AM1241

AM1241 is a cannabinoid (CB) receptor agonist that is selective for CB₂ over CB₁ with K_i values of 7.1 and 580 nM for human recombinant receptors transfected into HEK and CHO cells, respectively, in a radioligand binding assay.^1,2 It is considered a protean agonist as it has neutral antagonist and partial agonist activity, depending on the assay utilized.¹ It is also 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).³ AM1241 produces antinociception to thermal stimuli in rat hindpaw. The antinociceptive actions of AM1241 were blocked by the CB₂ receptor-selective antagonist AM630 (Item No. 10006974) but not by the CB₁ receptor-selective antagonist AM251 (Item No. 71670). AM1241 is neuroprotective, preventing HIV-1 glycoprotein Gp120-induced apoptosis in primary human and murine neural progenitor cells and increasing cell survival and differentiation. It increases hippocampal neurogenesis and decreases astro- and gliogenesis in GFAP/Gp120 transgenic mice when administered at a dose of 10 mg/kg daily for ten days.⁴ AM1241 also delays motor impairment in a murine model of amytrophic lateral sclerosis (ALS).⁵

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1. Yao, B.B., Mukherjee, S., Fan, Y., et al. In vitro pharmacological characterization of AM1241: A protean agonist at the cannabinoid CB₂ receptor? Br. J. Pharmacol. 149(2), 145-154 (2006).

2. Malan, T.P., Jr., Ibrahim, M.M., Deng, H., et al. CB₂ cannabinoid receptor-mediated peripheral antinociception. Pain 93(3), 239-245 (2001).

3. Bingham, B., Jones, P.G., Uveges, A.J., et al. Species-specific in vitro pharmacological effects of the cannabinoid receptor 2 (CB₂) selective ligand AM1241 and its resolved enantiomers. Br. J. Pharmacol. 151(7), 1061-1070 (2007).

4. Abraham, H.K., Jiang, S., Fu, Y., et al. The cannabinoid CB₂ receptor agonist AM1241 enhances neurogenesis in GFAP/Gp120 transgenic mice displaying deficits in neurogenesis. Br. J. Pharmacol. 171(2), 468-479 (2014).

5. Kim, K., Moore, D.H., Makriyannis, A., et al. AM1241, a cannabinoid CB₂ receptor selective compound, delays disease progression in a mouse model of amyotrophic lateral sclerosis. Eur. J. Pharmacol. 542(1-3), 100-105 (2006).