AM-1221 is a drug that acts as a potent and selective agonist for the cannabinoid receptorCB2, with a Ki of 0.28 nM at CB2 and 52.3 nM at the CB1 receptor, giving it around 180 times selectivity for CB2.[1] The 2-methyl and 6-nitro groups on the indole ring both tend to increase CB2 affinity while generally reducing affinity at CB1, explaining the high CB2 selectivity of AM-1221. However, despite this relatively high selectivity for CB2, its CB1 affinity is still too strong to make it useful as a truly selective CB2 agonist, so the related compound AM-1241 is generally preferred for research purposes.[2][3]
It is illegal to supply, trade, sell, distribute, import or transport the pharmaceutical drug in the UK under the Psychoactive Substances Act 2016 which
was in force on May 26, 2016.
^Deng H (2000). Design and synthesis of selective cannabinoid receptor ligands: Aminoalkylindole and other heterocyclic analogs (Ph.D. Dissertation). University of Connecticut. ProQuest304624325.
^Manera C, Tuccinardi T, Martinelli A (April 2008). "Indoles and related compounds as cannabinoid ligands". Mini Reviews in Medicinal Chemistry. 8 (4): 370–87. doi:10.2174/138955708783955935. PMID18473928.
