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Kisspeptin-10 is an active peptide from the kisspeptin protein family, encoded by the KISS1 gene. This decapeptide, made up of 10 amino acids, is the smallest functional fragment of kisspeptins that still works effectively. Kisspeptins play a key role in controlling the hypothalamic-pituitary-gonadal (HPG) axis, which is essential for reproductive health and puberty.
Kisspeptin-10 is an agonist of the G-protein-coupled receptor GPR54 (also known as KISS1R). This receptor-ligand interaction is crucial for regulating the release of gonadotropin-releasing hormone (GnRH). GnRH then affects the pituitary gland’s secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
Kisspeptin works by activating the GPR54 receptor on GnRH neurons in the hypothalamus. This activation causes a chain reaction that increases calcium levels, which in turn leads to the release of gonadotropin-releasing hormone (GnRH). GnRH then stimulates the anterior pituitary gland, prompting it to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
These two hormones regulate the function of the gonads, including the production of gametes and sex hormones. By activating this hypothalamic-pituitary-gonadal axis (known as HPG), Kisspeptin-10 plays a vital role in managing the onset of puberty, fertility, and reproductive hormone levels, making it a key focus for therapeutic research.
Regulation of the reproductive (hypothalamic-pituitary-gonadal) axis: Research has demonstrated that Kisspeptin, encoded by the KISS1 gene, is a critical regulator of the hypothalamic-pituitary-gonadal (HPG) axis, essential for puberty and reproductive function. Studies have shown that it activates GnRH neurons via the kisspeptin receptor (GPR54), stimulating gonadotropin (LH, FSH) and sex hormone release [1]. Mutations in kisspeptin or GPR54 cause reproductive disorders like idiopathic hypogonadotropic hypogonadism (IHH) or precocious puberty [2].
Kisspeptin integrates metabolic, stress, and hormonal signals, making it a promising therapeutic target for infertility, hypothalamic amenorrhea, and hormone-sensitive conditions. Chronic high-dose kisspeptin analogs may also treat sex hormone-dependent malignancies, highlighting its broad clinical potential in reproductive health management [3].
Effects on Sexual Desire, the Sexual Brain, and Psychosexual Processes: Research has shown that Kisspeptin plays a pivotal role in modulating sexual desire and psychosexual processes by enhancing brain activity in key sexual and emotional networks [4]. Studies suggest that in women with hypoactive sexual desire disorder (HSDD), kisspeptin infusion improved brain responses to erotic stimuli and facial attraction, correlating with reduced sexual aversion and distress [5].
In men with HSDD, kisspeptin increased penile tumescence by 56% and enhanced subjective arousal. Functional MRI studies revealed kisspeptin’s activation of sexual-processing brain regions, including the hippocampus and cingulate cortex [6]. These findings highlight kisspeptin’s potential as a therapeutic agent for HSDD, improving sexual desire and emotional well-being.
Effects on bone metabolism: Research has demonstrated that Kisspeptin positively impacts bone metabolism by promoting bone formation and inhibiting resorption. In vitro studies reveal that kisspeptin enhances osteoblast activity, leading to a 41% increase in alkaline phosphatase levels, while simultaneously reducing osteoclast resorptive activity by 53%.
A clinical study found that kisspeptin infusion in healthy men increased the bone-formation marker osteocalcin by 24%, regardless of sex steroid levels. These findings suggest that kisspeptin has a dual action on bone cells, making it a promising therapeutic candidate for osteoporosis and other bone-related disorders [7].
Interface between metabolism and reproduction: Studies indicate that Kisspeptin serves as a critical link between metabolism and reproduction, ensuring reproductive function aligns with favorable energy and metabolic conditions. Kisspeptin neurons respond to metabolic cues, acting directly via receptors in the brain, pancreas, and brown adipose tissue, and indirectly through gonadal hormones.
Disruptions in kisspeptin signaling, as seen in conditions like obesity, diabetes, or undernutrition, impair both metabolic and reproductive functions. Emerging evidence highlights kisspeptin’s potential as a therapeutic target for treating metabolic and reproductive disorders, including hypogonadotropic hypogonadism and polycystic ovary syndrome, offering a promising avenue for integrated management of these interconnected systems [8].
[1] K Kochar Kaur, G Allahbadia, and M Singh (2012) Kisspeptins in human reproduction-future therapeutic potential – Journal of Assisted Reproduction and Genetics, 2012 Oct Volume 29 (Issue 10), Pages 999-1011.
[2] J T Mogford, C N Jayasena, and W S Dhillo (2014) Evaluating the potential utility of kisspeptin to treat reproductive disorders – Expert Review of Endocrinology and Metabolism, Volume 9 (Issue 3), pages 251-261, May 2014.
[3] J K Prague and W S Dhillo (2015) Potential Clinical Use of Kisspeptin – Neuroendocrinology (2015) Volume 102 (Issue 3), Pages 238–245.
[4] A N Comninos, M B Wall, L Demetriou, et al (2017) Kisspeptin modulates sexual and emotional brain processing in humans – Journal of Clinical Investigations, 2017, Volume 127 (Issue 2), Pages 709-719.
[5] L Thurston, T Hunjan, and N Ert (2022) Effects of Kisspeptin Administration in Women With Hypoactive Sexual Desire Disorder – JAMA Network Open, October 26, 2022, Volume 5 (Issue 10), Page e2236131.
[6] E Mills, N Ertl, M B Wall, L Thurston, et al (2022) Kisspeptin administration has therapeutic potential for men with low sexual desire by increasing penile tumescence and sexual brain processing – Endocrine Abstracts (2022) Volume 81, abstract OC7.2
[7] A N Comninos, M S Hansen, A Courtney, S Choudhury, et al (2022) Acute Effects of Kisspeptin Administration on Bone Metabolism in Healthy Men – The Journal of Clinical Endocrinology & Metabolism, Volume 107, Issue 6, June 2022, Pages 1529–1540.
[8] J Helena Sliwowska, N E Woods, A Rzgallah Alzahrani, et al (2024) Kisspeptin a potential therapeutic target in treatment of both metabolic and reproductive dysfunction – Journal of Diabetes, 2024 Apr, Volume 16 (Issue 4), Page e13541.
The answers to the most frequently asked questions about Kisspeptin.
Buy Kisspeptin Peptide Nasal Spray from Peptide Works. Offered in 15ml and 30ml glass spray bottles, this nasal spray provides a non-invasive administration route for research purposes.
Kisspeptin is studied for its role in regulating reproductive hormones and sexual behavior. Research shows it can activate brain regions linked to attraction and stimulate natural hormone release like LH and FSH. Findings are early but encouraging, making kisspeptin a popular choice among researchers exploring hormonal and reproductive signaling pathways.
Research shows kisspeptin can trigger egg maturation in IVF by creating a natural LH surge, similar to hCG. Early studies suggest it may reduce the risk of ovarian hyperstimulation in some cases. Kisspeptin remains a research peptide and is not approved for IVF use, but it continues to show strong scientific promise.
In studies, kisspeptin has shown mild and short-term side effects. Reported reactions include headache, flushing and nausea. Some participants experienced fatigue or mood changes. Research is still ongoing to understand its long-term safety profile, as current findings come from short, controlled clinical studies.
Kisspeptin is not approved by the FDA for medical or human use in the United States. It can only be purchased for laboratory and research purposes from authorized suppliers. Regulations may differ in other countries, where local laws determine how research peptides can be bought, handled, or used. Always follow your country’s peptide regulations before purchasing.
This blog explores the role of the Kisspeptin hormone in testosterone production, focusing on its stimulation of the HPG axis and its effects on luteinizing hormone (LH) and Leydig cells. It also compares Kisspeptin with Sermorelin, outlining their distinct pathways and highlighting their potential for research in hormonal regulation and reproductive health.
This blog explores the roles of PT-141 and Kisspeptin in fertility and reproductive health. It compares their distinct mechanisms, with PT-141 enhancing libido through brain pathways and Kisspeptin regulating fertility hormones through the GnRH system. Together they offer complementary insights into hormonal balance, sexual function and the future of reproductive science.
This blog delves into the fascinating world of the "love hormone," oxytocin. It explores its role in bonding, emotional resilience, and stress control. The post also talks about related peptides such as Kisspeptin and PT-141, showing how they affect reproduction and behavior. In addition, it looks at how these signaling molecules shape trust, connection and new directions for future research.
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