Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.
David Y W Lee, Minsheng He, Leelakrishna Kondaveti, Lee-Yuan Liu-Chen, Zhongze Ma, Yulin Wang, Yong Chen, Jian-Guo Li, Cécile Béguin, William A Carlezon, Bruce M Cohen
Bioorganic & Medicinal Chemistry Letters October 1, 2005 DOI: 10.1016/j.bmcl.2005.06.092 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Peer reviewed |
|---|---|
| Interventions | Salvinorin A C(4)-modified salvinorin A analogues |
| Topics | Salvia divinorum |
| Key points | Modifying the C(4) position of salvinorin A produced a series of analogues that were screened at the human kappa-opioid receptor, and several potent new agonists were identified. The text does not report specific potencies or binding values. |
Abstract
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.
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- Synthetic studies of neoclerodane diterpenes from Salvia divinorum: semisynthesis of salvinicins A and B and other chemical transformations of salvinorin A. Journal of Natural Products 2006
- Synthetic studies of neoclerodane diterpenoids from Salvia splendens and evaluation of Opioid Receptor affinity. Tetrahedron December 20, 2008
- Synthesis of neoclerodane diterpenes and their pharmacological effects. Topics in current chemistry 2011
- CoMFA analyses of C-2 position salvinorin A analogs at the kappa-opioid receptor provides insights into epimer selectivity. Journal of molecular graphics & modelling April 1, 2010
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