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Rapakinin, Arg-Ile-Tyr, Derived From Rapeseed Napin, Shows Anti-Opioid Activity via the Prostaglandin IP Receptor Followed by the Cholecystokinin CCK(2) Receptor in Mice

Rapakinin, Arg-Ile-Tyr, Derived From Rapeseed Napin, Shows Anti-Opioid Activity via the Prostaglandin IP Receptor Followed by the Cholecystokinin CCK(2) Receptor in Mice

Yuko Yamada, Kousaku Ohinata, Andrzej W Lipkowski, Masaaki Yoshikawa

Peptides. 2011 Feb;32(2):281-5.

PMID: 21129424

Abstract:

Rapakinin, Arg-Ile-Tyr, is a vasorelaxing, anti-hypertensive and anorexigenic peptide derived from rapeseed napin. In this study, we found that rapakinin intracerebroventricularly administered to mice inhibited the analgesic effect of morphine, evaluated by the tail-pinch test. The anti-opioid activity of rapakinin was blocked by LY225910, an antagonist of the cholecystokinin (CCK) CCK(2) receptor, but not by lorglumide, an antagonist of the CCK(1) receptor. The anti-opioid activity of rapakinin was also blocked by CAY10441, an antagonist of the prostaglandin (PG) IP receptor. These results suggest that the anti-opioid activity of rapakinin is mediated by the CCK(2) and IP receptors. The anti-opioid activity induced by ciprostene, an IP receptor agonist, was blocked by LY225910, while that of CCK-8 was not blocked by CAY10441. Thus, it is demonstrated that the CCK-CCK(2) system was activated downstream of the PGI(2)-IP receptor system. Taken together, rapakinin shows anti-opioid activity via the activation of the PGI(2)-IP receptor system followed by the CCK-CCK(2) receptor system.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP133040774	LY225910		133040-77-4	Price

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