Kisspeptin-10 — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Kisspeptin-10, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| KISS1 receptor (KISS1R, GPR54) | Agonist | Expressed on hypothalamic GnRH neurons; the master regulator of GnRH pulsatility |
§2.2Mechanism of action
Kisspeptin acts on KISS1 receptors on hypothalamic gonadotropin-releasing hormone neurons to stimulate GnRH secretion, and thereby luteinising hormone and follicle-stimulating hormone release. Because it acts upstream of GnRH it preserves the pulsatile architecture of the axis, which distinguishes it from continuous GnRH agonist administration. Its principal clinical research applications are as a diagnostic probe of hypothalamic function and as an alternative trigger for oocyte maturation in assisted reproduction.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈4 min
- Time to maximum concentration
- immediate on infusion
- Volume of distribution
- not published
- Plasma protein binding
- not extensively bound
- Clearance
- high
- Bioavailability
- not established for subcutaneous administration
Rapid proteolysis. The very short half-life confines use to infusion or bolus in a controlled setting.
§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.
- D’Hondt M, Bracke N, Taevernier L, Gevaert B, Verbeke F, Wynendaele E, De Spiegeleer B. Related impurities in peptide medicines. Journal of Pharmaceutical and Biomedical Analysis 2014;101:2–30. doi:10.1016/j.jpba.2014.06.012 · PMID 25044089
- Manning MC, Chou DK, Murphy BM, Payne RW, Katayama DS. Stability of protein pharmaceuticals: an update. Pharmaceutical Research 2010;27(4):544–575. doi:10.1007/s11095-009-0045-6 · PMID 20143256
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.