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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

  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. Melanoma Associated With the Use of Melanotan-Ii. Hjuler KF, Lorentzen HF. Dermatology (Basel, Switzerland). 2014;228(1):34-6. doi:10.1159/000356389.
  13. 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.
  14. 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.

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ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATIONAL AND EDUCATIONAL PURPOSES ONLY. The products offered on this website are furnished for in-vitro studies only. In-vitro studies (Latin: in glass) are performed outside of the body. These products are not medicines or drugs and have not been approved by the FDA to prevent, treat or cure any medical condition, ailment or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law.