Neoclerodane diterpenes as a novel scaffold for μ opioid receptor ligands

Neoclerodane diterpenes as a novel scaffold for μ opioid receptor ligands
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DOI:
10.1021/jm048963m
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发表时间:
2005-07-28
影响因子:
7.3
通讯作者:
Prisinzano, TE
Prisinzano, TE
中科院分区:
医学1区
文献类型:
--
作者:
Harding, WW;Tidgewell, K;Prisinzano, TE

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通过对丹参活性成分salvinorin A的结构修饰,合成了具有阿片受体亲和力和活性的新型新氯罗丹二萜。我们在这项研究中报道了一种具有mu阿片受体亲和力的非氮新氯烷二萜(13),它是mu阿片受体的激动剂。这代表了一种新型结构类阿片受体激动剂的鉴定。
Structural modification of salvinorin A, the active component of Salvia divinorum, has resulted in the synthesis of novel neoclerodane diterpenes with opioid receptor affinity and activity. We report in this study a nonnitrogenous neoclerodane diterpene with mu opioid receptor affinity (13) that is an agonist at mu opioid receptors. This represents the identification of a novel structural class of mu opioid receptor agonists.