Identification of 9-fluoro substituted (-)-cytisine derivatives as ligands with high affinity for nicotinic receptors |
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Authors: | Houllier Nicolas Gopisetti JaganMohan Lestage Pierre Lasne Marie-Claire Rouden Jacques |
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Affiliation: | Laboratoire de Chimie Moléculaire et Thioorganique, UMR 6507 CNRS, ENSICAEN-Université de Caen Basse-Normandie, Institut Normand de Chimie Moléculaire, Médicinale et Macromoléculaire FR 3038 CNRS, 6 Boulevard du Maréchal Juin, 14050 Caen, France. |
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Abstract: | (-)-9-Fluorocytisine, (-)-9-methylcytisine and (-)-9-trifluoromethylcytisine were synthesized from the natural product (-)-cytisine. 9-Methyl and 9-trifluoromethyl cytisines display a remarkable affinity at the α(4)β(2) nicotinic receptor subtype (0.2 nM) with a high selectivity versus the α(7) nAChR subtype. Comparison of the affinity values suggests that the size of the substituent at the 9 position of (-)-cytisine seems more important than electronic factors for efficient binding and selectivity at α(4)β(2) nAChRs. |
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