Melanotan-2 is a lab-made ring-shaped peptide of seven amino acids (a cyclic heptapeptide) built from alpha-melanocyte-stimulating hormone (alpha-MSH), the body's own pigment signal. It switches on melanocortin (a hormone system controlling pigment and appetite) receptors MC1R through MC5R (five docking sites on cells that respond to that signal) without choosing between them 3Source 3Melanocortin peptide therapeutics: historical milestones, clinical studies and commercializationHadley ME, Dorr RT · 2006.
The tanning effect runs through MC1R on melanocytes, the pigment-making cells in skin. Switching that receptor on raises cyclic AMP (a messenger chemical) inside the cell, and that rise is the signal that turns up tyrosinase and the other melanin-making enzymes, increasing eumelanin, the darker pigment. That receptor pathway was mapped in cultured human melanocytes using alpha-MSH itself rather than melanotan-2 5Source 5Participation of the melanocortin-1 receptor in the UV control of pigmentationSuzuki I, Im S, Tada A, Scott C, Akcali C, Davis MB, Barsh G, Hearing V, Abdel-Malek Z · 1999.
The effect on erection is documented directly in people: melanotan-2 produced erections without any sexual stimulation in 17 of 20 men with erectile dysfunction, which points to an action in the brain and spinal cord rather than on the penis itself 4Source 4Melanocortin receptor agonists, penile erection, and sexual motivation: human studies with Melanotan IIWessells H, Levine N, Hadley ME, Dorr R, Hruby V · 2000. The work locating which melanocortin receptors carry that signal, and the appetite-suppressing signal, was done in rats, not in people 3Source 3Melanocortin peptide therapeutics: historical milestones, clinical studies and commercializationHadley ME, Dorr RT · 2006.
The D-phenylalanine substitution (one swapped-in amino acid) this family of analogues (modified versions of a natural molecule) carries makes them resist being broken down by enzymes in blood, which is why they act longer than natural alpha-MSH. That was shown for the parent analogue in frog skin and mouse melanoma cells, not in humans 2Source 24-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activitySawyer TK, Sanfilippo PJ, Hruby VJ, Engel MH, Heward CB, Burnett JB, Hadley ME · 1980. How long melanotan-2 itself lasts in a person has never been measured: no human pharmacokinetic (how the body absorbs and clears a compound) study (a study of how a drug moves through the body and how fast it is cleared) has been published, and in mice, clearance from the blood after injection was rapid.