HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with K_is of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats^[1][2][3].

The dose-effect curve of morphine for locomotor activity was shifted downwards in C57Bl/6 mice pretreated with HS014 and in A(y) mice. The dose-effect curve of morphine for antinociception is shifted two- and threefold to the left in C57Bl/6 mice pretreated with HS014 and in A(y) mice, respectively^[2].
Pretreatment with HS014 blocks the effect of IL-1beta on food intake and respiratory exchange ratio (RER) at later time points (beyond 8 h post injection), as well as the hypoactivity and increases metabolic rate^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1563.76

C₇₁H₉₄N₂₀O₁₇S₂

207678-81-7

Ac-Cys-Glu-His-{D-2Nal}-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2 (Disulfide bridge:Cys1-Cys8)

Ac-CEH-{D-2Nal}-RWGCPPKD-NH2 (Disulfide bridge:Cys1-Cys8)

Room temperature in continental US; may vary elsewhere.

• [1]. Schi?th HB,et al. Discovery of novel melanocortin4 receptor selective MSH analogues. Br J Pharmacol. 1998;124(1):75-82.  [Content Brief]

  [2]. Ercil NE, et al. HS014, a selective melanocortin-4 (MC4) receptor antagonist, modulates the behavioral effects of morphine in mice. Psychopharmacology (Berl). 2005;180(2):279-285.  [Content Brief]

  [3]. Kask A, et al. Selective antagonist for the melanocortin 4 receptor (HS014) increases food intake in free-feeding rats. Biochem Biophys Res Commun. 1998;245(1):90-93.  [Content Brief]