Biological ActivityMSG 606 is a potent human MC1 receptor antagonist (IC50 = 17 nM). Also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). Exhibits binding affinity for A375 melanoma cells in vitro. Reverses morphine-induced hyperalgesia in female mice, with no effect in male mice. γMSH analog.
(Modifications: X = Butanoic acid, Phe-4 = D-Phe, Trp-6 = D-Trp, Gly-11 = C-terminal amide, Carba sulfide bridge: X-1 - Cys-7)
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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Sex-specific mediation of opioid-induced hyperalgesia by the melanocortin-1 receptor.
Juni et al.
Spinal and supraspinal N-methyl-D-aspartate and melanocortin-1 receptors contribute to a qualitative sex difference in morphine-induced hyperalgesia.
Arout et al.
An unusual conformation of γ-melanocyte-stimulating hormone analogues leads to a selective human melanocortin 1 receptor antagonist for targeting melanoma cells.
Cai et al.
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