Kisspeptin 10 mg

Description

GPR54—also known as KISS1 receptor (KISS1R)—is a G‑protein‑coupled receptor that serves as the endogenous target for kisspeptin peptides. Genetic studies have shown that kisspeptins are the natural ligands for GPR54; loss‑of‑function mutations in GPR54 cause sexual immaturity and infertility in humans and mice. The KISS1 gene encodes a 54‑amino‑acid peptide (often called kisspeptin‑54 or metastin), but shorter C‑terminal fragments such as kisspeptin‑10, ‑13 and ‑14 retain full biological activity. In fact, the 10‑amino‑acid C‑terminal fragment is as potent as the full‑length peptide in stimulating the GPR54 receptor and in triggering luteinizing‑hormone secretion.

Activation of GPR54 is coupled to phospholipase‑C signalling, which increases intracellular Ca²⁺, stimulates arachidonic‑acid release and activates ERK1/2 and p38 MAP kinases. These downstream events depolarize gonadotropin‑releasing hormone (GnRH) neurons and lead to robust GnRH release. Kisspeptin‑10 can also enhance spontaneous calcium oscillations in GnRH neurons, producing long‑lasting depolarization and burst‑type firing. Consequently, central administration of kisspeptin in rodents causes a rapid surge in GnRH and downstream gonadotropin secretion. However, prolonged or high‑dose stimulation can desensitize this pathway: chronic administration of a kisspeptin analog (TAK‑448) markedly suppressed luteinizing‑hormone and testosterone secretion in male rodents, indicating that continuous exposure may down‑regulate the hypothalamic–pituitary–gonadal axis.

Together, these findings indicate that kisspeptin fragments—including kisspeptin‑10—act through GPR54 to activate the reproductive axis by depolarizing GnRH neurons and stimulating gonadotropin release, yet excessive or sustained stimulation may lead to receptor desensitization and suppression of reproductive hormones. PLEASE NOTE THAT ALL PRODUCTS FEATURED HERE ARE INTENDED EXCLUSIVELY FOR RESEARCH AND DEVELOPMENT PURPOSES. THEY ARE NOT DESIGNED FOR ANY FORM OF HUMAN CONSUMPTION. THESE PRODUCTS HAVE NOT UNDERGONE EVALUATION BY THE U.S. FOOD AND DRUG ADMINISTRATION.