Melanotan II 10mg

Melanotan II (MT-II)

Description

Melanotan II (MT-II) is a synthetic analog of the endogenous melanocortin peptide hormone α-melanocyte-stimulating hormone (α-MSH). It was originally developed to study the biological actions of melanocortin receptor activation, particularly in relation to pigmentation, energy metabolism, and sexual function. MT-II exhibits affinity for several melanocortin receptor subtypes, including MC1R, MC3R, MC4R, and MC5R, where it may modulate pigmentation, inflammation, and energy balance. (1)(2)Melanotan II is a cyclic heptapeptide designed to mimic α-MSH’s binding profile while improving stability and resistance to enzymatic degradation. It has been studied in both preclinical and clinical contexts for its potential to induce melanogenesis and influence hypothalamic neuropeptide signaling related to appetite and sexual behavior. (3)

Overview

Melanotan II’s primary mechanism of action appears to be activation of melanocortin receptors (MCRs), particularly MC1R in melanocytes, leading to increased synthesis of eumelanin via upregulation of tyrosinase and related enzymes. Activation of MC4R and MC3R receptors in the central nervous system has been associated with effects on energy homeostasis and sexual arousal pathways. (4)(5)Melanotan II has also been observed to exhibit anti-inflammatory and antioxidant activity in vitro, potentially mediated by the modulation of cytokine signaling and nitric oxide pathways. Because of its broad receptor binding profile, MT-II has been investigated across several domains of physiology, including pigmentation, sexual function, appetite, and energy metabolism.

Chemical Characteristics

Synonyms: MT-II, Melanotan-2, Melanocortin Analog, Afamelanotide (parent analog)

Research and Clinical Studies

Melanotan II and Pigmentation

The pigmentation-inducing potential of Melanotan II was first demonstrated in studies where the peptide significantly increased eumelanin synthesis and tanning response in humans. In a double-blind, placebo-controlled trial, daily subcutaneous administration of MT-II (0.025 mg/kg) resulted in increased melanin density and visible skin darkening compared to placebo, independent of UV exposure. (6) The peptide’s action on MC1R receptors in melanocytes is believed to upregulate melanin production while providing potential photoprotective effects against UV-induced DNA damage. (7)

Melanotan II and Sexual Function

Preclinical research has indicated that MT-II can activate MC4R receptors in the hypothalamus, which may influence libido and sexual arousal. A small clinical trial in male subjects with erectile dysfunction suggested that MT-II administration induced spontaneous erections within hours, apparently independent of sexual stimuli. (8) This action was likely mediated via central melanocortin receptor pathways involved in sexual behavior and reward processing. (9)

Melanotan II and Energy Metabolism

Studies on rodent models indicate that MT-II may reduce food intake and increase energy expenditure through hypothalamic activation of MC3R and MC4R receptors. These findings are consistent with the role of melanocortin signaling in appetite suppression and energy balance regulation. (10) However, chronic exposure may result in receptor desensitization, and long-term metabolic effects remain under investigation.

Melanotan II and Inflammatory Response

Research suggests that melanocortin analogs, including MT-II, can modulate immune response pathways. In animal models of sepsis and inflammation, MT-II reduced pro-inflammatory cytokine levels and oxidative stress biomarkers, suggesting a possible protective effect via melanocortin-mediated signaling cascades. (11)

Melanotan II — References

• Hadley, M. E., Hruby, V. J. Discovery and development of melanocortin receptor agonists: melanotan-I and -II. Annals of the New York Academy of Sciences. 1998;839:366–373.https://doi.org/10.1111/j.1749-6632.1998.tb10779.x
• Dorr, R. T., Dvorakova, K., Brooks, C., Lines, R., Levine, N., Hadley, M. E., Hruby, V. J. Phase I and II clinical trials with melanotan-II, a superpotent melanotropic peptide. Annals of the New York Academy of Sciences. 1993;680:539–541.https://doi.org/10.1111/j.1749-6632.1993.tb19798.x
• Hadley, M. E., Hruby, V. J. Melanocortin receptor ligands and their therapeutic potential. Expert Opinion on Investigational Drugs. 2000;9(12):2649–2657.https://doi.org/10.1517/13543784.9.12.2649
• Wessells, H., Fuciarelli, K., Hansen, J., Hadley, M. E., Hruby, V. J., Dorr, R., Levine, N. Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo-controlled crossover study. Urology. 2000;56(4):641–646.https://doi.org/10.1016/S0090-4295(00)00692-4
• Levine, N., Stake, J., Brown, D., Robinson, D., Dorr, R., Hadley, M. E., Hruby, V. J. Randomized, double-blind, controlled trial of melanotan II in men with erectile dysfunction. Archives of Sexual Behavior. 2003;32(6):511–518.https://doi.org/10.1023/A:1026063420467
• Dhillo, W. S., Chaudhri, O. B., Patterson, M., Thompson, E. L., Murphy, K. G., Badman, M. K., Ghatei, M. A., Bloom, S. R. The effects of the melanocortin agonist melanotan II on appetite and food intake in humans. Journal of Clinical Endocrinology & Metabolism. 2004;89(1):54–59.https://doi.org/10.1210/jc.2003-031279
• Shadiack, A. M., Sharma, S. D., Earle, D. C., Spana, C., Hall, J. M. Melanocortins in erectile function. Annals of the New York Academy of Sciences. 2003;994:90–105.https://doi.org/10.1111/j.1749-6632.2003.tb03165.x
• MacNeil, D. J. The role of melanocortins in appetite regulation, sexual function, and tanning. Molecular Genetics and Metabolism. 2001;74(1–2):133–146.https://doi.org/10.1006/mgme.2001.3220

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