Ranolazine attenuates behavioral signs of neuropathic pain.
Ranolazine attenuates behavioral signs of neuropathic pain.
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DOI：
10.1097/fbp.0b013e3283323c90
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发表时间：
2009-12
影响因子：
1.6
通讯作者：
Taylor BK
中科院分区：
文献类型：
--
作者：
Gould HJ 3rd;Garrett C;Donahue RR;Paul D;Diamond I;Taylor BK
雷诺嗪调节心脏电压门控钠通道（Nav 1.5），FDA批准用于治疗缺血性心脏病。雷诺嗪还靶向参与神经性疼痛的神经元（Nav 1.7，1.8）亚型。因此，我们确定雷诺嗪在神经性疼痛的临床前动物模型中的镇痛功效。雷诺嗪的腹腔注射和口服给药均剂量依赖性地抑制与备用神经损伤相关的机械性和冷异常性疼痛，而不产生共济失调或其他行为副作用。这些数据保证雷诺嗪在治疗神经性疼痛中的潜在用途的临床研究。
Ranolazine modulates the cardiac voltage-gated sodium channel (Nav 1.5) and is FDA-approved for the treatment of ischemic heart disease. Ranolazine also targets neuronal (Nav 1.7, 1.8) isoforms that are implicated in neuropathic pain. Therefore, we determined the analgesic efficacy of ranolazine in a pre-clinical animal model of neuropathic pain. Both i.p. and oral administration of ranolazine dose-dependently inhibited the mechanical and cold allodynia associated with spared nerve injury, without producing ataxia or other behavioral side effects. These data warrant clinical investigation of the potential use of ranolazine in the treatment of neuropathic pain.