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

…, W Tueckmantel, KJ Kellar, AP Kozikowski

文献索引：Wei, Zhi-Liang; Xiao, Yingxian; Yuan, Hongbin; Baydyuk, Maryna; Petukhov, Pavel A.; Musachio, John L.; Kellar, Kenneth J.; Kozikowski, Alan P. Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 1721 - 1724

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被引用次数: 43

摘要

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.