Rush Anthony M, Cummins Theodore R
NeuroSolutions Ltd., Coventry CV4 7ZS, UK.
Mol Interv. 2007 Aug;7(4):192-5, 180. doi: 10.1124/mi.7.4.4.
Voltage-gated sodium channels in nociceptive neurons are attractive targets for novel pain therapeutics. Although drugs that target voltage-gated sodium channels have proven value as pain therapeutics, the drugs that are currently available are non-specific sodium channel inhibitors, which limit their usefulness. Recently, a selective small-molecule inhibitor of Na(v)1.8, a voltage-gated sodium channel isoform that participates in peripheral pain mechanisms, has been developed. This exciting new compound shows efficacy in several animal models of pain and is anticipated to be only the first of many new isoform-specific sodium channel blockers.
伤害性神经元中的电压门控钠通道是新型疼痛治疗药物的有吸引力的靶点。尽管靶向电压门控钠通道的药物已被证明具有作为疼痛治疗药物的价值，但目前可用的药物是非特异性钠通道抑制剂，这限制了它们的效用。最近，已开发出一种选择性小分子抑制剂，作用于Na(v)1.8，这是一种参与外周疼痛机制的电压门控钠通道亚型。这种令人兴奋的新化合物在几种疼痛动物模型中显示出疗效，预计它只是众多新型亚型特异性钠通道阻滞剂中的第一个。
