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Kisspeptin — Alphagenics vial
Sexual Health

Kisspeptin

Kisspeptin-10 · Metastin (45-54) · KP-10

Kisspeptin receptor agonist (KISS1R / GPR54)

Molecular weight1302.4 g/mol
CAS374675-21-5
Length10 amino acids
Available presentations
Certificate of analysis (COA)
10mg
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About Kisspeptin

Kisspeptin-10 is the biologically active C-terminal fragment of kisspeptin-54, encoded by the KISS1 gene.

Kisspeptins act on the KISS1R (GPR54) receptor of GnRH-releasing neurons in the hypothalamus and are considered the main upstream regulator of the reproductive axis: their signaling is necessary for the onset of puberty and for the pulsatile release of LH and FSH.

Quick guide · 5 key points

Kisspeptin and the reproductive axis

Kisspeptin acts in the hypothalamus, upstream of GnRH, and is a key signal of the reproductive axis. Here are five things the research shows.

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  1. 1

    The switch that turns on puberty

    Kisspeptins act on the GPR54 (KISS1R) receptor. People and mice with GPR54 mutations have been shown to have hypogonadotropic hypogonadism, without normal pubertal development. That is why it is considered essential for GnRH secretion and puberty.3,1

    GPR54Receptor essential for GnRH and the onset of puberty
  2. 2

    It raises LH and testosterone in men

    In healthy men, an intravenous bolus of kisspeptin-10 was associated with a rise in LH from 4.1 to 12.4 IU/L within 30 minutes, and its infusion with more LH pulses and higher testosterone. Kisspeptin-54 also raised LH, FSH and testosterone compared with saline.2,3

    3×LH at 30 min after a kisspeptin-10 bolus
  3. 3

    Egg maturation in IVF

    In 53 women undergoing IVF, a single kisspeptin-54 injection was associated with egg maturation at every dose tested. Embryos were transferred in 92%, and 12 of 53 had a clinical pregnancy (23%).4

    12 of 53clinical pregnancies after a single kisspeptin-54 injection
  4. 4

    It acts on the emotional brain too

    In a brain-imaging study of 29 healthy young men, kisspeptin was associated with greater limbic activity in response to sexual and couple-bonding stimuli, compared with placebo. It also attenuated negative mood.5

    29healthy men in the functional MRI study
  5. 5

    Short action, and the effect fades with repeat doses

    The plasma half-life of kisspeptin-54 in men was 27.6 minutes. In women with hypothalamic amenorrhea, twice-daily injections for 2 weeks were associated with desensitization (tachyphylaxis): the LH rise fell from 24.0 IU/L on day 1 to 2.5 IU/L on day 14. At the doses tested, GnRH was 2–3 times more potent.3,6,7

    24.0 → 2.5IU/L LH rise: day 1 vs. day 14
References
  1. Seminara SB, et al. The GPR54 gene as a regulator of puberty. N Engl J Med. 2003;349(17):1614-27. PMID 14573733
  2. George JT, et al. Kisspeptin-10 is a potent stimulator of LH and increases pulse frequency in men. J Clin Endocrinol Metab. 2011;96(8):E1228-36. PMID 21632807
  3. Dhillo WS, et al. Kisspeptin-54 stimulates the hypothalamic-pituitary gonadal axis in human males. J Clin Endocrinol Metab. 2005;90(12):6609-15. PMID 16174713
  4. Jayasena CN, et al. Kisspeptin-54 triggers egg maturation in women undergoing in vitro fertilization. J Clin Invest. 2014;124(8):3667-77. PMID 25036713
  5. Comninos AN, et al. Kisspeptin modulates sexual and emotional brain processing in humans. J Clin Invest. 2017;127(2):709-719. PMID 28112678
  6. Jayasena CN, et al. Subcutaneous injection of kisspeptin-54 acutely stimulates gonadotropin secretion in women with hypothalamic amenorrhea, but chronic administration causes tachyphylaxis. J Clin Endocrinol Metab. 2009;94(11):4315-23. PMID 19820030
  7. Jayasena CN, et al. Direct comparison of the effects of intravenous kisspeptin-10, kisspeptin-54 and GnRH on gonadotrophin secretion in healthy men. Hum Reprod. 2015;30(8):1934-41. PMID 26089302

Structure and sequence

2D structure generated from PubChem CID 25240297

Sequence

Y1N2W3N4S5F6G7L8R9F10-NH2

Five findings from studies

Summary of results reported in the scientific literature. Each finding describes what was observed in the cited study, in its specific population and conditions; it does not constitute a therapeutic indication.

  1. Clinical study

    In healthy men, administration of kisspeptin-10 has shown an increase in serum LH and in LH pulse frequency, with an increase in testosterone.

    George JT et al. J Clin Endocrinol Metab. 2011;96:E1228-E1236 · PMID 21632807
  2. Clinical study

    In healthy men, intravenous kisspeptin-54 has shown an increase in LH, FSH and testosterone.

    Dhillo WS et al. J Clin Endocrinol Metab. 2005;90:6609-6615 · PMID 16174713
  3. Clinical study

    In women undergoing in vitro fertilization, a single dose of kisspeptin-54 has triggered final oocyte maturation.

    Jayasena CN et al. J Clin Invest. 2014;124:3667-3677 · PMID 25036713
  4. Clinical study

    In neuroimaging studies in men, kisspeptin has been associated with greater activity in limbic regions in response to sexual and bonding stimuli.

    Comninos AN et al. J Clin Invest. 2017;127:709-719 · PMID 28112678
  5. Clinical study

    In women with hypothalamic amenorrhea, kisspeptin has been associated with acute stimulation of gonadotropin secretion; with repeated administration for 2 weeks, desensitization (tachyphylaxis) has been observed.

    Jayasena CN et al. J Clin Endocrinol Metab. 2009;94:4315-4323 · PMID 19820030

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