws_home/506087/description#description |
Published version: | http://dx.doi.org/10.1016/s0014-2999(01)00842-1 |
Appears in Collections: | Anaesthesia and Intensive Care publications Aurora harvest 2 |
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