一个人的副作用是另一个人的治疗机会：靶向平滑肌疾病中的 Kv7 通道。
One man's side effect is another man's therapeutic opportunity: targeting Kv7 channels in smooth muscle disorders.
机构信息
Division of Biomedical Sciences, St George's, University of London, Cranmer Terrace, UK.
出版信息
Br J Pharmacol. 2013 Jan;168(1):19-27. doi: 10.1111/j.1476-5381.2012.02133.x.
Abstract
Retigabine is a first in class anticonvulsant that has recently undergone clinical trials to test its efficacy in epileptic patients. Retigabine's novel mechanism of action - activating Kv7 channels - suppresses neuronal activity to prevent seizure generation by hyperpolarizing the membrane potential and suppressing depolarizing surges. However, Kv7 channels are not expressed exclusively in neurones and data generated over the last decade have shown that Kv7 channels play a key role in various smooth muscle systems of the body. This review discusses the potential of targeting Kv7 channels in the smooth muscle to treat diseases such as hypertension, bladder instability, constipation and preterm labour.
摘要
瑞替加滨是一种新型抗癫痫药物，最近已进行临床试验以测试其在癫痫患者中的疗效。瑞替加滨的新颖作用机制——激活 Kv7 通道——通过超极化膜电位和抑制去极化波来抑制神经元活动，从而防止癫痫发作。然而，Kv7 通道并非仅在神经元中表达，过去十年的数据表明，Kv7 通道在体内各种平滑肌系统中发挥着关键作用。本文综述了针对平滑肌 Kv7 通道治疗高血压、膀胱不稳定、便秘和早产等疾病的潜力。
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本文引用的文献
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The urinary safety profile and secondary renal effects of retigabine (ezogabine): a first-in-class antiepileptic drug that targets KCNQ (K(v)7) potassium channels.瑞替加滨（依佐加滨）的尿安全性概况和继发性肾脏影响：一种靶向 KCNQ（K(v)7）钾通道的首创抗癫痫药物。
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Ezogabine AKA Retigabine: Is More Better? Trying to Find the Right Dose From Clinical Trials.依佐加滨又名瑞替加滨：越多越好吗？试图从临床试验中找到合适剂量。
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Reduced KCNQ4-encoded voltage-dependent potassium channel activity underlies impaired β-adrenoceptor-mediated relaxation of renal arteries in hypertension.在高血压中，KCNQ4 编码的电压依赖性钾通道活性降低，导致肾脏动脉β-肾上腺素能受体介导的松弛受损。
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Clinical utility of adjunctive retigabine in partial onset seizures in adults.辅助瑞替加滨治疗成人部分发作性癫痫的临床效用。
Ther Clin Risk Manag. 2012;8:7-14. doi: 10.2147/TCRM.S22605. Epub 2012 Jan 20.
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Pharmacological dissection of K(v)7.1 channels in systemic and pulmonary arteries.K(v)7.1 通道在体循环和肺循环动脉中的药理学剖析。
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The spectrum of anticonvulsant efficacy of retigabine (ezogabine) in animal models: implications for clinical use.雷替加滨（依佐加滨）在动物模型中的抗惊厥疗效谱：对临床应用的影响。
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The mechanism of action of retigabine (ezogabine), a first-in-class K+ channel opener for the treatment of epilepsy.瑞替加滨（依佐加滨）作用机制，一种用于癫痫治疗的首个钾通道开放剂。
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Novel medications for epilepsy.新型抗癫痫药物。
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Driving with no brakes: molecular pathophysiology of Kv7 potassium channels.无刹车驾驶：Kv7 钾通道的分子病理生理学。
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