新型9-和10-取代金雀花碱衍生物的合成与药理评价。亚型选择性增强的烟碱配体。
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
作者信息
Chellappan Sheela K, Xiao Yingxian, Tueckmantel Werner, Kellar Kenneth J, Kozikowski Alan P
机构信息
Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Illinois 60612, USA.
出版信息
J Med Chem. 2006 May 4;49(9):2673-6. doi: 10.1021/jm051196m.
Abstract
We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the alpha4beta2 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.
摘要
我们报告了几种金雀花碱衍生物的合成及药理特性。其中，两种10-取代衍生物在结合试验中对α4β2烟碱型乙酰胆碱受体亚型的选择性比金雀花碱高得多。发现9-乙烯基衍生物具有与金雀花碱非常相似的激动剂活性谱。
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