Kisspeptin

What is Kisspeptin and Its Mechanism of Action

Kisspeptin 10 (also known as KISS) is a neuropeptide encoded by the KISS1 gene, primarily involved in regulating the hypothalamic-pituitary-gonadal (HPG) axis, initiating puberty, maintaining reproductive function, and suppressing tumors.

KISS exerts its effects through the GPR54 receptor. GPR54 comprises seven transmembrane domains and belongs to the G protein-coupled receptor family.

Outside the hypothalamic region, GPR1 distribution aligns with KISS, with both highly expressed in placental tissue, the central nervous system, pancreas, and liver. This suggests KISS involvement in metabolism and homeostasis.

Further studies indicate KISS is a neuropeptide involved in the hypothalamic-pituitary-gonadal (HPG) axis, controlling all stages of reproduction. It also plays a regulatory role in puberty, the menstrual cycle, spermatogenesis, and human placental implantation and development.

The KISS/GPR54 complex has been reported as a negative regulator of cancer metastasis in breast, gastric, pancreatic, bladder, and prostate cancers. Expression levels of the KISS1/GPR54 complex are considered a biomarker for ovarian cancer progression.

Kisspeptin Benefits

Kisspeptin stimulates the secretion of gonadotropin-releasing hormone (GnRH), thereby increasing the release of LH (luteinizing hormone) and FSH (follicle-stimulating hormone). This, in turn, stimulates Leydig cells in the testes, leading to increased testosterone production.

Kisspeptin binds to receptors in the pituitary gland, initiating a series of reactions that prompt the pituitary to release neurotransmitters. These neurotransmitters then signal the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). These hormones play crucial roles in the production of testosterone and estradiol. Without kisspeptin, the entire chain reaction is disrupted.

Kisspeptin mimics the effects of clomiphene and hCG, thereby maintaining male fertility and preventing testicular atrophy. It has been safely and effectively used in both males and females.

Kisspeptin Dosage

100 micrograms administered subcutaneously daily. Some recommend approximately 100–200 micrograms per injection, administered subcutaneously 1–2 times weekly to avoid desensitization. It is advocated for use 2–3 times weekly in combination with testosterone replacement therapy (TRT). Ideally, patients should take kisspeptin concurrently with TRT, typically 2-3 times weekly at 100-200 mcg per injection. Dosage may be adjusted based on individual circumstances and physician guidance.

Kisspeptin Side Effects

Redness, swelling, or pain may occur at the injection site. Initial symptoms of poor tolerance to the substance may include nausea, vomiting, diarrhea, headache, or increased sweating.

Seek immediate medical attention if severe side effects occur.