Klinik für Anaesthesiologie und Operative Intensivmedizin, Campus Benjamin Franklin, Berlin, Germany.
Anesthesiology. 2012 Feb;116(2):448-57. doi: 10.1097/ALN.0b013e318242b2ea.
Kinins (e.g., bradykinin) acting through the constitutively expressed B2 and the injury-induced B1 receptors are involved in pain and hyperalgesia, as previously shown by use of receptor-selective antagonists and single-receptor knockout models. Because the overall contribution of kinins to painful processes remains unclear, the aim of this study was to analyze pain-related behaviors of mice unable to respond to kinins because of a lack of both B1 and B2 receptors.
In knockout mice lacking both B1 and B2 receptors and in wild-type mice (n = 8-21 per group) the authors assessed nociceptive thresholds to mechanical and heat stimuli (von Frey and Hargreaves tests, respectively) in healthy animals and after induction of inflammatory and neuropathic pain, acid-induced visceral nociception, and modulation of nociceptive responses by peripherally administered opioid agonists.
In knockout mice lacking both B1 and B2 receptors baseline nociceptive responses to heat were unaltered, nocifensive responses to bradykinin were abolished, acute acetic acid-induced visceral nociception was reduced by approximately 70% (mean difference: 19.5 writhes/30 min) and heat hypersensitivity in carrageenan-induced paw inflammation was decreased 48 h after injection (mean difference 2.88 s), hypersensitivities in chronic complete Freund's adjuvant-induced paw inflammation or after chronic constriction injury of the sciatic nerve were unchanged, and peripheral μ- and δ-opioid-induced analgesia after chronic constriction injury was reduced by 30-35% (mean differences: μ-agonist: 0.495 g, δ-agonist: 0.555 g).
These data suggest that kinins are important for nociception associated with acute short-lasting inflammation but are less essential in chronic stages of pain. The results also highlight a new protective function of kinins via interactions with the opioid system.
先前使用受体选择性拮抗剂和单受体基因敲除模型的研究表明,激肽(例如缓激肽)通过组成型表达的 B2 受体和损伤诱导的 B1 受体发挥作用,参与疼痛和痛觉过敏。由于激肽对疼痛过程的总体贡献仍不清楚,因此本研究的目的是分析由于缺乏 B1 和 B2 受体而无法对激肽产生反应的小鼠的疼痛相关行为。
在缺乏 B1 和 B2 受体的基因敲除小鼠和野生型小鼠(每组 8-21 只)中,作者评估了健康动物和诱导炎症和神经病理性疼痛、酸诱导内脏疼痛以及外周给予阿片类激动剂对疼痛反应的调制后,对机械和热刺激的痛觉阈值(分别使用 von Frey 和 Hargreaves 测试)。
在缺乏 B1 和 B2 受体的基因敲除小鼠中,基线热痛觉反应不受影响,缓激肽的伤害性反应被消除,急性醋酸引起的内脏疼痛减少了约 70%(平均差异:19.5 次扭体/30 分钟),并且在注射后 48 小时,角叉菜胶诱导的爪炎症中的热敏感性降低了 48 小时(平均差异 2.88 秒),慢性完全弗氏佐剂诱导的爪炎症或坐骨神经慢性缩窄性损伤后的超敏反应保持不变,慢性缩窄性损伤后的外周 μ-和 δ-阿片类诱导镇痛减少了 30-35%(平均差异:μ-激动剂:0.495 g,δ-激动剂:0.555 g)。
这些数据表明,激肽在与急性短暂炎症相关的伤害感受中很重要,但在慢性疼痛阶段则不那么重要。结果还突出了激肽通过与阿片系统相互作用的新的保护功能。