Synthesis and pharmacological evaluation of novel 9-and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity

…, W Tueckmantel, KJ Kellar, AP Kozikowski

Index: Chellappan, Sheela K.; Xiao, Yingxian; Tueckmantel, Werner; Kellar, Kenneth J.; Kozikowski, Alan P. Journal of Medicinal Chemistry, 2006 , vol. 49, # 9 p. 2673 - 2676

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Citation Number: 43

Abstract

We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the α4β2 nAChR subtype in binding assays than cytisine. The 9-vinyl derivative was found to have a very similar agonist activity profile to that of cytisine.