Description
Melanotan 1 (also known as afamelanotide) is a synthetic 13-amino-acid peptide and an analog of natural alpha-melanocyte-stimulating hormone (alpha-MSH). Structurally, melanotan 1 differs from native alpha-MSH through two amino acid substitutions that make the compound more resistant to enzymatic degradation and extend its half-life.
The central research mechanism lies in the activation of the melanocortin-1 receptor (MC1R) on melanocytes. Activation leads to increased tyrosinase activity and thus enhanced eumelanin synthesis. In preclinical studies, melanotan 1 has been associated with dose- and time-dependent effects on skin pigmentation. The research data is substantial as the compound has also been used in dermatological research on erythropoietic protoporphyria.
Compared to melanotan 2, melanotan 1 is substantially more selective for MC1R, while melanotan 2 activates multiple melanocortin receptor subtypes. This selectivity makes melanotan 1 a clearer research tool when isolated investigation of the pigmentation pathway is the goal, without the additional effects on MC3R/MC4R that occur with melanotan 2.
With a half-life of approximately 30 minutes, melanotan 1 is short, requiring frequent application intervals in preclinical setups. In dermatological research, implant formulations are also used that enable continuous release over weeks.
Melanotan 1 is available in 10mg vials as 10-vial packs.
This information is for research and educational purposes only. No medical recommendations.
Risks & Safety
Melanotan 1 is comparatively well documented through its use as afamelanotide in dermatological research and, due to its MC1R selectivity, is considered the milder profile compared to melanotan 2.
Observed in research and user reports:
- Nausea: nausea and mild malaise shortly after application are among the more frequently reported observations.
- Flushing: facial flushing and transient warmth are described in the literature.
- Pigment changes: MC1R activation can lead to darkening of moles, freckles and existing pigmented areas. A change in moles is considered observation-relevant.
- Injection site: redness or pressure at the injection site is among the common observations.
- No long-term data: robust human studies on longer-term non-clinical use exist only to a limited extent. The profile rests on dermatological study data and anecdotal experience.
This classification does not replace medical advice. Risk and responsibility for any actual use lie entirely with the buyer.
Studies
- Afamelanotide for the treatment of erythropoietic protoporphyria - NEJM 2015: Clinical research data.
- 4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity - PNAS 1980: First description of the analogue with norleucine at position 4 and D-phenylalanine at position 7: resistant to degradation by serum enzymes and 26 times as potent as alpha-MSH in the adenylate cyclase assay.
- Effects of a superpotent melanotropic peptide in combination with solar UV radiation on tanning of the skin in human volunteers - Archives of Dermatology 2004: Three phase 1 trials of melanotan-1 combined with UV-B or sunlight: enhanced tanning that lasted at least 3 weeks longer than in controls, with nausea and transient facial flushing as side effects.
- Pharmacokinetics and Pharmacodynamics of Afamelanotide and its Clinical Use in Treating Dermatologic Disorders - Clinical Pharmacokinetics 2017: Review of the pharmacokinetics and pharmacodynamics of afamelanotide: it binds the MC1 receptor and is fully bioavailable subcutaneously, whereas oral and transdermal administration produced no measurable plasma levels.
