SER-601

SER-601 is a potent and selective peripheral cannabinoid (CB₂) receptor agonist with 190-fold selectivity for CB₂ over the central CB₁ receptor (K_is = 6.3 and 1,220 nM, respectively).^1,2 At 3 mg/kg, SER-601 has analgesic effects in a formalin-induced nocifensive study in mice without cannabis-like behavioral effects due to its low affinity for the CB₁ receptor.^1,2 SER-601 also has antidiabetic effects.³ Two to four week exposure to SER-601 ameliorates insulin resistance in vivo and increases insulin secretion and accumulation in pancreatic islets isolated from high-fat diet/streptozotocin (HFD/STZ)-induced diabetic mice.

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1. Pasquini, S., Botta, L., Semeraro, T., et al. Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo. J. Med. Chem. 51(16), 5075-5084 (2008).

2. Pasquini, S., Ligresti, A., Mugnaini, C., et al. Investigations on the 4-quinolone-3-carboxylic acid motif. 3. Synthesis, structure-affinity relationships, and pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ligands. J. Med. Chem. 53(16), 5915-5928 (2012).

3. Zhang, X., Gao, S., Niu, J., et al. Cannabinoid 2 receptor agonist improves systemic sensitivity to insulin in high-fat diet/streptozotocin-induced diabetic mice. Cell Physiol. Biochem. 40(5), 1175-1185 (2016).