Transient receptor potential channels: targeting pain at the source.

Transient receptor potential channels: targeting pain at the source.
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DOI:
10.1038/nrd2757
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发表时间:
2009-01
期刊:
Nature reviews. Drug discovery
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--
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--
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其他
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疼痛是由中枢神经系统不同水平的神经信号的复杂处理引起的,每个信号都可能提供多种药物干预机会。开发新型止痛药的一个合乎逻辑的策略是瞄准疼痛通路的起点,并将潜在的治疗直接瞄准伤害性感受器--检测伤害性刺激的高阈值初级感觉神经元。在伤害性感受器中作为伤害性刺激检测器的最大受体是瞬时受体电位(Trp)通道家族。这篇综述重点介绍了支持特定Trp通道作为镇痛剂靶点的证据,指出了Trp通道作用药物的可能疗效,并讨论了在人体上测试候选镇痛剂所需的开发途径。
Pain results from the complex processing of neural signals at different levels of the central nervous system, with each signal potentially offering multiple opportunities for pharmacological intervention. A logical strategy for developing novel analgesics is to target the beginning of the pain pathway, and aim potential treatments directly at the nociceptors — the high-threshold primary sensory neurons that detect noxious stimuli. The largest group of receptors that function as noxious stimuli detectors in nociceptors is the transient receptor potential (TRP) channel family. This Review highlights evidence supporting particular TRP channels as targets for analgesics, indicates the likely efficacy profiles of TRP-channel-acting drugs, and discusses the development pathways needed to test candidates as analgesics in humans.
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