Abstract:
:Kisspeptin (KP), the endogenous ligand of GPR54, is a mammalian amidated neurohormone, which belongs to the RF-amide peptide family. However, in contrast with the related members of the RF-amide family, little information is available regarding its role in the gastrointestinal motility. With regard to the recent data suggesting KP play an important role in food intake, and while gastrointestinal motility are closely related to it. Thus, in the present work, effects of central administration of KP-13, one of the endogenous active isoforms, on gastrointestinal motility were investigated. The results indicated that intracerebroventricular (i.c.v.) infused of KP-13 significantly facilitated gastrointestinal transit, bead expulsion and fecal pellet output, respectively, while has no effect on gastric emptying. The effects were significantly reversed by GPR54 antagonist 234, but not GnRH receptor antagonist Cetrorelix. However, i.p. injected of KP-13 or compound 5 (10mg/kg), a high metabolic stability kisspeptin analog, did not affect gastrointestinal transit, suggesting that KP-13 or compound 5 facilitated gastrointestinal transit through the activation of central GPR54. Then the gastrointestinal motility-enhancing effects were also presented after infusion of KP-13 into the hypothalamus. In vitro, KP-13 (10-6M) also modulated colonic contraction, but not in the stomach and small intestine. Similarly, KP-13 (10-6M)-induced contractions of circular and longitudinal colonic muscle were significantly attenuated by antagonist 234 (10-6M). In conclusion, all the results indicated that KP-13 promoted gastrointestinal motility through the activation of GPR54, which implicate that KP/GPR54 system might be a new target to treat gastrointestinal function disorder.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Jiang J,Jin W,Peng Y,He Z,Wei L,Li S,Wang X,Chang M,Wang Rdoi
10.1016/j.ejphar.2016.11.041subject
Has Abstractpub_date
2017-01-05 00:00:00pages
216-223eissn
0014-2999issn
1879-0712pii
S0014-2999(16)30754-3journal_volume
794pub_type
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