Fontana Gianfranco, Savona Giuseppe, Rodríguez Benjamín, Dersch Christina M, Rothman Richard B, Prisinzano Thomas E
Dipartimento di Chimica Organica 'E. Paternò', Università degli Studi di Palermo, Parco d'Orleans 2, I-90128 Palermo, Italy.
Tetrahedron. 2009 Feb 21;65(8):1708-1715. doi: 10.1016/j.tet.2008.12.009.
Salvinorin A (1), a neoclerodane diterpene from the hallucinogenic mint Salvia divinorum, is the only known naturally occurring non-nitrogenous and specific κ-opioid agonist. Some oxidative modifications of the A ring in the congeners of 1 isolated from Salvia splendens salviarin, splenolide B, splendidin and in the non-natural 8-epi-salviarin gave new derivatives, some of which were tested as agonists at opioid receptors. However, none of these compounds were active. The presence of the C-18, C-19 lactone could be at the origin of the observed lack of binding affinity.
萨尔维诺林A（1）是从致幻薄荷鼠尾草中提取的一种新克罗烷二萜，是唯一已知的天然存在的非含氮特异性κ-阿片受体激动剂。从鼠尾草、脾内酯B、灿烂菌素中分离出的1的同系物以及非天然的8-表鼠尾草素中A环的一些氧化修饰产生了新的衍生物，其中一些作为阿片受体激动剂进行了测试。然而，这些化合物均无活性。C-18、C-19内酯的存在可能是观察到缺乏结合亲和力的原因。
