AM1241

A CB2 receptor agonist; selective for CB2 over CB1 (Kis = 7.1 and 580 nM); considered a protean agonist because it has neutral antagonist and partial agonist activity, depending on the assay utilized; acts in a species-dependent manner in vitro, acting as an agonist at human CB2 receptors (EC50 = 190 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 216 and 463 nM, respectively); produces antinociception to thermal stimuli in rat hindpaw; neuroprotective, preventing Gp120-induced apoptosis in vitro and increasing survival and differentiation of neural progenitor cells; increases hippocampal neurogenesis in GFAP/Gp120 transgenic mice when administered at a dose of 10 mg/kg daily for ten days; delays motor impairment in a murine model of ALS