AM2233 is a full agonist of the central cannabinoid (CB1) receptor (Ki = 2.8 nM). Most of the affinity towards the CB1 receptor resides within the (R)-enantiomer of AM2233, which exhibits a Ki value of 0.2 nM and has ~8-fold higher affinity for CB1 compared to WIN 55,212-2 (Ki = 1.6 nM).
AM2233 was developed for use as a selective radioligand for mapping the distribution of the CB1 receptor in the brain. Recently, however, AM2233 has received attention as a cannabimimetic acquired for recreational use as a “legal high” replacement for restricted substances. This compound is intended for forensic and research applications.