Adelaide Research & Scholarship
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https://hdl.handle.net/2440/5994
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| Type: | Journal article |
| Title: | GABAB receptor antagonism by resolved (R)-saclofen in the guinea pig ileum |
| Author: | Kerr, D. Ong, J. Vaccher, C. Berthelot, P. Floquet, N. Vaccher, M.P. Debaert, M. |
| Citation: | European Journal of Pharmacology, 1996; 308(3):1-2 |
| Publisher: | Elsevier BV |
| Issue Date: | 1996 |
| ISSN: | 0014-2999 1879-0712 |
| Statement of Responsibility: | 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 In Vitro Techniques |
| DOI: | 10.1016/0014-2999(96)00334-2 |
| Published version: | http://dx.doi.org/10.1016/0014-2999(96)00334-2 |
| Appears in Collections: | Anaesthesia and Intensive Care publications Aurora harvest 5 |
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