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https://hdl.handle.net/2440/5985
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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 1879-0712 |
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 |
DOI: | 10.1016/0014-2999(95)00641-9 |
Published version: | http://dx.doi.org/10.1016/0014-2999(95)00641-9 |
Appears in Collections: | Anaesthesia and Intensive Care publications Aurora harvest |
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