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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

GABAB receptor antagonism by resolved (R)-saclofen in the guinea-pig ileum.

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.[1]

References

  1. GABAB receptor antagonism by resolved (R)-saclofen in the guinea-pig ileum. Kerr, D.I., Ong, J., Vaccher, C., Berthelot, P., Flouquet, N., Vaccher, M.P., Debaert, M. Eur. J. Pharmacol. (1996) [Pubmed]
 
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