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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. It is considered a protean agonist as it has neutral antagonist and partial agonist activity, depending on the assay utilized. 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). AM1241 produces antinociception to thermal stimuli in rat hindpaw. The antinociceptive actions of AM1241 were blocked by the CB₂ receptor-selective antagonist AM630 but not by the CB₁ receptor-selective antagonist AM251 . 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. AM1241 also delays motor impairment in a murine model of amytrophic lateral sclerosis (ALS).

(2-Iodo-5-nitrophenyl)[1-[(1-methyl-2-piperidinyl)methyl]-1H-indol-3-yl]methanone is a compound from the aminkalkylindole family which exerts potent and selective agonist activity for the cannabinoid receptor CB2.

Potent and selective CB2 receptor agonist (Ki=3.4nM (mouse), Ki=280nM (rat) also in vivo.

AM1241 acts as an antinociceptive agent in several animal pain models. It has a potential to delay disease progression in amyotrophic lateral sclerosis (ALS) mouse model. Intrathecal, intravenous or intraperitoneal administration of AM1241 reduces hyperalgesia and allodynia in neuropathic rats.

CB2

[1] B B YAO. In vitro pharmacological characterization of AM1241: a protean agonist at the cannabinoid CB2 receptor?[J]. British Journal of Pharmacology, 2009, 149 2: 145-154. DOI: 10.1038/sj.bjp.0706838
[2] T.PHILIP MALAN JR. . CB2 cannabinoid receptor-mediated peripheral antinociception[J]. PAIN?, 2001, 93 3: Pages 239-245. DOI: 10.1016/s0304-3959(01)00321-9
[3] HAVA KARSENTY AVRAHAM. The cannabinoid CB2 receptor agonist AM1241 enhances neurogenesis in GFAP/Gp120 transgenic mice displaying deficits in neurogenesis[J]. British Journal of Pharmacology, 2013, 171 2: 468-479. DOI: 10.1111/bph.12478
[4] KATHLINE KIM . AM1241, a cannabinoid CB2 receptor selective compound, delays disease progression in a mouse model of amyotrophic lateral sclerosis[J]. European journal of pharmacology, 2006, 542 1: Pages 100-105. DOI: 10.1016/j.ejphar.2006.05.025