Molecular Nociception Group, Wolfson Institute for Biomedical Research, University College London, London WC1E 6BT, UK.
J Physiol. 2010 Jun 1;588(Pt 11):1897-904. doi: 10.1113/jphysiol.2010.187807. Epub 2010 Feb 8.
Pain remains a major clinical challenge, severely afflicting around 6% of the population at any one time. Channelopathies that underlie monogenic human pain syndromes are of great clinical relevance, as cell surface ion channels are tractable drug targets. The recent discovery that loss-of-function mutations in the sodium channel Nav1.7 underlie a recessive pain-free state in otherwise normal people is particularly significant. Deletion of channel-encoding genes in mice has also provided insights into mammalian pain mechanisms. Ion channels expressed by immune system cells (e.g. P2X7) have been shown to play a pivotal role in changing pain thresholds, whilst channels involved in sensory transduction (e.g. TRPV1), the regulation of neuronal excitability (potassium channels), action potential propagation (sodium channels) and neurotransmitter release (calcium channels) have all been shown to be potentially selective analgesic drug targets in some animal pain models. Migraine and visceral pain have also been associated with voltage-gated ion channel mutations. Insights into such channelopathies thus provide us with a number of potential targets to control pain.
疼痛仍然是一个主要的临床挑战,大约每 6%的人口在任何时候都会受到严重影响。导致单基因人类疼痛综合征的通道病与临床密切相关,因为细胞膜离子通道是可治疗的药物靶点。最近发现,钠离子通道 Nav1.7 的功能丧失性突变会导致正常人出现隐性无痛状态,这一点尤其重要。在小鼠中删除编码通道的基因也为哺乳动物疼痛机制提供了新的见解。免疫系统细胞表达的离子通道(如 P2X7)已被证明在改变疼痛阈值方面发挥着关键作用,而参与感觉转导(如 TRPV1)、神经元兴奋性调节(钾通道)、动作电位传播(钠通道)和神经递质释放(钙通道)的通道也已被证明在一些动物疼痛模型中是潜在的选择性镇痛药靶点。偏头痛和内脏疼痛也与电压门控离子通道突变有关。因此,对这些通道病的深入了解为我们提供了许多控制疼痛的潜在靶点。
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