Melanotan 1, Afamelanotide, or just Melanotan as is it is commonly referred is a synthetic peptide t...

1. Understanding Melanotan 1 or Melanotan
Melanotan 1, Afamelanotide, or just Melanotan as is it is commonly referred is a synthetic peptide
that is an analog to alpha melanocytes stimulating hormone. Alpha melanocytes stimulating hormone
or a-MSH is a naturally produced hormone by the body, the hormone is responsible for
melanogenesis, or the formation of melanin a pigment that is important for skin tanning. Alpha MSH
activates specific melanocortin receptors, which in turn contributes to melanogenesis, the hormone
is also influential in accentuating appetite, lipid metabolism, and sexual libido through the receptors.
PT-141 and Melanotan 2 have been studied for a potential remedy for sexual dysfunction, Melanotan
is extensively researched for skin protection against ultraviolet properties because of melanogenesis
stimulating properties. Melanotan 2 and Melanotan are analogs of the peptide alpha-MSH, which
induces skin tanning. Melanotan 2 has shown effects of increasing libido, and has aphrodisiac
properties. Melanotan is a non-selective agonist of the melanocortin receptors MC3-5R and MC1R.
The mechanism and principle of action is through mimicking of the natural body tanning process.
The first created peptide of Melanotan was produced at the University of Arizona. During their
scientific research on the development of a mechanism to fight melanoma, the scientists focused on
the production of melanin though the natural process which in turn would alleviate the chances of
developing skin cancer as it protects the skin against harmful ultraviolet radiation. The production of
Melanotan with a better half life prompted the scientists to develop a peptide sequence, which
included Nle4, D-Phe7-a-MSH, this was a thousand times more potent than the natural a-MSH. The
peptide was first named Melanotan and later renamed Melanotan 1. Melanotan gives a photo
protective effect on the skin by triggering the signal cascade through the activation of the MC1R on
the cells that produce melanin or melanocytes. When MGF C-Terminal binds to MC1R on the
melanocytes or cells producing melanin the epidermis layer of the skin begins a series of reactions
and actions that result in the production of eumelanin a brown/black photo protective pigment.
The binding of MC1R leads to the activation of adenylate cyclase or AC and the stimulation of
adenine monophosphate cAMP. The cyclic adenosine monophosphate activates protein kinase A or
PKA causes phosphorylation or addition of phosphate group to the cAMP response-binding element

2. CREB. Phosphorylated CREB binds to cAMP response element CRE on the MITF or microphtalmia-
associated transcription factor gene that in turn leads to the biosynthesis of the MITF protein.
Microphtalmia associated transcription factor gene is capable of activating other several genes
which include the MC1R gene which is vital in melanogenesis. The initiation of melanogenesis is
essential in increasing the levels of melanogenic enzymes within melanocytes. The level of the
enzymes plays a crucial role in determining whether the cells will form eumelanin or pheomelanin.
The production of eumelanin instead of pheomelanin by the skin cells increases the pigmentation of
the skin, this pigmentation is essential in protecting the skin against harmful ultraviolet radiation.
Other studies show that Melanotan is vital in treating of erythropoietic photoporphyria, which is
intolerance to light, continuous research will give more insight on the use of the hormone in
alleviating cancer problems.