Substance class
Melanocortin
3 entries
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PT-141
Bremelanotid
PT-141 (bremelanotide) is a synthetic cyclic heptapeptide and an agonist at melanocortin receptors, particularly MC3R and MC4R. It is a metabolite of Melanotan II but contains no acetyl group at the N-terminus. Unlike peripheral vasodilators (e.g. PDE-5 inhibitors), PT-141 acts primarily centrally via the hypothalamus and other CNS areas involved in regulating sexual desire. MC4R activation in the hypothalamus is postulated as the main mechanism of its pro-sexual effect.
Melanotan II
MT-2
Melanotan II is a synthetic cyclic heptapeptide and a non-selective agonist at melanocortin receptors (MC1R, MC3R, MC4R, MC5R). Activation of MC1R in melanocytes stimulates melanin synthesis, leading to increased skin pigmentation. MC4R activation in the hypothalamus is associated with effects on sexual desire and erectile mechanisms. Unlike PT-141 (bremelanotide, a metabolite), Melanotan II has broader receptor selectivity and an additional N-terminal acetylation, resulting in a different side-effect profile.
Melanotan I
Melanotan-1
Melanotan I is a linear analog of α-melanocyte-stimulating hormone (α-MSH) with increased stability through the Nle4 and D-Phe7 substitutions. It binds predominantly to the melanocortin-1 receptor (MC1R) on melanocytes and stimulates the formation of eumelanin. This enhances skin pigmentation, which is used for photoprotection in a medical context. Unlike Melanotan II, its affinity for other melanocortin receptors is lower.