TRP channels and analgesia.
TRP channels and analgesia.
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DOI：
10.1016/j.lfs.2012.08.010
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发表时间：
2013-03-19
期刊：
影响因子：
6.1
通讯作者：
Abooj M
中科院分区：
文献类型：
--
作者：
Premkumar LS;Abooj M
自从克隆和表征第一个伤害性离子通道瞬时受体电位 (TRP) Vanilloid 1 (TRPV1) 以来，其他参与伤害感受的 TRP 通道也已被克隆和表征，其中包括 TRP Vanilloid 2 (TRPV2)、TRP Vanilloid 3 (TRPV3)、TRP Vanilloid 4 (TRPV4)、TRP 锚蛋白 1 (TRPA1) 和 TRP Melastatin 8 (TRPM8)，最近的 TRP Canonical 1, 5, 6 (TRPC1, 5, 6)，TRP Melastatin 2 (TRPM2) 和 TRP Melastatin 3 (TRPM3)。这些通道主要在 C 和 Aδ 伤害感受器中表达，并传递有害的热、机械和化学敏感性。 TRP 通道受促炎介质、神经肽和细胞因子调节。通过拮抗剂或激动剂针对这些受体来治疗疼痛状况已经取得了重大进展。在这篇综述中，我们将讨论 TRP 通道作为下一代镇痛药的靶点，以及由于阻断/激活这些受体而可能产生的副作用，因为它们还涉及生理功能，如血管活性神经肽的释放和血管张力的调节、体温的维持、胃肠道运动、膀胱控制等。
Since cloning and characterizing the first nociceptive ion channel Transient Receptor Potential (TRP) Vanilloid 1 (TRPV1), other TRP channels involved in nociception have been cloned and characterized, which include TRP Vanilloid 2 (TRPV2), TRP Vanilloid 3 (TRPV3), TRP Vanilloid 4 (TRPV4), TRP Ankyrin 1 (TRPA1) and TRP Melastatin 8 (TRPM8), more recently TRP Canonical 1, 5, 6 (TRPC1, 5, 6), TRP Melastatin 2 (TRPM2) and TRP Melastatin 3 (TRPM3). These channels are predominantly expressed in C and Aδ nociceptors and transmit noxious thermal, mechanical and chemical sensitivities. TRP channels are modulated by pro-inflammatory mediators, neuropeptides and cytokines. Significant advances have been made targeting these receptors either by antagonists or agonists to treat painful conditions. In this review, we will discuss TRP channels as targets for next generation analgesics and the side effects that may ensue as a result of blocking/activating these receptors, because they are also involved in physiological functions such as release of vasoactive neuropeptides and regulation of vascular tone, maintenance of the body temperature, gastrointestinal motility, urinary bladder control etc.