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AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability[1]. AM6538 is a cannabinoid antagonist that binds CB1 receptors expressed in HEK-293 cells in a wash-resistant manner[1]. AM6538 (1~10 mg/kg) antagonizes the antinociceptive effects of cannabinoid agonists in mice[1].AM6538 (10 mg/kg) shows that there are some recovery in the effects of AM4054. AM6538 dose dependently decreases the tau values for all cannabinoid agonists, reflecting reductions in the available receptors. AM6538 produces enduring antagonism, with robust effects on the tetrahydrocannabinol dose-effect function evident up to 7 days after treatment[1].

[1]. Paronis CA, et al. Long-Lasting In Vivo Effects of the Cannabinoid CB1 Antagonist AM6538. J Pharmacol Exp Ther. 2018;364(3):485-493.