Melanotan 2 djeluje kao neselektivni agonist melanokortinskih receptora, MC1, MC3, MC4, MC5. U mjeri u kojoj melanotan II proizvodi melanogenezu, smatra se da je to uzrokovano aktivacijom MC1 receptora, dok se smatra da su njegovi klinički dokumentirani seksualni učinci povezani s njegovom sposobnošću aktiviranja MC4 receptora (iako se smatra da MC3 također može biti uključen).

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