Carey F, Haworth D, Whalley E T
Bioscience Department II, ICI Pharmaceuticals Division, Macclesfield, Cheshire, U.K.
Eur J Pharmacol. 1988 Oct 26;156(1):161-4. doi: 10.1016/0014-2999(88)90159-8.
A comparison of the effects of bradykinin (BK), sigma-cyclo-BK and sigma-cyclo-kallidin (sigma-cyclo-KD) to induce oedema, hyperalgesia and blood flow in the rat paw was made. BK produced dose-dependent increases in oedema and blood flow and a reduction in the nociceptive pressure threshold. Sigma-Cyclo-BK and sigma-cyclo-KD were more potent than BK at inducing oedema and increasing blood flow but had no effect on nociceptive pressure threshold at the doses used. The relative lack of hyperalgesic activity of sigma-cyclo-BK and sigma-cyclo-KD compared with BK raises the possibility of differences between kinin receptors mediating permeability and blood flow changes and those involved in nociception in this model.
比较了缓激肽(BK)、σ-环化BK和σ-环化胰激肽(σ-环化KD)对大鼠爪部诱导水肿、痛觉过敏和血流的影响。BK产生剂量依赖性的水肿和血流增加以及伤害性压力阈值降低。σ-环化BK和σ-环化KD在诱导水肿和增加血流方面比BK更有效,但在所使用的剂量下对伤害性压力阈值没有影响。与BK相比,σ-环化BK和σ-环化KD相对缺乏痛觉过敏活性,这增加了在该模型中介导通透性和血流变化的激肽受体与参与痛觉的受体之间存在差异的可能性。