Modimelanotide

Sexual & Body Composition

Also known as: Melanocortin Agonist Peptide, Modified Melanotan

Melanocortin PeptidesResearch phase: Preclinical/early clinicalRegulatory: Not approved by any regulatory agency. Research peptide. Limited published data under this specific name. Related compounds (MT-II, bremelanotide) provide class context.

Mechanism

Modimelanotide is a research melanocortin receptor agonist in the same peptide family as Melanotan II and PT-141 (bremelanotide). Melanocortin peptides activate MC1R-MC5R receptors, with effects ranging from skin tanning (MC1R), sexual arousal (MC3R/MC4R), appetite suppression (MC4R), to anti-inflammatory effects (MC1R/MC3R). Modimelanotide is designed with modifications to improve receptor selectivity and reduce the side effects (nausea, flushing) associated with less selective melanocortins like MT-2.

Technical detail

Modimelanotide is a synthetic cyclic peptide analog of alpha-MSH targeting melanocortin receptors (MCRs). The melanocortin system comprises five G-protein coupled receptors (MC1R-MC5R) with diverse physiological roles: MC1R (pigmentation, anti-inflammation), MC2R (adrenal ACTH receptor), MC3R (energy homeostasis, sexual function), MC4R (appetite, energy expenditure, erectile function), MC5R (sebaceous gland function). Modimelanotide is designed for improved selectivity at MC1R and/or MC4R over the broad-spectrum agonism of earlier compounds (α-MSH, MT-II). Melanocortin agonism at MC1R: activates Gs/cAMP/PKA pathway in melanocytes, upregulating tyrosinase and melanin production; at MC4R in hypothalamic PVN: activates satiety circuits and descending autonomic pathways involved in penile erection (via sacral parasympathetic outflow). Structural modifications aim to reduce MC3R/MC5R-mediated side effects.

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