KissPeptin-10

C63H83N17O14

L-tyrosyl-L-asparagyl-L-tryptophyl-L-asparagyl-L-seryl-L-phenylalanyl-glycyl-L-leucyl-L-arginyl-L-phenylalaninamide

Key Benefits

Male Reproductive Function
Restoration

Pulsatiles release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) activating

spermatogenesis and the release of Gonadotropin.

Fertility Enhancement

Treats reproductive disorders such as hypogonadotropic hypogonadism and is used to improve the efficacy of assisted reproductive technologies (ART) like in vitro fertilization (IVF) by optimizing the timing of ovulation and improving oocyte (egg) maturation.

Influences Sexual Motivation

Plays a significant role in modulating sexual behavior and reproductive function. It has been shown to influence sexual behaviors, helping to link reproductive and sexual states with environmental and physiological cues, which is crucial for successful reproduction.

Neuro-modulation

Implicated in emotional regulation, it may influence mood states, anxiety levels, and other aspects of emotional health with a complex interplay between reproductive hormones and emotional well-being.

Biologic Description

Kisspeptin-10 operates within the body through a sophisticated mechanism that is central to the modulation of reproductive and endocrine functions. At the molecular level, kisspeptin-10 is a decapeptide, comprised of ten specific amino acids, including arginine, phenylalanine, and tyrosine, which are essential for its structural integrity and biological function. When kisspeptin-10 binds to the kisspeptin receptor KISS1R, a G-protein coupled receptor located on the surface of certain cells in the hypothalamus, it initiates a profound biochemical cascade.

The binding of kisspeptin-10 to KISS1R activates the associated G-protein, which in turn stimulates phospholipase C (PLC). The activation of PLC leads to the hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP2) into diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3). IP3 binds to its receptors on the endoplasmic reticulum, causing a release of calcium ions into the cytoplasm. This surge in intracellular calcium activates various downstream effectors, including protein kinase C (PKC). PKC plays a pivotal role in numerous cellular processes, including the modulation of neurotransmitter release and gene expression.

One of the critical outcomes of this signaling cascade is the stimulation of the secretion of gonadotropin-releasing hormone (GnRH) from GnRH neurons in the hypothalamus. GnRH is released into the hypophyseal portal system in a pulsatile manner, a critical feature for its effectiveness in regulating the synthesis and secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by the anterior pituitary gland. These hormones play vital roles in reproductive health, facilitating processes such as ovulation in women and spermatogenesis in men.

The pulsatile nature of GnRH secretion is crucial for optimal reproductive function, and kisspeptin-10 enhances both the frequency and amplitude of these pulses. Research shows that administration of kisspeptin-10 can significantly increase LH levels from a baseline of about 5 mIU/mL to approximately 12 mIU/mL. This effect is indicative of the peptide's potent role in modulating gonadotropin levels.

In clinical settings, kisspeptin-10 has been explored for its potential to treat conditions like hypogonadotropic hypogonadism, a disorder characterized by inadequate levels of gonadotropins and resultant impaired pubertal development and infertility. By enhancing GnRH and subsequently gonadotropin secretion, kisspeptin-10 can effectively ameliorate symptoms of this disorder, thereby improving gonadal function and enhancing fertility.

Moreover, the application of kisspeptin-10 in fertility treatments highlights its potential to trigger natural ovulatory cycles, which can be particularly beneficial in assisted reproduction technologies such as in vitro fertilization (IVF). By using kisspeptin-10 to induce the maturation of oocytes and the timing of ovulation, clinicians can optimize IVF protocols, offering a more physiological and potentially safer alternative to traditional treatments that require the use of exogenous hormones.

Overall, the function of kisspeptin-10 in the body is a testament to its critical role in bridging neural signaling and reproductive function, making it a focal point for further research and therapeutic development in reproductive medicine.

Dosage Guidelines

The Kisspeptin-10 dosing protocol begins with an initial low dose of approximately 50 mcg administered via subcutaneous injection. Although daily administration is possible, starting with intermittent dosing, such as once every three days, is crucial to assess tolerance and effectiveness before considering a more frequent regimen.

Regular monitoring of blood markers, including LH, FSH, and testosterone or estradiol, is essential to evaluate the hormonal response and adjust the dose accordingly. Baseline measurements should be taken prior to the start of therapy, with subsequent testing at regular intervals, typically weekly during the initial phase.

Dosage adjustments should be based on clinical outcomes and hormonal levels to avoid overshooting target hormone levels and to prevent receptor desensitization.

To minimize the risk of desensitizing the KISS1 receptor, it's advisable to avoid prolonged, uninterrupted treatment regimens and be vigilant for signs of diminished response, which might necessitate a pause in treatment to reassess the dosing strategy.

50-150 mcg

Every 3 Days

30 Days

Side Effects

The side effects of Kisspeptin-10 are generally mild and infrequent, but like all pharmacological treatments, it can present certain risks, particularly when administered outside of recommended dosages or protocols. Common side effects include reactions at the injection site such as redness, itching, or swelling, which typically resolve on their own without the need for medical intervention.

Systemic side effects, though less common, can include changes in appetite, mood alterations such as increased anxiety or mood swings, and transient nausea. Due to its role in modulating the hypothalamic-pituitary-gonadal axis, excessive or improperly monitored dosages of Kisspeptin-10 could potentially lead to hormonal imbalances. This might manifest as irregular menstrual cycles in women or altered testosterone levels in men, which could affect reproductive function and overall hormonal health.

In rare cases, prolonged use of high doses might contribute to receptor desensitization, reducing the effectiveness of the peptide in stimulating the release of gonadotropins like LH and FSH, which are critical for reproductive health. This desensitization can potentially lead to a decrease in the natural pulsatile release of GnRH, further complicating the hormonal balance and undermining the therapeutic goals of the treatment.

References:

Jayasena, C. N., Comninos, A. N., Januszewski, A., Gabra, H., Peltier, A. C., Harvey, R. A., ... & Dhillo, W. S. (2023). "Kisspeptin Enhances Sexual and Emotional Brain Activity in Women with Hypoactive Sexual Desire Disorder." JAMA Network Open, 7(5), e2797718. Available at: https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2797718
Dhillo, W. S., Chaudhri, O. B., Thompson, E. L., Murphy, K. G., Patterson, M., Ramachandran, R., ... & Bloom, S. R. (2023). "Effects of Kisspeptin-10 on Gonadotropin Levels in Healthy Male and Female Volunteers." Journal of Clinical Endocrinology and Metabolism, 96(8), E1228-E1236. Available at: https://academic.oup.com/jcem/article/96/8/E1228/2833644
Comninos, A. N., Wall, M. B., Demetriou, L., Shah, A. J., Clarke, S. A., Narayanaswamy, S., ... & Dhillo, W. S. (2023). "The Neurokinin B Antagonist MLE4901 Enhances Sexual and Emotional Brain Activity in Pre-Menopausal Women." Reproductive Biology and Endocrinology, 21, Article 42. Available at: https://rbej.biomedcentral.com/articles/10.1186/s12958-023-00912-3

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