Melanotan-II — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Melanotan-II, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| Melanocortin-1 receptor (MC1R) | Potent agonist | Mediates melanogenesis; the effect for which the compound is used |
| Melanocortin-4 receptor (MC4R) | Agonist | Mediates appetite suppression and sexual effects |
| Melanocortin-3 and -5 receptors | Agonist | Non-selective |
§2.2Mechanism of action
Melanotan-II is a potent non-selective melanocortin receptor agonist. MC1R agonism stimulates eumelanin synthesis in melanocytes, producing pigmentation without ultraviolet exposure. MC4R agonism concurrently suppresses appetite and induces sexual arousal. The non-selectivity that produces the tanning effect is inseparable from the systemic effects.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈1 h (reported)
- Time to maximum concentration
- ≈30–60 min
- Volume of distribution
- not published
- Plasma protein binding
- not published
- Clearance
- not published
- Bioavailability
- not established
Proteolytic degradation to fragments, one of which is bremelanotide. No formal human pharmacokinetic study has been published.
§2.4Interactions
- Not characterised
References cited on this page
References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.
- Clayton AH, Althof SE, Kingsberg S, DeRogatis LR, Kroll R, Goldstein I, Kaminetsky J, Spana C, Lucas J, Jordan R, Portman DJ. Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial. Women’s Health 2016;12(3):325–337. doi:10.2217/whe-2016-0018 · PMID 27181790
- Carvalho M, Dinis-Oliveira RJ. Analytical and forensic aspects of counterfeit peptide hormones. Drug Testing and Analysis 2023;15(1):5–19. identifier not held by the Institute The digital object identifier previously carried on this record did not resolve and has been withdrawn. Journal and year are retained.
Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.