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GABAB Receptor Antagonism by Resolved (R)-saclofen in the Guinea-Pig Ileum

D I Kerr, J Ong, C Vaccher, P Berthelot, N Flouquet, M P Vaccher, M Debaert

Eur J Pharmacol. 1996 Jul 25;308(3):R1-2.

PMID: 8858312

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP125464428 Saclofen Saclofen 125464-42-8 Price
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