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Type: Journal article
Title: The (S)-enantiomer of 2-hydroxysaclofen is the active GABAB receptor antagonist in central and peripheral preparations
Author: Kerr, D.
Ong, J.
Doolette, D.
Schafer, K.
Prager, R.
Citation: European Journal of Pharmacology, 1995; 287(2):185-189
Publisher: Elsevier
Issue Date: 1995
ISSN: 0014-2999
Abstract: In the guinea-pig isolated ileum, (RS)-(+/-)-baclofen induced a depression of cholinergic twitch contractions, reversibly and competitively antagonised by (S)-2-hydroxysaclofen (pA2 = 5.2 +/- 0.2), but not by (R)-2-hyroxysaclofen. The depression of excitatory field potentials by baclofen ( 5 mu M) in rat CA1 hippocampal slices was antagonised by (S)-2-hydroxysaclofen (100 mu m) (pA2 = 4.3), whilst in rat neocortex, (S)-2-hyroxysaclofen (50-500 mu M) antagonised the baclofen (10 mu M)-induced suppression of spontaneous discharges, the (R)-enantiomer being inactive. These results show that (S)-2-hydroxysaclofen is the active antagonist at central and peripheral GABAB receptors.
Keywords: GABAB receptor; (RS)-(±)-Baclofen; (S)-2-Hydroxysaclofen; (R)-2-Hydroxysaclofen; Ileum, guinea pig; Hippocampus, rat; Neocortex, rat
Rights: © 1995 Elsevier Science B.V. All rights reserved
RMID: 0030006083
DOI: 10.1016/0014-2999(95)00641-9
Appears in Collections:Anaesthesia and Intensive Care publications

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