1.
Bioorg Med Chem Lett
; 20(22): 6667-70, 2010 Nov 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20880707
RESUMO
(-)-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)ß(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)ß(2) nAChRs.