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Melanotan I Peptide: Potential in Research

Melanotan I Peptide: Potential in Research

Studies suggest that Melanotan, which stands for the synthetic analog of α-MSH, is a hormone that may stimulate melanocyte production. The α-MSH is a hormone in the body that is one of many melanocortin peptides. Research suggests the melanocortin receptors 1, 3, 4, and 5 are bound by Melanotan.

The Melanotan family has two distinct molecular kinds: Melanotan I and Melanotan II. Melanin formation and skin tanning have been associated with these two factors. Although researchers highly seek after both Melanotan molecules, this review will emphasize Melanotan I.

Melanotan I: Mechanism of Action

The synthetic peptide Melanotan I has a linear structure with the molecular formula [Nle-D-Phe]-α-MSH. It has the same structure as α-MSH except for two important distinctions and is thirteen amino acids long. First, norleucine is the fourth amino acid in melanotan I, and second, D-phenylalanine is the seventh amino acid.

Research suggests Melanotan I may be more powerful and resistant to breakdown than α-MSH in the body, and it might mainly connect with the MC1R receptor. Data suggests that MT-1 may improve melanin production and lessen the severity of UV radiation.

Melanotan I and Melanotan II (Ac-Nle-[Asp-His-D-Phe-Arg-Trp-Lys]- α-MSH-NH2) are indistinguishable. Investigations purport that Melanotan II may be more effective than MT-1 in increasing libido and decreasing hunger hormone signaling.

Melanotan I Peptide Research

The following theorized properties of Melanotan I have been derived from the many studies assessing its potential and impact.

Melanotan I Peptide and Melanin

Findings imply that when Melanotan I binds to the MC1R, it may stimulate the production of melanin. As a byproduct, this might cause melanocyte and tyrosinase levels to rise. Research has purported that MT-1 may decrease the amount of sunburnt cells and speed up the skin pigmentation process.

Two different concentrations of Melanotan I were studied in three phase I clinical studies by dermatological clinics at the Arizona Health Sciences Center. The trials compared applying tiny amounts of UV-B to the neck or buttocks or applying full sunlight to half of the back. Melanotan I trial research models appeared to show “significantly enhanced tanning” on their backs and 47% fewer sunburn cells on their necks than the control group.

Melanotan I Peptide and Behavior

Photodynamic therapy (PDT) uses light and photosensitization to kill cancer cells. As results of multiple phase II clinical experiments sponsored by Clinuvel Pharmaceuticals suggest, Melanotan I may offer psychological properties.

Melanotan I implants, also known as afamelanotide implants, were the subject of a phase II, multicenter, double-blind, placebo-controlled pilot trial in 2008 that sought to determine if they may lessen the duration of phototoxicity that research models undergoing photodynamic treatment with porfimer sodium would suffer.

The findings hinted that Melanotan I was associated with heightened positive behavior compared to a placebo in a trial of 16 research models (9 presented with MT-1 and 7 given a placebo). Scientists speculate it is possible that these alterations occurred as a side consequence of lessened pain.

Melanotan I and Skin

Acne vulgaris has been studied as a possible option for Melanotan I. Research models with mild to severe acne vulgaris were the subjects of a phase II randomized trial in Germany that examined the potential and effectiveness of two concentration regimens of bioresorbable afamelanotide implants in 2011.

Melanotan I seemed to reduce the number of inflammatory acne lesions on the faces of research models who received the substance (three presentations every three weeks or two every four weeks). Melanotan I research models displayed pain-free sun exposure for up to seven times longer than those who received a placebo, and researchers discovered an overall improvement in the models’ quality of life as evaluated by DLQI from day 0 to day 56.

Melanotan I Peptide and Xeroderma Pigmentosum 

Xeroderma pigmentosum (XP) is a hereditary condition characterized by severe photosensitivity; Melanotan I has been studied as a potential adjuvant for XP. The purpose of the 2019 German proof-of-concept, phase IIa open-label trial was to assess the effectiveness and potential of Melanotan I in research models with XP. T

Melanotan I Peptide and Polymorphic Light Eruption

In 2010, researchers in Germany, the Netherlands, and Belgium conducted a phase III study to assess the potential and effectiveness of Melanotan I for research models of polymorphic light eruption (PLE). In this skin condition, a rash appears after being exposed to sunlight. The study was randomized, double-blind, placebo-controlled, and conducted in parallel groups.

Presenting Melanotan I over four months seemed to alleviate PLE-related pruritus, as suggested by the study’s authors.

Melanotan I Peptide and Erythropoietic Protoporphyria 

Melanotan I was the subject of a European study  in 2011 that sought to validate their potential and effectiveness in the context of erythropoietic protoporphyria (EPP). Researchers speculated that compared to the placebo group, those exposed to Melanotan I displayed less pain perception.

Researchers interested in further studying Melanotan I peptide may visit corepeptides.com.

References

[i] Mahiques-Santos L. Melanotan [Melanotan]. Actas Dermosifiliogr. 2012 May;103(4):257-9. Spanish. doi: 10.1016/j.ad.2011.08.002. Epub 2011 Nov 1. PMID: 22051769.

[ii] Hadley ME, Dorr RT. Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization. Peptides. 2006 Apr;27(4):921-30. doi: 10.1016/j.peptides.2005.01.029. Epub 2006 Jan 18. PMID: 16412534.

[iii] Dorr RT, Dvorakova K, Brooks C, Lines R, Levine N, Schram K, Miketova P, Hruby V, Alberts DS. Increased eumelanin expression and tanning is induced by a superpotent melanotropin [Nle4-D-Phe7]-alpha-MSH in humans. Photochem Photobiol. 2000 Oct;72(4):526-32. doi: 10.1562/0031-8655(2000)072<0526:ieeati>2.0.co;2. PMID: 11045725.

[iv] Dorr RT, Ertl G, Levine N, Brooks C, Bangert JL, Powell MB, Humphrey S, Alberts DS. Effects of a superpotent melanotropic peptide in combination with solar UV radiation on tanning of the skin in human volunteers. Arch Dermatol. 2004 Jul;140(7):827-35. doi: 10.1001/archderm.140.7.827. PMID: 15262693.

[v] Wikberg JE, Muceniece R, Mandrika I, Prusis P, Lindblom J, Post C, Skottner A. New aspects on the melanocortins and their receptors. Pharmacol Res. 2000 Nov;42(5):393-420. doi: 10.1006/phrs.2000.0725. PMID: 11023702.

[vi] Ryakhovsky VV, Khachiyan GA, Kosovova NF, Isamiddinova EF, Ivanov AS. The first preparative solution phase synthesis of melanotan II. Beilstein J Org Chem. 2008;4:39. doi: 10.3762/bjoc.4.39. Epub 2008 Oct 30. PMID: 19043625; PMCID: PMC2587946.

[vii] Ugwu SO, Blanchard J, Dorr RT, Levine N, Brooks C, Hadley ME, Aickin M, Hruby VJ. Skin pigmentation and pharmacokinetics of melanotan-I in humans. Biopharm Drug Dispos. 1997 Apr;18(3):259-69. doi: 10.1002/(sici)1099-081x(199704)18:3<259::aid-bdd20>3.0.co;2-x. PMID: 9113347.

[viii] A Phase II, Multicentre, Double-blind, Placebo Controlled, Pilot Study to Evaluate the Safety and Efficacy of CUV1647 Administered as A Subcutaneous Bioresorbable 16mg Implant in Patients Undergoing Photodynamic Therapy (PDT) utilising Porfimer Sodium – Results. (2020). 

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