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Kisspeptin-10

Sexual Health

Also known as: KP-10, Metastin (54-64)

Half-life: ~3-4 minutes (plasma)

Last reviewed:  ·  Published:

Sexual Health

Overview

Kisspeptin-10 is the most potent active fragment of kisspeptin, a hypothalamic neuropeptide that sits at the top of the reproductive hormone cascade. Kisspeptin neurons in the arcuate nucleus and preoptic area of the hypothalamus express the KISS1R (formerly GPR54) receptor on GnRH neurons; when activated, kisspeptin neurons trigger pulsatile GnRH release, which in turn drives LH and FSH release from the pituitary, ultimately stimulating gonadal sex steroid production and gametogenesis. Loss-of-function mutations in either KISS1 or KISS1R cause hypogonadotropic hypogonadism — establishing kisspeptin as essential for normal pubertal development and adult reproductive function.

In clinical research, kisspeptin has been investigated as a fertility-stimulating agent in women undergoing IVF and as a diagnostic tool for distinguishing hypothalamic from pituitary causes of hypogonadism. Studies at Imperial College London (Waljit Dhillo's group) have established kisspeptin as a more physiologic trigger of egg maturation in IVF than hCG, potentially with lower risk of ovarian hyperstimulation syndrome. Kisspeptin has also been studied for its effects on libido and sexual arousal in both men and women, with some studies showing increases in sexual-stimulus-related brain activation.

Research-grade Kisspeptin-10 is sold by peptide vendors and is used both in legitimate hormonal research and in self-experimentation by users seeking effects on libido, testosterone, or fertility. Single-dose tolerability in clinical studies has been good. Chronic dosing has not been studied in humans and could theoretically produce GnRH-axis desensitization analogous to that observed with GnRH analogs (Triptorelin).

History

KISS1 was originally identified in 1996 as a metastasis-suppressor gene (hence the alias "metastin"). Its role in reproductive endocrinology emerged in 2003-2004 when independent groups identified loss-of-function mutations in KISS1R as causing hypogonadotropic hypogonadism in humans. Subsequent clinical research, particularly from Waljit Dhillo's group at Imperial College London, established kisspeptin as a therapeutic and diagnostic tool in reproductive medicine.

Effects

  • Triggers GnRH pulse from hypothalamus
  • Stimulates LH and FSH release from pituitary
  • Indirectly raises testosterone (men) or estrogen (women)
  • Triggers egg maturation in IVF protocols
  • May increase libido and sexual arousal
  • Increases sexual-stimulus brain activation

Side Effects

  • Generally well-tolerated at single doses
  • Headache (uncommon)
  • Theoretical: GnRH-axis desensitization with chronic dosing
  • Possible flushing or warmth sensation
  • Limited long-term safety data

Tolerability

Single subcutaneous or IV doses of Kisspeptin-10 in clinical research have been very well-tolerated, with adverse events rare and generally limited to mild headache. The peptide has been used safely in IVF protocols at clinical institutions. Chronic dosing safety in humans is essentially unstudied; based on analogy with GnRH agonist therapy, prolonged high-dose use could theoretically produce paradoxical down-regulation of the HPG axis.

Dosing Ranges

Libido / HPG axis stimulation

Dose Range

50-200 mcg

Frequency

Once or twice daily (SubQ)

Duration

Cycle-based, 2-4 weeks per cycle

IVF trigger (clinical, IV)

Dose Range

6.4-12.8 nmol/kg

Frequency

Single dose 36 hours pre-collection

Duration

One-time

Dosing information is for educational purposes only. Consult a healthcare professional before using any peptide.

Reconstitution

Preparation Details

Typical Vial Size

5 mg

Water Type

Bacteriostatic water (BAC water)

Mixing Volume

2 mL

Half-Life

~3-4 minutes (plasma)

Molecular Weight

1,302 Da

Store reconstituted vial refrigerated at 2-8°C. Use within 14-21 days. Subcutaneous administration is the most common research route. Clinical IVF use is IV per protocol.

Calculate Kisspeptin-10 dose

Where to buy Kisspeptin-10

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Regulatory Status

FDA Status

Not FDA approved as a therapeutic.

Legal Status

Unregulated research chemical. Prohibited by WADA.

USA

Not approved

Research-only; clinical investigation ongoing for IVF use

EU

Not approved

Research-only; clinical investigation ongoing

UK

Not approved

Research-only; clinical trials ongoing at Imperial College

Australia

Not approved

TGA has not authorized

Canada

Not approved

Not authorized for human use

Cited Studies

The GPR54 gene as a regulator of puberty

Seminara SB, Messager S, Chatzidaki EE, Thresher RR, Acierno JS Jr, Shagoury JK, Bo-Abbas Y, Kuohung W, Schwinof KM, Hendrick AG, Zahn D, Dixon J, Kaiser UB, Slaugenhaupt SA, Gusella JF, O'Rahilly S, Carlton MB, Crowley WF Jr, Aparicio SA, Colledge WH

New England Journal of Medicine (2003)

Landmark identification of GPR54 (KISS1R) loss-of-function mutations as the cause of idiopathic hypogonadotropic hypogonadism in humans, establishing the kisspeptin system as the master upstream regulator of puberty and reproductive function.

View Study →

The clinical applications of kisspeptin in reproductive medicine

Abbara A, Clarke SA, Dhillo WS

Endocrine Reviews (2018)

Comprehensive review by Waljit Dhillo's group at Imperial College London of clinical applications of kisspeptin, including its use as an ovulation trigger in IVF and as a diagnostic tool for hypogonadism.

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Kisspeptin enhances brain responses to olfactory and visual cues of attraction in men

Comninos AN, Wall MB, Demetriou L, Shah AJ, Clarke SA, Narayanaswamy S, Nesbitt A, Izzi-Engbeaya C, Prague JK, Abbara A, Ratnasabapathy R, Salem V, Nijher GM, Jayasena CN, Tanner M, Bassett P, Mehta A, Rabiner EA, Hönigsperger C, Silva MR, Brandtzaeg OK, Lundanes E, Wilson SR, Brown RC, Thomas SA, Bloom SR, Dhillo WS

Journal of Clinical Investigation (2017)

Demonstrated that intravenous kisspeptin enhanced brain responses to sexual visual and olfactory cues in healthy men using fMRI, providing mechanistic support for kisspeptin's effects on sexual arousal beyond its hormone-axis effects.

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