Melanotan 1: Melanin production and tanning

Studies suggest Melanotan 1 is an agonist of melanocortin receptors 1, 3, 4, and 5 and a synthetic peptide called MT-1. It is considered to be similar to alpha-melanotocyte stimulating hormone. MT-1's potential to connect to melanocortin receptor 1 is believed to increase melanin production.

The peptide has been studied in animal models of erythropoietic protoporphyria, and in the context of erectile dysfunction, rosacea, vitiligo, and skin tanning. However, it is most typically studied in relation to the skin cells and melanin-synthesis.

Melanotan 1 Peptide: Mechanism of Action

One speculated function is activating melanogenesis. Melanotan 1 (MT1) is a synthetic version of alpha-melanocyte-stimulating hormone (α-MSH). Alpha MSH is also recognised for potentially influencing hunger and libido.

Test models are thought to have enhanced melanin synthesis and tanning as a result of Melanotan 1 binding to melanocortin receptors 1, 3, 4, and 5 (MC1R, MC3R, MC4R, MC5R)

Like natural α-MSH, Melanotan 1 is composed of 13 amino acids and has a linear structure. In contrast to α-MSH, MT1 has D-phenylalanine as its seventh amino acid and norleucine as its fourth. The modified version of MT1 outperforms natural α-MSH regarding potency and breakdown resistance.

Even though Melanotan 1 is the main topic of this guide, researchers should be aware that Melanotan 2 (MT2) also exists and has been examined for its potential on melanin synthesis, libido, hunger, and sexual desire.

Melanotan 1 Peptide Potential

Here, we shall review the key potential impacts of Melanotan 1, as suggested in these studies, which have attracted much scientific attention.

Melanotan 1 Peptide: Tanning and Melanin Synthesis

Tyrosinase, melanocytes, and melanin are all the melanocortin 1 receptor (MC1R) components, which MT1 has been speculated to bind to. Studies suggest that Melanotan 1 may potentially speed up the tanning process and reduce the occurrence of sunburnt cells in animal research models. It is also hypothesised to influence the pace of melanin formation.

Three preliminary experimental studies performed by researchers at the Arizona Health Sciences Center suggested that MT1 exposed animal models exhibited tanned backs more easily than the control group and that small concentrations of UV-B light reduced sunburn on the necks by 47%.

Melanotan 1 Peptide: Hormone Regulation and Mood

Research data suggests that Melanotan I may potentially exert psychological impacts, as suggested by research within the context of various illnesses.

Compared to a control compound, Melanotan 1 appeared to have enhanced mood and related behavioral exhibitions in the phase II experimental study, including animal models exposed to photodynamic treatment (PDT). These animal models have been hypothesised to be aided by MT1 as a post-PDT exposure.

Research models of porfimer sodium photodynamic procedures have also been studied following exposure to Melanotan 1. Research models of Melanotan 1 implants appeared to exhibit psychological impacts, including better moods, as suggested by phase II multicenter, double-blind, placebo-controlled pilot research conducted in 2008.

A subsequent experiment attempted to assess the potential of Melanotan I, but the data is not yet available. Researchers now have several avenues to explore MT1-related impacts.

Melanotan 1 Peptide and Acne Vulgaris

At least one phase 2 experiment has looked at Melanotan 1 for the context of acne vulgaris.

Melanotan 1 concentrations were evaluated in one phase II randomised experiment in 2011 at three-week or twice at one-month intervals. According to German research, Melanotan 1 seemed to have improved DLQI levels and reduced the number of inflammatory acne lesions. The results of a subsequent study are not yet available.

Melanotan 1 Peptide and Light Sensitivity Disorders

The peptide has also been evaluated for its potential impact in research within the field of light sensitivity illnesses, including:

●      An uncommon skin disorder known as Xeroderma pigmentosum (XP) that induces increased sensitivity to UV rays;

●      Rash outbreaks following sunlight exposure, known as polymorphic light eruption (PLE); and,

●      The condition is known as erythropoietic protoplasmosis (EPP).

Phase II experimental studies have purported that Melanotan I may offer potential as an approach for various disorders, and research into MT1 is still underway.

For instance, a German proof-of-concept, phase IIa open-label research in 2019 sought to examine MT1's potential for XP. The positive profile of Melanotan was suggested in a follow-up experiment.

According to a 2010 European phase III randomised, double-blind, placebo-controlled, parallel-group trial, MT1 seemed to have mitigated the severity of PLE when routinely exposed to the peptide over four months.

Finally, a European experiment conducted in 2011 indicated that MT1 may have reduced pain in EPP models compared to a control group.

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References   

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[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.

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[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) utilizing Porfimer Sodium – Results. (2020).