Medicinal Chemistry of Cb1 Cannabinoid eceptor Antagonists

摘要

The long history of Cannabis use has resulted in the development of cannabinoid receptor agonist drugs,such as tetra-hydrocannabinol (DELTA~9-THC,dronabinol)(Figure 1),which have a stimulatory effect on appetite. Only within the past 15 years the research efforts in the cannabinoid area have resulted in the crucial discovery of the endocannabinoid system [1]which comprises to date of two characterized and cloned G-protein-coupled cannabinoid receptors CB_1 and CB_2,five endogenous polyunsatu-rated lipid-like ligands (the so-called endocannabinoids)and the enzymes involved in their formation and breakdown,such as fatty acid amide hydrolase (FAAH)and monoglyceride lipase.