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GABAB receptor antagonism by resolved (R)-saclofen in the guinea-pig ileum.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 1996 Jul 25; Vol. 308 (3), pp. R1-2. - Publication Year :
- 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.
Details
- Language :
- English
- ISSN :
- 0014-2999
- Volume :
- 308
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 8858312
- Full Text :
- https://doi.org/10.1016/0014-2999(96)00334-2