Bradykinin as a pain mediator: receptors are localized to sensory neurons, and antagonists have analgesic actions.

Bradykinin as a pain mediator: receptors are localized to sensory neurons, and antagonists have analgesic actions.
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缓激肽作为疼痛介质:受体定位于感觉神经元,拮抗剂具有镇痛作用。

DOI:
10.1073/pnas.85.9.3245
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发表时间:
1988
影响因子:
11.1
通讯作者:
Snyder,SH
Snyder,SH
中科院分区:
综合性期刊1区
文献类型:
--
作者:
Steranka,LR;Manning,DC;DeHaas,CJ;Ferkany,JW;Borosky,SA;Connor,JR;Vavrek,RJ;Stewart,JM;Snyder,SH

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放射自显影研究将[3H]缓激肽受体结合位点定位于豚鼠的胶状质、背根以及背根和三叉神经节中的小细胞亚群。在心肌/冠状动脉内脏传入纤维上也观察到[3H]缓激肽标记。[3H]缓激肽受体定位于伤害性通路支持缓激肽在疼痛介导中的作用。几种缓激肽拮抗剂阻断缓激肽诱导的大鼠急性血管痛。缓激肽拮抗剂也缓解缓激肽和尿酸盐诱导的大鼠爪痛敏。这些结果表明,缓激肽是疼痛的生理介质,缓激肽拮抗剂在急性和慢性疼痛模型中具有镇痛活性。
Autoradiographic studies localize [3H]bradykinin receptor binding sites to the substantia gelatinosa, dorsal root, and a subset of small cells in both the dorsal root and trigeminal ganglia of the guinea pig. [3H]Bradykinin labeling is also observed over myocardial/coronary visceral afferent fibers. The localization of [3H]bradykinin receptors to nociceptive pathways supports a role for bradykinin in pain mediation. Several bradykinin antagonists block bradykinin-induced acute vascular pain in the rat. The bradykinin antagonists also relieve bradykinin- and urate-induced hyperalgesia in the rat paw. These results indicate that bradykinin is a physiologic mediator of pain and that bradykinin antagonists have analgesic activity in both acute and chronic pain models.