AM-630 (6-Iodopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptorCB2, with a Ki of 32.1nM at CB2 and 165x selectivity over CB1, at which it acted as a weak partial agonist. It is used in the study of CB2 mediated responses and has been used to investigate the possible role of CB2 receptors in the brain. AM-630 is significant as one of the first indole derived cannabinoid ligands substituted on the 6-position of the indole ring, a position that has subsequently been found to be important in determining affinity and efficacy at both the CB1 and CB2 receptors, and has led to the development of a large number of related derivatives.
^Eissenstat, M. A.. et al. (1995). "Aminoalkylindoles: Structure-Activity Relationships of Novel Cannabinoid Mimetics". Journal of Medicinal Chemistry38 (16): 3094–105. doi:10.1021/jm00016a013. PMID7636873.CS1 maint: Explicit use of et al. (link)edit
^Frost, J. M. et al. (2008). "Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity". Journal of Medicinal Chemistry51 (6): 1904–12. doi:10.1021/jm7011613. PMID18311894.CS1 maint: Explicit use of et al. (link)edit