MS 15203 is a selective GPR171 agonist that increases morphine antinociception and is effective in reducing chronic pain. It can reduce chronic neuropathic and inflammatory pain in male mice.

b-LEN:80 ± 1 nM

To assess the selectivity of MS 15203 for GPR171, screened the ligand against a panel of 80 different transmembrane and soluble receptors, including ~70 GPCRs. MS 15203 dose-dependently displaced radiolabeled b-LEN from hypothalamic membranes with an affinity that was lower than that of b-LEN. IC50 = 80 ± 1 (nM). [1]

To examine the effects of long-term activation of GPR171, administered MS 15203 (2.5 mg/kg) to mice by intraperitoneal injection every third day and fed a high-fat diet to exacerbate the effects of the compound. Knockdown of GPR171 in the hypothalamus significantly at tenuated MS 15203-induced weight gain, implying that chronic administration of MS 15203 affects body weight through GPR171. [1]