MT2

What is melanotan II?

Melanotan II is an unlicensed and largely untested form of alpha-melanocyte-stimulating hormone, which causes pigmentation (tanning) of human skin. Melanotan II is a variant of melanotan I (afamelanotide), a drug used in the treatment of erythropoietic protoporphyria.

Melanotan II is not approved for the treatment of any medical conditions currently. It has been reported to cause a wide range of potentially serious side effects. Warnings against its use have been issued from the US, UK and several other countries.

How does melanotan II work?

Melanotan II non-selectively mimics the action of melanocortin peptides. These are natural hormones involved with pigmentation, energy homeostasis, sexual functioning, the immune system, inflammation, and the cardiovascular system. Much like melanotan I (afamelanotide), melanotan II stimulates the production of eumelanin, causing the skin to go darker (tanning).

Melanotan II is usually administered as an injection of liquid underneath the skin, commonly every second day. Trials have shown that the tanning effect can occur within 5 doses.

Side effects of melanotan II

Short term side effects after administration include:

        Facial flushing

        Reduced appetite, nausea and vomiting

        In males, spontaneous erections 1-5 hours after administration (priapism), associated with yawning and stretching complex

Long term, there is concern that melanotan II may increase the risk of:

        Melanoma – a potentially serious form of skin cancer

        Deepening of the colour of moles, new molesand atypical melanocytic naevi

        Melanonychia – brown to black discolouration of one or more nails

        Rhabdomyolysis – potentially fatal destruction of muscle cells

        Encephalopathy syndrome

There is also concern about possible side effects due to contamination or lack of sterility if melanotan II is prepared incorrectly or needles are shared.

Sexual dysfunction

During clinic trials for its use as a tanning agent, melanotan II was found to be a potent stimulator of male erections. A new drug based on melanotan II, bremelanotide, was developed to take advantage of this property. It has been noted across several studies to increase rigidity and duration of male erection, as well as male sexual desire. It has also been shown to increase female sexual desire in patients with sexual arousal disorder.

Drug interactions with melanotan II

No specific drug interactions have not been identified with melanotan II.

Safety measures

Melanotan II has not been fully tested, and due to its potential side effects it is not recommended that anybody use this drug.

No evidence exists for the use of melatonin II in pregnancy or breast feeding but it is recommended that it should be avoided.

Melanotan II

Melanotan II is a synthetic variant of the naturally occurring peptide hormone alpha-melanocyte stimulating hormone (α-MSH)1, which acts to stimulate the production of melanin in the skin – the molecule responsible for hair and skin pigmentation – through a process called melanogenesis2. Naturally occurring α-MSH has also been shown to play a role in feeding, the maintenance of useable and stored energy, and sexual activity through its action as an agonist of melanocortin receptors MC1, MC3, and MC4; MC1 being responsible for skin pigmentation effects, and MC3 and MC4 being responsible for effects on appetite, metabolism, and sexual activity3.Melanotan II is a cyclic heptapeptide originally developed as a defense against the potential cancer-causing effects of the sun’s ultraviolet radiation through its action of stimulating natural melanin production in the absence of sunlight4, which allows for the sunless darkening of skin tone.In addition to its promotion of skin tanning, Melanotan II has been shown to be a lipolytic (fat cell-destroying) agent5, a suppressant of appetite6, and a stimulant of libido in animal test subjects7. Melanotan II has demonstrated great efficacy in reducing caloric intake, while eliminating cholesterol and fat stores in obese mice through its targeted metabolic action8.

Product Comparison – Melanotan II

Melanotan II and Melatonan I, both synthetic analogues of α-MSH, produce similar effects in terms of skin tanning by binding the MC1 receptor9, though Melanotan II is unique in this family of agents in that it stimulates an aphrodisiac effect (MC3 and MC4), improving libido significantly in test subjects.

PT-141 is structurally similar to the biosynthetic peptide hormone Melanotan II, but has shown to be a potent binding agent of MC3 and MC4 only, showing no affinity for MC1. In animal tests, PT-141 has proven quite effective at correcting sexual dysfunction7, while Melanotan II induces an additional effect on skin tone.

Unlike other agents that have an effect on erectile response, Melanotan II performs no action on the vascular system, but rather induces arousal and heightens sexual desire via the nervous system – binding important receptors in the brain10.

Research products only, they are not for human consumption.

Synonyms:

Melanotan 2; Melanotan-2; MT-2; MT-II; Melanotide; Tanexin

Peer-Reviewed Sources:

1. Dorr, R. T., Lines, R., Levine, N., Brooks, C., Xiang, L., Hruby, V. J., & Hadley, M. E. (1996). Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study. Life sciences, 58(20), 1777-1784.

2. Hadley, M. E., Hruby, V. J., Blanchard, J., Dorr, R. T., Levine, N., Dawson, B. V., & Sawyer, T. K. (1998). Discovery and development of novel melanogenic drugs. In Integration of Pharmaceutical Discovery and Development (pp. 575-595). Springer US.

3. King, S.H.; 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.

4. Pawelek, J. M. (2001). Approaches to increasing skin melanin with MSH analogs and synthetic melanins. Pigment cell research, 14(3), 155-160. ↩︎

5. Brito, M. N., Brito, N. A., Baro, D. J., Song, C. K., & Bartness, T. J. (2007). Differential activation of the sympathetic innervation of adipose tissues by melanocortin receptor stimulation. Endocrinology, 148(11), 5339-5347.

6. Vergoni, A. V., & Bertolini, A. (2000). Role of melanocortins in the central control of feeding. European journal of pharmacology, 405(1), 25-32. ↩︎

7. Allard, J., & Giuliano, F. (2001). Central nervous system agents in the treatment of erectile dysfunction: how do they work?. Current urology reports, 2(6), 488-494.

8. Chen, A. S., Metzger, J. M., Trumbauer, M. E., Guan, X. M., Yu, H., Frazier, E. G., & Van der Ploeg, L. H. (2000). Role of the melanocortin-4 receptor in metabolic rate and food intake in mice. Transgenic research, 9(2), 145-154.

9. Schiöth, H. B., Muceniece, R., Mutulis, F., Prusis, P., Lindeberg, G., Sharma, S. D., & Wikberg, J. E. (1997). Selectivity of cyclic [D-Nal 7] and [D-Phe 7] substituted MSH analogues for the melanocortin receptor subtypes. Peptides,18(7), 1009-1013.

10. Wessells, H., Fuciarelli, K., Hansen, J., Hadley, M. E., Hruby, V. J., Dorr, R., & Levine, N. (1998). Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo controlled crossover study. The Journal of urology, 160(2), 389-393.

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