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Melanotan 2 Spray — Alphagenics spray
Regenerative · Skin and Beauty

Melanotan 2 Spray

Melanotan II · MT-II

Cyclic α-MSH analog, non-selective melanocortin receptor agonist

Molecular weight1024.2 g/mol
CAS121062-08-6
Length7 amino acids
Available presentations
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About Melanotan 2 Spray

Melanotan II is a cyclic heptapeptide analog of alpha-melanocyte-stimulating hormone (α-MSH), designed at the University of Arizona.

It non-selectively activates several melanocortin receptors: MC1R, found on melanocytes and linked to skin pigmentation, and MC4R, found in the central nervous system and linked to sexual function and appetite. It was studied in small clinical trials for its effects on tanning and erection, and PT-141 (bremelanotide) was derived from it. It has no regulatory approval.

Quick guide · 5 key points

Melanotan 2 Spray: pigmentation and sexual function

Melanotan II is a cyclic analog of alpha-melanocyte-stimulating hormone (α-MSH), studied in small trials for its effects on tanning and erection. Here are five things the research shows.

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  1. 1

    An α-MSH analog that hits several receptors

    Melanotan II is a cyclic heptapeptide (lactam-bridged) derived from α-MSH. In laboratory studies, the melanocortin receptors MC1R, MC3R, MC4R and MC5R all recognize it, so it is considered non-selective. In mice, MC4R has been associated with erectile function. PT-141 (bremelanotide) was derived from melanotan II.1,4,2,3,9

    Melanotan IIStudied in small pigmentation and erection trials. No regulatory approval.
    PT-141 (bremelanotide)Derived from melanotan II. FDA-approved in 2019 (Vyleesi®) for hypoactive sexual desire disorder in premenopausal women.
    4Melanocortin receptors that recognize it in lab studies
  2. 2

    More skin pigmentation in a pilot study

    In a pilot phase I study in 3 healthy men, melanotan II (subcutaneous in the study, 5 low doses) has been associated with increased pigmentation of the face, upper body and buttocks in 2 of them.4

    2 of 3Volunteers with increased pigmentation measured by reflectance
  3. 3

    Erections in psychogenic erectile dysfunction

    In a double-blind, placebo-controlled crossover study in 10 men with psychogenic erectile dysfunction, melanotan II (subcutaneous in the study) has been associated with clinically apparent erections in 8 of them. Tip rigidity above 80% lasted a mean of 38 minutes versus 3 with placebo, measured by RigiScan®.5

    38 vs 3 minRigidity above 80%: melanotan II versus placebo
  4. 4

    Also with organic risk factors, plus more desire

    In another crossover study in 10 men with erectile dysfunction and organic risk factors, erections were reported after 12 of 19 injections, versus 1 of 21 with placebo, and sexual desire was significantly higher than with placebo.6

    12 of 19Injections followed by an erection, versus 1 of 21 with placebo
  5. 5

    Limited evidence and known safety signals

    Human data come from very small trials. In them, nausea (severe after 4 of 19 injections), yawning and spontaneous erections were observed. With unregulated use, changes in moles, new nevi and four cases of melanoma have been reported; a causal link has not been shown. It has no regulatory approval.4,5,6,7,8

    23Total participants across the three clinical trials cited
References
  1. Hruby VJ, et al. Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. J Med Chem. 1995;38(18):3454-61. PMID 7658432
  2. Van der Ploeg LH, et al. A role for the melanocortin 4 receptor in sexual function. Proc Natl Acad Sci USA. 2002;99(17):11381-6. PMID 12172010
  3. Hadley ME, Dorr RT. Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization. Peptides. 2006;27(4):921-30. PMID 16412534
  4. Dorr RT, et al. Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study. Life Sci. 1996;58(20):1777-84. PMID 8637402
  5. Wessells H, et al. Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo controlled crossover study. J Urol. 1998;160(2):389-93. PMID 9679884
  6. Wessells H, et al. Effect of an alpha-melanocyte stimulating hormone analog on penile erection and sexual desire in men with organic erectile dysfunction. Urology. 2000;56(4):641-6. PMID 11018622
  7. Habbema L, et al. Risks of unregulated use of alpha-melanocyte-stimulating hormone analogues: a review. Int J Dermatol. 2017;56(10):975-980. PMID 28266027
  8. Schulze F, et al. Eruptive naevi and darkening of pre-existing naevi 24 h after a single mono-dose injection of melanotan II. Eur J Dermatol. 2014;24(1):107-9. PMID 24334249
  9. U.S. Food and Drug Administration. Vyleesi (bremelanotide injection) prescribing information. NDA 210557, 2019. Official source

Structure and sequence

2D structure generated from PubChem CID 92432

Sequence

AcNlecyclo[Asp-His-D-Phe-Arg-Trp-Lys]NH2

Five findings from studies

Summary of results reported in the scientific literature. Each finding describes what was observed in the cited study, in its specific population and conditions; it does not constitute a therapeutic indication.

  1. Clinical study

    In a pilot phase I study in 3 healthy volunteers, subcutaneous melanotan II (5 low doses) has been associated with increased skin pigmentation measured by reflectance; mild nausea, yawning and spontaneous erections were also observed.

    Dorr RT et al. Life Sci. 1996;58:1777-1784 · PMID 8637402
  2. Clinical study

    In a double-blind, placebo-controlled crossover study in 10 men with psychogenic erectile dysfunction, 8 developed erections; mean duration of tip rigidity above 80% was 38 minutes versus 3 minutes with placebo.

    Wessells H et al. J Urol. 1998;160:389-393 · PMID 9679884
  3. Clinical study

    In 10 men with erectile dysfunction and organic risk factors, it has been associated with erections after 12 of 19 injections (versus 1 of 21 with placebo) and with greater sexual desire; 4 of 19 injections were followed by severe nausea.

    Wessells H et al. Urology. 2000;56:641-646 · PMID 11018622
  4. Review

    A review by its developers describes the clinical development of melanotan II for erectile dysfunction and its derivative PT-141, later studied for sexual function in men and women.

    Hadley ME, Dorr RT. Peptides. 2006;27:921-930 · PMID 16412534
  5. Review

    A review of published cases has described, with unregulated use of melanotan I and II, changes in existing moles, new nevi and four cases of melanoma; a causal link has not been shown.

    Habbema L et al. Int J Dermatol. 2017;56:975-980 · PMID 28266027

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