Costello A H, Hargreaves K M
Neurobiology and Anesthesiology Branch, National Institutes of Health, Bethesda, MD 20892.
Eur J Pharmacol. 1989 Nov 21;171(2-3):259-63. doi: 10.1016/0014-2999(89)90118-0.
Although bradykinin (BK) antagonists have antinociceptive effects, they have not been evaluated for anti-inflammatory activity. When administered with carrageenan into the rat hindpaw, NPC567 significantly blocked carrageenan-induced hyperalgesia, hyperthermia and edema. In addition, NPC567 did not alter the in vitro release of immunoreactive BK by plasma kallikrein. These results indicate that the antinociceptive activity of NPC567, a BK antagonist, may be related to its overall anti-inflammatory activity and that is mechanism of action does not include inhibition of plasma kallikrein.
尽管缓激肽(BK)拮抗剂具有抗伤害感受作用,但尚未对其抗炎活性进行评估。当与角叉菜胶一起注射到大鼠后爪时,NPC567能显著阻断角叉菜胶诱导的痛觉过敏、体温过高和水肿。此外,NPC567不会改变血浆激肽释放酶引起的免疫反应性BK的体外释放。这些结果表明,BK拮抗剂NPC567的抗伤害感受活性可能与其整体抗炎活性有关,并且其作用机制不包括抑制血浆激肽释放酶。