Features
Afamelanotide is a potent, linear synthetic analog of the naturally occurring peptide hormone α-melanocyte-stimulating hormone (α-MSH).Modified to have a stronger binding affinity to melanocortin- 1 receptor (MC1R) and a smaller disassociation constant, afamelanotide has a longer half-life and subsequently exerts longer pharmacologic activity than its parent hormone.
Uses
Melanotan 1 is a highly potent melanotropin with extended biological activity and resistance to enzymatic degredation by serum enzymes. [Nle4, D-Phe7]-α-Melanocyte Stimulating Hormone trifluoroacetate salt has been used to detect its effect on O2 consumption and CO2 production in C57BL/6 mice. It is also used to determine its effect on leptin secretion in the primary cultures of differentiated adipocytes.
Definition
ChEBI: Afamelanotide is a polypeptide comprising of 13 amino acids which is an analogue of alpha-melanocyte stimulating hormone. It is approved as a dermatologic drug for the prevention of phototoxicity in adult patients with erythropoietic protoporphyria. It has a role as a dermatologic drug.
General Description
[Nle4, D-Phe7]-α-melanocyte stimulating hormone is a potent analogue of α;-melanocyte-stimulating hormone (α -MSH). αMSH is a tridecapeptide, mostly produced by the cells in the brain, pituitary and in circulation.
Biochem/physiol Actions
[Nle4, D-Phe7]-α-melanocyte stimulating hormone is 100 times more potent than α-MSH in stimulating melanoma tyrosinase, which is a rate limiting enzyme in melanin biosynthesis and is 26 times as potent as α-MSH in S91adenylate cyclase assay. α –MSH has an essential role to play in melanin production in animals. It also regulates development of several skin diseases, including cutaneous inflammation and hyper-proliferative skin diseases.
Side effects
The TGA has previously warned consumers against the use of Melanotan-I and Melanotan-II for tanning and weight loss. Side-effects include darkened skin, increased moles and freckles, nausea, vomiting, loss of appetite, flushing of the face, involuntary stretching and yawning, and spontaneous erections.
