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.
Bioorg Med Chem Lett. 2010 Nov 15;20(22):6667-70. doi: 10.1016/j.bmcl.2010.09.017. Epub 2010 Sep 15.
(-)-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.
（-）-9-氟胞啶、（-）-9-甲基胞啶和（-）-9-三氟甲基胞啶是从天然产物（-）-胞啶合成的。9-甲基和 9-三氟甲基胞啶在α（4）β（2）烟碱型乙酰胆碱受体亚型（0.2 nM）上表现出显著的亲和力，对α（7）nAChR 亚型具有很高的选择性。亲和力值的比较表明，（-）-胞啶 9 位取代基的大小对于在α（4）β（2）烟碱型乙酰胆碱受体上的有效结合和选择性似乎比电子因素更为重要。
