Latest progress in the identification of novel synthetic ligands for the cannabinoid CB2 receptor.
Cannabinoid receptors, belonging to the superfamily of G-protein coupled receptors, play a major role in pathophysiology of a wide range of disparate diseases. Cannabinoid CB2 receptor, which mainly locates in peripheral tissues, represents as a promising drug target for the treatment of pain, osteoporosis, liver disorders, and so on without serious CNS side effects. In the past decades, the identification and optimization of selective ligands for the CB2 receptor has been a major objective in drug discovery. In the present review, we describe recent advances in the development of novel chemotypes of the CB2 receptor selective ligands, and give a simple discussion for the corresponding structure-activity relationships of them.
Shuang
S
Han
Jiong-Jiong
JJ
Chen
College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Rd, Hangzhou 310058, Zhejiang, P. R. China. chjz@zju.edu.cn.
Jian-Zhong
JZ
Chen
D000818:Animals; D063386:Cannabinoid Receptor Agonists / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D063387:Cannabinoid Receptor Antagonists / Q000032:analysis / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D055808:Drug Discovery; D006801:Humans; D008024:Ligands; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D063386:Cannabinoid Receptor Agonists; D063387:Cannabinoid Receptor Antagonists; D008024:Ligands; D043885:Receptor, Cannabinoid, CB2