A hypothalamic neuropeptide that stimulates GnRH release and is being investigated for fertility and hypogonadism.
Kisspeptin is a family of neuropeptides encoded by the KISS1 gene, produced primarily in the arcuate nucleus and anteroventral periventricular nucleus of the hypothalamus. The most studied form for research purposes is Kisspeptin-10 (KP-10), the C-terminal decapeptide. Kisspeptin is recognized as the master regulator of the hypothalamic-pituitary-gonadal (HPG) axis — without kisspeptin signaling, puberty does not occur and reproductive function is absent. It has been investigated in Phase I and II clinical trials for hypogonadotropic hypogonadism, female infertility, and as a diagnostic tool for HPG axis assessment. Kisspeptin levels are regulated by sex steroids (both positive and negative feedback), metabolic status (leptin, insulin), and stress, making it a key integrator of reproductive and metabolic signaling.
“A hypothalamic neuropeptide that stimulates GnRH release and is being investigated for fertility and hypogonadism.”
Kisspeptin binds to the KISS1 receptor (KISS1R, also known as GPR54) — a Gq/11-coupled GPCR expressed on GnRH neurons in the hypothalamus. KISS1R activation triggers the PLC-IP3-DAG pathway, increasing intracellular calcium and depolarizing GnRH neurons, which triggers pulsatile GnRH release into the hypothalamic-pituitary portal circulation. GnRH then binds to GnRH receptors on gonadotroph cells in the anterior pituitary, stimulating the synthesis and pulsatile secretion of LH and FSH. LH acts on Leydig cells in the testes to stimulate testosterone synthesis, while FSH supports spermatogenesis and follicular development. The pulsatile nature of kisspeptin-GnRH-LH signaling is critical: continuous kisspeptin stimulation leads to receptor desensitization and gonadotropin suppression, while pulsatile administration maintains or restores reproductive function.
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The statements made within this website have not been evaluated by the US Food and Drug Administration. The products and information provided are not intended to diagnose, treat, cure, or prevent any disease. This website is intended for educational and research purposes only. Many peptides described on this site are not approved by the FDA for human therapeutic use and are classified as research chemicals. Nothing on this site constitutes medical advice.
Phase II trials for hypogonadotropic hypogonadism
Demonstrated LH and testosterone stimulation in human studies
Phase I/II trials for female infertility ongoing
Multiple animal studies and/or early human trials. Reasonable confidence in mechanism, but human data is limited.
Peptides commonly used alongside Kisspeptin for synergistic effects.
The most selective GHRP available, stimulating GH release with minimal cortisol or prolactin elevation.
An FDA-approved GHRH analog used for GH deficiency diagnosis and treatment, with a favorable safety profile.
Category
Hormone & GH
Status
Dose
1–10 mcg/kg
Frequency
Pulsatile (every 90 minutes) or as directed
Cycle
4–8 weeks
Peptides
Protocols
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FDA Disclaimer: The statements made within this website have not been evaluated by the US Food and Drug Administration. The products and information provided are not intended to diagnose, treat, cure, or prevent any disease. This website is intended for educational and research purposes only. Many compounds described on this site are not approved by the FDA for human therapeutic use. Some are available only as compounded preparations or as materials sold for laboratory use, and several are on FDA's Category 2 list for significant safety risks. Nothing on this site constitutes medical advice or a recommendation to use any compound described.
