Melanotan II is a synthetic analogue of the peptide hormone α-melanocyte-stimulating hormone (α-MSH).
It was under development as drug candidate for female sexual dysfunction and erectile dysfunction but clinical development ceased by 2003, and as of 2018, no product containing melanotan II was marketed and all commercial development had ceased. Unlicensed, untested, or fraudulent products sold as “melanotan II” are found on the Internet, and purported to be effective as “tanning drugs”, though side effects such as uneven pigmentation, new nevi (moles), and darkening or enlargement of existing moles are common and have led to medical authorities discouraging use.
Melanotan II acts as a non-selective agonist of the melanocortin receptors MC1, MC3, MC4, and MC5.
To the extent that melanotan II produces melanogenesis, this is thought to be caused by activation of the MC1 receptor, whereas its clinically documented sexual effects are thought to be related to its ability to activate the MC4 receptor (though the MC3 is thought to possibly also be involved).
Other effects of melanotan II, mostly regarded as adverse effects, include flushing, nausea, vomiting, stretching, yawning, and loss of appetite (the last via activation of MC4).
“Melanotan II”. AdisInsight. Retrieved 13 Jan 2018.
- Brennan R, Wells JS, Van Hout MC (September 2017). “The injecting use of image and performance-enhancing drugs (IPED) in the general population: a systematic review”. Health & Social Care in the Community. 25 (5): 1459–1531. doi:10.1111/hsc.12326. PMID 26806443.
- Habbema L, Halk AB, Neumann M, Bergman W (October 2017). “Risks of unregulated use of alpha-melanocyte-stimulating hormone analogues: a review”. International Journal of Dermatology. 56 (10): 975–980. doi:10.1111/ijd.13585. PMID 28266027.
- Wikberg JE (2001). “Melanocortin receptors: new opportunities in drug discovery”. Expert Opinion on Therapeutic Patents. 11 (1): 61–76. doi:10.1517/13543718.104.22.168. ISSN 1354-3776.
- Norris DO, Lopez KH (25 November 2010). Hormones and Reproduction of Vertebrates. Academic Press. pp. 4–. ISBN 978-0-08-095809-5.
- King SH, Mayorov AV, Balse-Srinivasan P, Hruby VJ, Vanderah TW, Wessells H (2007). “Melanocortin receptors, melanotropic peptides and penile erection”. Curr Top Med Chem. 7 (11): 1098–1106. doi:10.2174/1568026610707011111. PMC 2694735. PMID 17584130.