Melanotan II (revision 4)
Old revision·06:51, 14 Dec 2024·PriorAuthPaz
| Melanotan II | |
|---|---|
| Class | Melanocortin receptor agonist |
| Selectivity | Non-selective across MC1R, MC3R, MC4R, MC5R |
| Status | Not approved in any jurisdiction |
| Related approved compound | Bremelanotide (MC4R-directed) |
| Compound infobox · conventions | |
Melanotan II is a synthetic cyclic analogue of α-melanocyte-stimulating hormone and a non-selective agonist at melanocortin receptors. It is not approved in any jurisdiction and is distributed as a research chemical.[1]
Non-selectivity is the defining property. Agonism at MC1R produces melanogenesis, the effect for which it is sought; agonism at MC4R affects appetite and sexual function; agonism at MC3R and MC5R contributes further effects. A single compound producing all of them simultaneously is a pharmacological blunt instrument.[1]
Pharmacology
[edit]The melanocortin system comprises five receptors with distinct distributions. MC1R on melanocytes controls the switch between pheomelanin and eumelanin synthesis; MC4R in the hypothalamus is central to appetite regulation and is the target of approved anti-obesity compounds in rare genetic conditions. See Arcuate nucleus.[2]
Melanotan II activates all of these. Selective compounds developed subsequently — bremelanotide for sexual dysfunction, and MC4R-directed agents for genetic obesity — represent the pharmacological correction of that non-selectivity.[1]
References
- ^ a b c Hadley ME, Dorr RT. "Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization." Peptides 26(10):1687–1689 (2005). PMID 16112778.
- ^ Cone RD. "Anatomy and regulation of the central melanocortin system." Nature Neuroscience 8(5):571–578 (2005). PMID 15856065.