AM6538 is a long-acting, high affinity, and pseudo-irreversible cannabinoid antagonist, structurally analogous to rimonabant. It serves as a valuable tool for assessing the apparent efficacy of cannabinoid partial and full agonists. Additionally, AM6538 holds potential for future investigations that necessitate 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].