kisspeptin-10 5mg
Kisspeptin peptides are critical in human reproductive physiology and are potential therapies for infertility. Kisspeptin-10 stimulates gonadotropin release in both male and female rodents. However, few studies have investigated the effects of kisspeptin-10 on gonadotropin release in humans, and none have investigated the effect in women. If kisspeptin is to be useful for treating reproductive disease, its effects in both men and women must be established.
In healthy men, serum LH and FSH were elevated after iv bolus kisspeptin-10, at doses as low as 0.3 and 1.0 nmol/kg, respectively. In healthy women during the follicular phase of the menstrual cycle, no alterations in serum gonadotropins were observed after iv bolus, sc bolus, or iv infusion of kisspeptin-10 at maximal doses of 10 nmol/kg, 32 nmol/kg, and 720pmol/kg/min, respectively. In women during the preovulatory phase, serum LH and FSH were elevated after iv bolus kisspeptin-10 (10 nmol/kg).
Kisspeptin-10 stimulates gonadotropin release in men as well as women during the preovulatory phase of menstrual cycle but fails to stimulate gonadotropin release in women during the follicular phase. The sexual dimorphism of the responsiveness of healthy men and women to kisspeptin-10 administration has important clinical implications for the potential of kisspeptin-10 to treat disorders of reproduction.
The kisspeptins are critical regulators of mammalian reproductive physiology. In humans, inactivating mutations of the kisspeptin receptor (KISS1R) cause pubertal failure, and activating mutations can lead to precocious puberty. The human kisspeptin peptides, kisspeptin-10, -13, -14, and -54, are named according to their number of constituent amino acids. All kisspeptin peptides share the C-terminal decapeptide sequence, kisspeptin-10, which is required for biological activity in vitro.
Central or peripheral administration of the shorter kisspeptin peptide, kisspeptin-10, has been demonstrated to stimulate gonadotropin release in several mammalian species. This effect is abolished by preadministration of an antagonist to the hypothalamic hormone GnRH. Kisspeptin-10 is therefore thought to stimulate the release of GnRH from the hypothalamus, which then stimulates gonadotropin release from the pituitary gland. The longer kisspeptin peptide, kisspeptin-54, has also been shown to stimulate gonadotropin release in rodents. In addition, administration of kisspeptin-54 stimulates gonadotropin secretion in humans. Kisspeptin therefore has the potential to become a novel therapy for treatment of reproductive disorders in humans.
The shorter amino acid sequence of kisspeptin-10 makes it simpler and cheaper to synthesize than kisspeptin-54. Future kisspeptin therapies may therefore be based upon kisspeptin-10 rather than kisspeptin-54. It is therefore therapeutically important to determine whether kisspeptin-10 can stimulate reproductive hormone release in healthy men and women. Kisspeptin-10 stimulates gonadotropin release in male rhesus monkeys (. Furthermore, two recent reports have suggested that kisspeptin-10 administration to healthy men stimulates gonadotropin release. Although kisspeptin-10 is known to stimulate gonadotropin release in animals, there are no published data examining the effects of administering kisspeptin-10 to female primates or humans.
This study aimed to determine the effects of kisspeptin-10 administration on reproductive hormone release in healthy men and, for the first time, in healthy women.
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