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 |
| |
Authors: | Yamada Yuko Ohinata Kousaku Lipkowski Andrzej W Yoshikawa Masaaki |
| |
Institution: | a Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Gokasho, Uji, Kyoto 611-0011, Japan b Medical Research Centre, Polish Academy of Sciences, 02106 Warsaw, Poland c Frontier Research Center, Graduate School of Engineering, Osaka University, Suita, Osaka 565-0871, Japan |
| |
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) CCK2 receptor, but not by lorglumide, an antagonist of the CCK1 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 CCK2 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-CCK2 system was activated downstream of the PGI2-IP receptor system. Taken together, rapakinin shows anti-opioid activity via the activation of the PGI2-IP receptor system followed by the CCK-CCK2 receptor system. |
| |
Keywords: | Anti-opioid activity Rapakinin Prostaglandin I2 IP receptor Cholecystokinin CCK2 receptor |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|