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 27638896
- Carvalho M, Dinis-Oliveira RJ. Analytical and forensic aspects of counterfeit peptide hormones. Drug Testing and Analysis 2023;15(1):5–19. doi:10.1002/dta.3379
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.