C(4)修饰的鼠尾草酚A类似物的合成及体外药理学研究
Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.
作者信息
Lee David Y W, He Minsheng, Kondaveti Leelakrishna, Liu-Chen Lee-Yuan, Ma Zhongze, Wang Yulin, Chen Yong, Li Jian-Guo, Beguin Cecile, Carlezon William A, Cohen Bruce
机构信息
Bioorganic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.
出版信息
Bioorg Med Chem Lett. 2005 Oct 1;15(19):4169-73. doi: 10.1016/j.bmcl.2005.06.092.
Salvinorin A is the most potent naturally occurring opioid agonist with a high selectivity and affinity for kappa-opioid receptor. To explore its structure-activity relationships, modifications at the C(4) position have been studied and a series of salvinorin A derivatives were prepared. These C(4)-modified salvinorin A analogues were screened for binding and functional activities at the human kappa-opioid receptor and several potent new agonists have been identified.
萨尔维诺林A是最有效的天然存在的阿片类激动剂，对κ-阿片受体具有高选择性和亲和力。为了探索其构效关系，对C(4)位的修饰进行了研究，并制备了一系列萨尔维诺林A衍生物。对这些C(4)修饰的萨尔维诺林A类似物进行了人κ-阿片受体结合和功能活性筛选，已鉴定出几种强效的新激动剂。
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