›› 2004, Vol. 24 ›› Issue (3): 167-171.

• 论文 • 上一篇    下一篇

P2受体与疼痛的实验研究

  

  1. 江西医学院生理学教研室,南昌 330006
  • 收稿日期:2004-05-31 出版日期:2004-01-25 发布日期:2013-03-19
  • 基金资助:

    国家自然科学基金资助项目(No.30260030)

Experimental Investigation of P2 Receptors and Pain

  1. Dept of Physiology, Jiangxi Medical College, Nanchang 330006, China
  • Received:2004-05-31 Online:2004-01-25 Published:2013-03-19

摘要: 嘌呤与嘧啶受体(受体)分为P1和P2受体两大类。P1受体又称为腺苷受体;P2受体是ATP,UTP及其类似物激活的受体,其亚型分为P2X(离子通道型受体)和P2Y(G-蛋白偶联型受体)。P2受体通过与其内源性配体核苷酸结合,参与机体组织器官多种功能的调节,在疼痛病理状态(如神经病理性痛、急性疼痛、炎性痛及内脏痛等),P2受体发挥着重要的介导作用。P2X3受体在感觉神经元中高度表达,通过P2X3受体基因敲除方法,P2X3受体反义寡核苷酸技术和一种新的选择性P2X3受体拮抗剂A-317491的应用,表明P2X3受体在痛觉中发挥重要作用;异聚体P2X2/3受体也涉及疼痛。P2Y受体的某些亚型在感觉神经元中高度表达及其介导的作用,也表明P2Y受体与痛觉有关。P2Y1和P2Y2受体能够引起类似于伤害性反应的细胞兴奋性,P2Y6受体可能是抗损伤。P2受体各亚型的激动剂和拮抗剂有可能为痛觉等病理状态发现新的治疗药物。

关键词: 嘌呤2受体, 三磷酸腺苷, 痛觉

Abstract: Receptors for purines and pyrimidines (P receptors ) could be subdivided into P1 (adenosine) receptors and P2 receptors. P2 receptors were activated preferentially by ATP、UTP and analogs, and P2 receptors subtypes were placed in two major families: P2X (ligand-gated ion channels, LGICs) and P2Y (G protein-coupled receptors, GPCRs).Endogenous nucleotide mediate a lot of functions via cell P2 receptors In many organs, and P2 receptors have crucial mediated roles in the pathologic status of pain (such as neuropathic pain、actuepain、inflanmm-atory pain、visceral pain, and so on).The P2X3-like immunoreactivity and functional expression in sensory neurons and using P2X3 receptor gene knockout and antisense oligonucleotide technologies, A-317491(a novel, selective P2X3 antagonist), demonstrate a crucial role of ATP and P2X3 receptors in pain; the heteromeric P2X2/3 receptor is also involved in pain. In addition, several subtypes of P2Y receptor are also expressed in sensory neurons. P2Y receptors might also be relative with pain.P2Y1 and P2Y2 receptors could generate excitability as nociception, while P2Y6 being antinociceptive. Agonists and antagonists for P2 receptors may provide novel drugs in patho-logic status such as pain.

Key words: P2 receptor, ATP, Pain