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GABAB receptor antagonism by resolved (R)-saclofen in the guinea-pig ileum
1Department of Anaesthesia and Intensive Care, University of Adelaide, South Australia, Australia. dkerr@medicine.adelaide.edu.au
European Journal of Pharmacology
|July 25, 1996
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.