期刊
PEPTIDES
卷 30, 期 7, 页码 1348-1354出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.peptides.2009.04.002
关键词
Human opiorphin; Antinociception; Opioid receptor; Enkephalins; Neutral endopeptidase; Aminopeptidase N
资金
- National Nature Science Foundation of China [J0630644]
In the present study, we investigated the effects of human opiorphin on colonic motility and nociception in mice. In in vitro bioassay, opiorphin (10(-6) to 10(-4) M) caused colonic contraction in a concentration-dependent manner, which was completely blocked by naloxone and partially attenuated by beta-funaltrexamine and naltrindole. Moreover, opiorphin (10(-4) M) significantly enhanced the contractile response induced by Met-enkephalin. The data suggested that the effect of opiorphin on colonic contraction may be due to the protection of enkephalins. In in vivo bioassay, intracerebroventricular (i.c.v.) administration of opiorphin (1.25-10 mu g/kg) dose- and time-dependently induced potent analgesic effect (ED50 = 3.22 mu g/kg). This effect was fully blocked by naloxone and significantly inhibited by co-injection (i.c.v.) with beta-funaltrexamine or naltrindole, but not by nor-binaltorphimine, indicating the involvement of both mu- and delta-opioid receptors in the analgesic response evoked by opiorphin. In addition, i.c.v. administration of 5 mu g/kg opiorphin produced the comparative effect as 10 mu g/kg morphine on the analgesia, suggesting that opiorphin displayed more potent analgesic effect than that induced by morphine. (C) 2009 Elsevier Inc. All rights reserved.
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