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新生大鼠体外模型中周围神经和脊髓缓激肽受体的激活

Activation of a bradykinin receptor in peripheral nerve and spinal cord in the neonatal rat in vitro.

作者信息

Dray A, Bettaney J, Forster P, Perkins M N

机构信息

Sandoz Institute for Medical Research, London.

出版信息

Br J Pharmacol. 1988 Dec;95(4):1008-10. doi: 10.1111/j.1476-5381.1988.tb11732.x.

DOI:10.1111/j.1476-5381.1988.tb11732.x
PMID:2905907
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1854282/
Abstract

In an in vitro preparation of the neonatal rat spinal cord with attached tail, administration of bradykinin (Bk) to the spinal cord or to the tail produced depolarization of a ventral root (L3-L5). The effect of Bk at each site was selectively and reversibly antagonized by D-Arg [Hyp2, Thi5,8 D-Phe7]-Bk but could not be mimicked or antagonized by the B1-receptor ligands [des-Arg9]-Bk or Leu8[des-Arg9]-Bk, respectively. Peripherally evoked noxious responses produced by capsaicin or heat, were unaffected by either antagonist administered to the spinal cord. These data suggest that Bk-evoked responses in the spinal cord and at peripheral nociceptors were mediated via a receptor which by definition is of the B2-type. Additionally Bk is unlikely to be a physiological mediator of acute nociception in the spinal cord.

摘要

在带有尾巴的新生大鼠脊髓的体外制备物中，向脊髓或尾巴施用缓激肽（Bk）会导致腹根（L3 - L5）去极化。D - Arg [Hyp2, Thi5,8 D - Phe7] - Bk可选择性且可逆地拮抗Bk在每个部位的作用，但B1受体配体[des - Arg9] - Bk或Leu8[des - Arg9] - Bk分别无法模拟或拮抗其作用。辣椒素或热引起的外周诱发伤害性反应，不受施用于脊髓的任何一种拮抗剂的影响。这些数据表明，脊髓和外周伤害感受器中Bk诱发的反应是通过一种根据定义属于B2型的受体介导的。此外，Bk不太可能是脊髓中急性伤害感受的生理介质。

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本文引用的文献

1
Bradykinin analogue blocks bradykinin-induced inhibition of a spinal nociceptive reflex in the rat.缓激肽类似物可阻断缓激肽诱导的大鼠脊髓伤害性反射抑制。
Eur J Pharmacol. 1987 Jun 4;137(2-3):281-5. doi: 10.1016/0014-2999(87)90237-8.
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New synthetic antagonists of bradykinin.缓激肽的新型合成拮抗剂。
Br J Pharmacol. 1987 Dec;92(4):851-5. doi: 10.1111/j.1476-5381.1987.tb11390.x.
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Bradykinin analogues: differential agonist and antagonist activities suggesting multiple receptors.缓激肽类似物：不同的激动剂和拮抗剂活性提示存在多种受体。
Br J Pharmacol. 1988 May;94(1):3-5. doi: 10.1111/j.1476-5381.1988.tb11492.x.
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Bradykinin as a pain mediator: receptors are localized to sensory neurons, and antagonists have analgesic actions.缓激肽作为一种疼痛介质：其受体定位于感觉神经元，拮抗剂具有镇痛作用。
Proc Natl Acad Sci U S A. 1988 May;85(9):3245-9. doi: 10.1073/pnas.85.9.3245.
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