Product Overview
Melanotan II: Clinical Profile
Melanotan II (MT-II) is a synthetic cyclic heptapeptide analogue of α-melanocyte-stimulating hormone (α-MSH) that acts as a non-selective agonist at melanocortin receptors, primarily MC1R and MC4R. MT-II is used off-label for its ability to induce skin hyperpigmentation (tanning) and, less commonly, for its effects on sexual function and appetite suppression.[1][2][3][4]
Mechanism and Clinical Effects
- MT-II stimulates melanogenesis by activating MC1R on melanocytes, leading to increased eumelanin production and skin darkening.
- MT-II also activates MC4R, which is implicated in appetite suppression and sexual arousal. Spontaneous penile erections and increased sexual desire have been reported in both men and women following MT-II administration.[2][3]
- In rodent models, peripheral MT-II administration reduces food intake and body weight, with effects mediated by MC4R activation in circumventricular organs outside the blood-brain barrier. MT-II treatment in diet-induced obese rodents leads to generalized reduction in both visceral and subcutaneous adipose tissue.[5][6][7][8]
Safety Profile and Adverse Effects
- Common side effects include nausea, somnolence, fatigue, and stretching/yawning complexes. These effects are dose-dependent and typically mild, but can be more pronounced at higher doses.[1][9]
- Serious adverse events have been reported, including systemic toxicity, sympathomimetic excess, rhabdomyolysis, and acute renal dysfunction following supratherapeutic dosing.[10]
- MT-II use is associated with cutaneous complications, including rapid pigmentary changes in existing nevi, development of new (dysplastic) nevi, and, in rare cases, melanoma coinciding with use and sunbed exposure.[11][12]
- The unregulated nature of MT-II acquisition (often via internet sources) raises concerns about product contamination, transmission of infectious diseases, and polypharmacy.[9][11][13][14]
Regulatory and Clinical Considerations
- MT-II is not approved by regulatory agencies for any medical indication. Its use is unregulated and associated with significant safety concerns.[11][14]
- Afamelanotide, a related α-MSH analogue, is approved for specific photoprotection indications and has a more established safety profile.[11][14]
- Clinicians should be vigilant for unexpected skin pigmentation, rapid changes in pigmented lesions, and systemic symptoms in individuals who may be using MT-II, especially in populations engaged in tanning culture or fitness/bodybuilding.[9][11][12][13][14]
Summary
MT-II (10mg) is a potent melanocortin analogue that induces skin tanning, suppresses appetite, and enhances sexual arousal via MC1R and MC4R activation. Its use is associated with a range of adverse effects, including nausea, fatigue, pigmentary changes, and rare but serious systemic toxicity. The unregulated status and potential for contaminated products further increase risk. MT-II is not approved for clinical use, and clinicians should counsel patients regarding its hazards and monitor for cutaneous and systemic complications.[1][2][3][4][5][6][9][10][11][12][13][14][7][8]
References
- Evaluation of Melanotan-Ii, a Superpotent Cyclic Melanotropic Peptide in a Pilot Phase-I Clinical Study. Dorr RT, Lines R, Levine N, et al. Life Sciences. 1996;58(20):1777-84. doi:10.1016/0024-3205(96)00160-9.
- Melanocortin Peptide Therapeutics: Historical Milestones, Clinical Studies and Commercialization. Hadley ME, Dorr RT. Peptides. 2006;27(4):921-30. doi:10.1016/j.peptides.2005.01.029.
- Discovery That a Melanocortin Regulates Sexual Functions in Male and Female Humans. Hadley ME. Peptides. 2005;26(10):1687-9. doi:10.1016/j.peptides.2005.01.023.
- Journey Through the Spectacular Landscape of Melanocortin 1 Receptor. Upadhyay PR, Swope VB, Starner RJ, Koikov L, Abdel-Malek ZA. Pigment Cell & Melanoma Research. 2024;37(5):667-680. doi:10.1111/pcmr.13180.
- Exploring the Site of Anorectic Action of Peripherally Administered Synthetic Melanocortin Peptide MT-II in Rats. Trivedi P, Jiang M, Tamvakopoulos CC, et al. Brain Research. 2003;977(2):221-30. doi:10.1016/s0006-8993(03)02683-0.
- The Effects of the Melanocortin Agonist (MT-II) on Subcutaneous and Visceral Adipose Tissue in Rodents. Strader AD, Shi H, Ogawa R, Seeley RJ, Reizes O. The Journal of Pharmacology and Experimental Therapeutics. 2007;322(3):1153-61. doi:10.1124/jpet.107.123091.
- The Effect of the Melanocortin Agonist, MT-II, on the Defended Level of Body Adiposity. Seeley RJ, Burklow ML, Wilmer KA, et al. Endocrinology. 2005;146(9):3732-8. doi:10.1210/en.2004-1663.
- Activation of the Central Melanocortin System Chronically Reduces Body Mass Without the Necessity of Long-Term Caloric Restriction. Côté I, Sakarya Y, Kirichenko N, et al. Canadian Journal of Physiology and Pharmacology. 2017;95(2):206-214. doi:10.1139/cjpp-2016-0290.
- An in-Depth Case Examination of an Exotic Dancer's Experience of Melanotan. Van Hout MC, Brennan R. The International Journal on Drug Policy. 2014;25(3):444-50. doi:10.1016/j.drugpo.2013.10.008.
- Melanotan II Injection Resulting in Systemic Toxicity and Rhabdomyolysis. Nelson ME, Bryant SM, Aks SE. Clinical Toxicology (Philadelphia, Pa.). 2012;50(10):1169-73. doi:10.3109/15563650.2012.740637.
- Risks of Unregulated Use of Alpha-Melanocyte-Stimulating Hormone Analogues: A Review. Habbema L, Halk AB, Neumann M, Bergman W. International Journal of Dermatology. 2017;56(10):975-980. doi:10.1111/ijd.13585.
- Melanoma Associated With the Use of Melanotan-Ii. Hjuler KF, Lorentzen HF. Dermatology (Basel, Switzerland). 2014;228(1):34-6. doi:10.1159/000356389.
- Melanotan II User Experience: A Qualitative Study of Online Discussion Forums. Gilhooley E, Daly S, McKenna D. Dermatology (Basel, Switzerland). 2021;237(6):995-999. doi:10.1159/000514492.
- Melanotropic Peptides: More Than Just 'Barbie Drugs' and 'Sun-Tan Jabs'?. Langan EA, Nie Z, Rhodes LE. The British Journal of Dermatology. 2010;163(3):451-5. doi:10.1111/j.1365-2133.2010.09891.x.
All information provided is for research purposes only.
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All information provided is for research purposes only.
Storage & Handling (Research Use)
- Lyophilized powder: Store sealed at −20 °C to −80 °C (desiccated, light-protected). Short-term (≤2–3 weeks) at 2–8 °C is acceptable.
- After reconstitution: Store at 2–8 °C and use within 7 days, or aliquot and freeze at −20 °C to −80 °C for ≤3 months.
- Handling: Prepare small aliquots to avoid freeze–thaw; keep on ice during prep; minimize air/light exposure.
- Vehicle & pH: Reconstitute per lot guidance (e.g., sterile saline/BWFI) near pH 7.0–7.4; avoid reactive metals/oxidants.
- Labeling: Record concentration, solvent, and prep date; follow lab SOPs and lot-specific stability notes.
All information provided is for research purposes only.