Kisspeptin-10 is the shortest active fragment (10 amino acids) of kisspeptin, a hypothalamic peptide that signals through the KISS1R (GPR54) receptor. It has been studied in cell assays, rodents and small human physiology studies.
Kisspeptin-10 binds the G-protein-coupled receptor KISS1R (GPR54); in receptor-expressing cells this triggered ERK1/2 and p38 MAPK phosphorylation [1]. In rats it raised LH, FSH and testosterone and stimulated GnRH (LHRH) release from hypothalamic explants, but not LH release from isolated pituitary tissue, indicating action mainly upstream at the hypothalamus [2]. Human studies have measured gonadotropin responses and found differences between men and women [3][4].
| Study | Model | Reported result | Source |
|---|---|---|---|
| Receptor identification and signaling [1] | Cell CHO-K1 cells expressing GPR54 | Kisspeptin peptides, including the 10-residue form, activated the receptor and induced ERK1/2 and p38 MAPK phosphorylation. | Peer-reviewed J Biol Chem 2001 |
| Central and peripheral administration in rats [2] | Rat Adult male rats; central and peripheral administration; hypothalamic explants and pituitary fragments | Researchers measured plasma LH, FSH and testosterone and hypothalamic LHRH release; no effect on LH/FSH from pituitary fragments at 100-1000 nM. | Peer-reviewed J Neuroendocrinol 2004 |
| LH pulse study in men [3] | Human Healthy men, three small studies (n=6, 4, 4): single-blind ascending bolus vs vehicle and continuous infusions up to 22.5 h | Endpoints: serum LH, FSH and testosterone, LH pulse frequency (deconvolution), and tachyphylaxis. Published. | Peer-reviewed J Clin Endocrinol Metab 2011 |
| Sex comparison study [4] | Human Healthy men and women (4-5 per group); women studied at two menstrual phases | Endpoint: circulating LH and FSH after bolus and infusion, compared between sexes and menstrual phases. Published. | Peer-reviewed J Clin Endocrinol Metab 2011 |
| Kisspeptin and the HPG axis [5] | Review Narrative review of kisspeptin isoforms, receptor and reproductive-axis research | Summarizes kisspeptin-10 cell signaling, rodent and human hormone studies; notes many findings are isoform- and species-specific. | Peer-reviewed Front Endocrinol 2022 |
Human trials are listed for research context only; outcomes are reported in the linked publications. Animal and lab results do not establish effects in humans.
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