N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki = 50 nM).

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

N-Oleoyl glycine, a lipoamino acid, was able to promote 3T3-L1 adipogenesis through the activation of CB1 receptor and the enhancement of insulin-mediated Akt signaling pathway.