[D-Trp8]-γ-MSH (trifluoroacetate salt)

[D-Trp⁸]-γ-MSH is a melanocortin receptor 3 (MC3R) agonist and an analog of γ-melanocyte-stimulating hormone (γ-MSH).¹ It selectively induces cAMP accumulation in cells expressing MC3R over cells expressing MC4R or MC5R (EC₅₀s = 0.33, 100, and 82 nM, respectively, for the human receptors). In vivo, [D-Trp⁸]-γ-MSH (162 nmol/kg, i.v.) reduces the incidence of ventricular tachycardia, ventricular fibrillation, and death in a rat model of myocardial ischemia-reperfusion injury.² It also inhibits urate-induced chemokine (C-X-C) motif ligand 1 (CXCL1) release and peritoneal polymorphonuclear leukocyte accumulation in recessive yellow (e/e) mice with a non-functional MC1R.³

1.Grieco, P., Balse, P.M., Weinberg, D., et al.D-Amino acid scan of γ-melanocyte-stimulating hormone: Importance of Trp8 on human MC3 receptor selectivityJ. Med. Chem.43(26)4998-5002(2000) 2.Mioni, C., Giuliani, D., Cainazzo, M.M., et al.Further evidence that melanocortins prevent myocardial reperfusion injury by activating melanocortin MC3 receptorsEur. J. Pharmacol.477(3)227-234(2003) 3.Getting, S.J., Lam, C.W., Leoni, G., et al.[D-Trp8]-γ-melanocyte-stimulating hormone exhibits anti-inflammatory efficacy in mice bearing a nonfunctional MC1R (recessive yellow e/e mouse)Mol. Pharmacol.70(6)1850-1855(2006)