痛觉和TRP通道。

Current drug targets. CNS and neurological disorders Pub Date : 2004-12-01 DOI:10.2174/1568007043336789

Mitsuko Numazaki, Makoto Tominaga

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引用次数: 27

摘要

有害的热、机械或化学刺激通过刺激被称为伤害感受器的外周末梢来引起疼痛，许多种类的嗜离子性和代谢性感受器参与了这一过程。辣椒素受体TRPV1是一种伤害受体特异性离子通道，是辣椒素的分子靶点。TRPV1不仅可以被辣椒素激活，也可以被有毒的热量(热阈值>43摄氏度)或质子(酸化)激活，所有这些都是已知的在体内引起疼痛的物质。对TRPV1缺陷小鼠的研究表明，TRPV1对疼痛感觉的选择性模式和热痛觉过敏至关重要。由组织损伤/炎症引发并以超敏性为特征的炎症性疼痛的一种机制是TRPV1的致敏。哺乳动物除TRPV1外，还有5个热敏离子通道，均属于TRP (transient receptor potential，瞬时受体电位)超家族。这些包括TRPV2, TRPV3, TRPV4, TRPM8和TRPA1。这些通道表现出不同的热激活阈值(TRPV2 > 52℃，TRPV3 >约34-38℃，TRPV4 >约27-35℃，TRPM8 <约25-28℃，TRPA1 < 17℃)，并在初级感觉神经元和其他组织中表达。一些热敏TRP通道可能与热痛觉有关，因为它们的激活阈值在有害的温度范围内。

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Nociception and TRP Channels.

Pain is initiated when noxious stimuli excite the peripheral terminals of specialized primary afferent neurons called nociceptors. Many molecules are involved in conversion of the noxious stimuli to the electrical signals in the nociceptor endings. Among them, TRP channels play important roles in detecting noxious stimuli.

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Current drug targets. CNS and neurological disorders

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