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|Title:||GABAB receptor antagonism by resolved (R)-saclofen in the guinea pig ileum|
|Citation:||European Journal of Pharmacology, 1996; 308(3):1-2|
|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|
|Appears in Collections:||Anaesthesia and Intensive Care publications|
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