AM-1221 is a drug that acts as a potent and selective agonist for the cannabinoid receptor CB<sub>2</sub>, with a K<sub>i</sub> of 0.28 nM at CB<sub>2</sub> and 52.3 nM at the CB<sub>1</sub> receptor, giving it around 180 times selectivity for CB<sub>2</sub>. The 2-methyl and 6-nitro groups on the indole ring both tend to increase CB<sub>2</sub> affinity while generally reducing affinity at CB<sub>1</sub>, explaining the high CB<sub>2</sub> selectivity of AM-1221. However, despite this relatively high selectivity for CB<sub>2</sub>, its CB<sub>1</sub> affinity is still too strong to make it useful as a truly selective CB<sub>2</sub> agonist, so the related compound AM-1241 is generally preferred for research purposes.
In the United States, all CB<sub>1</sub> receptor agonists of the 3-(1-naphthoyl)indole class such as AM-1221 are Schedule I Controlled Substances.
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.