Pravadoline is a cannabinoid receptor agonist. Pravadoline inhibited the PGs synthesis in mouse brain and displayed antinociceptive activity in rodents subjected to a variety of thermal, chemical, and mechanical nociceptive stimuli.

A potent, and selective CB1 receptor antagonist with Ki of 0.7 nM/0.12 nM in binding and functional assays respectively; has low affinity (Ki=7600 nM) for human CB2 receptors; reverses cannabinoid agonist mediated responses, reduces food intake, and increases energy expenditure and fat oxidation in rodents.ObesityPhase 3 Discontinued

A potent, selective full agonist of the peripheral cannabinoid receptor CB2 with Ki of 1.8 nM.