Kisspeptin 234 is an analogue of kisspeptin 10 which acts as a kisspeptin receptor antagonist. Of a series, kisspeptin 234 most potently inhibited kisspeptin 10 stimulation of inositol phosphate release in Chinese hamster ovarian cells stably expressing the human GPR54 with an IC50 of 7 nM. Intracerebroventricular administration of kisspeptin 234 causes delayed vaginal opening in rats (an indicator of puberty) and prevents an increase in circulating luteinising hormone concentration when co-administrated with kisspeptin 10.
