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Type: Journal article
Title: GABAB receptor antagonism by resolved (R)-saclofen in the guinea pig ileum
Author: Kerr, D.
Ong, J.
Vaccher, C.
Berthelot, P.
Floquet, N.
Vaccher, M.
Debaert, M.
Citation: European Journal of Pharmacology, 1996; 308(3):1-2
Issue Date: 1996
ISSN: 0014-2999
Statement of
Kerr, David I.B. ; Ong, Jennifer ; Vaccher, Claude ; Berthelot, Pascal ; Flouquet, Nathalie ; Vaccher, Marie-Pierre ; Debaert, Michel
Abstract: The GABAB receptor antagonist saclofen (3-amino-2-(4-chlorophenyl)propylsulphonic acid) has been resolved by chiral high-performance liquid chromatography. The enantiomer (R)-saclofen, but not (S)-saclofen, reversibly antagonised the (R,S)-baclofen-induced depression of cholinergic twitch contractions in the guinea-pig ileum with an apparent pA2 of 5.3. Also, 2-hydroxy-saclofen was resolved by the same method, its (S)-enantiomer yielding an apparent pA2 of 5.0. This method provides a convenient resolution of these antagonists.
Keywords: Ileum; Animals; Guinea Pigs; Baclofen; GABA Antagonists; Chromatography, High Pressure Liquid; Stereoisomerism; GABA-B Receptor Antagonists; In Vitro Techniques
RMID: 0030006076
DOI: 10.1016/0014-2999(96)00334-2
Appears in Collections:Anaesthesia and Intensive Care publications

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