瑞替加滨
Retigabine.
作者信息
Porter Roger J, Nohria Virinder, Rundfeldt Chris
机构信息
Department of Pediatrics, School of Medicine, Emory University, Atlanta, Georgia 30322, USA.
出版信息
Neurotherapeutics. 2007 Jan;4(1):149-54. doi: 10.1016/j.nurt.2006.11.012.
Abstract
Retigabine is a novel antiseizure drug that acts through potassium channels and has activity in a broad range of animal models of epilepsy. It is also effective in several preclinical pain models. The drug has been extensively studied in phase I and II studies, with very promising results. The maximal tolerated dose for most patients is 1,200 mg/day. Adverse effects have been largely CNS-related and mild; most have occurred during the titration periods in the various studies. At present, retigabine is in two pivotal phase III studies.
摘要
瑞替加滨是一种新型抗癫痫药物，通过钾通道发挥作用，在多种癫痫动物模型中均有活性。它在几种临床前疼痛模型中也有效。该药物已在I期和II期研究中进行了广泛研究，结果非常有前景。大多数患者的最大耐受剂量为1200毫克/天。不良反应主要与中枢神经系统相关且较为轻微；大多数发生在各项研究的滴定期。目前，瑞替加滨正处于两项关键的III期研究中。
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本文引用的文献
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The anti-hyperalgesic activity of retigabine is mediated by KCNQ potassium channel activation.瑞替加滨的抗痛觉过敏活性是由KCNQ钾通道激活介导的。
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The anticonvulsant retigabine attenuates nociceptive behaviours in rat models of persistent and neuropathic pain.抗惊厥药物瑞替加滨可减轻持续性疼痛和神经性疼痛大鼠模型中的伤害性反应行为。
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KCNQ4, a K+ channel mutated in a form of dominant deafness, is expressed in the inner ear and the central auditory pathway.KCNQ4是一种在一种显性耳聋形式中发生突变的钾离子通道，在内耳和中枢听觉通路中表达。
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The novel anticonvulsant retigabine activates M-currents in Chinese hamster ovary-cells tranfected with human KCNQ2/3 subunits.新型抗惊厥药瑞替加滨可激活转染人KCNQ2/3亚基的中国仓鼠卵巢细胞中的M电流。
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Effects of retigabine (D-23129) on different patterns of epileptiform activity induced by low magnesium in rat entorhinal cortex hippocampal slices.瑞替加滨（D - 23129）对低镁诱导的大鼠内嗅皮层海马切片不同模式癫痫样活动的影响。
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