期刊
PERSPECTIVES IN MEDICINAL CHEMISTRY
卷 8, 期 -, 页码 -出版社
SAGE PUBLICATIONS LTD
DOI: 10.4137/PMC.S32171
关键词
classical cannabinoids; phytocannabinoids; cannabidiol; tetrahydrocannabinol; Cannabis sativa
资金
- Institutional Development Award (IDeA) from the National Institute of General Medical Sciences (NIGMS) [P20GM104932]
- Research Core(s) of the COBRE, a component of the National Institutes of Health (NIH) [P20GM104932]
The cannabinoids are members of a deceptively simple class of terpenophenolic secondary metabolites isolated from Cannabis sativa highlighted by (-)-Delta(9)-tetrahydrocannabinol (THC), eliciting distinct pharmacological effects mediated largely by cannabinoid receptor (CB1 or CB2) signaling. Since the initial discovery of THC and related cannabinoids, synthetic and semisynthetic classical cannabinoid analogs have been evaluated to help define receptor binding modes and structure-CB1/CB2 functional activity relationships. This perspective will examine the classical cannabinoids, with particular emphasis on the structure-activity relationship of five regions: C3 side chain, phenolic hydroxyl, aromatic A-ring, pyran B-ring, and cyclohexenyl C-ring. Cumulative structure-activity relationship studies to date have helped define the critical structural elements required for potency and selectivity toward CB1 and CB2 and, more importantly, ushered the discovery and development of contemporary nonclassical cannabinoid modulators with enhanced physicochemical and pharmacological profiles.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据