• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

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.

DOI:10.1016/j.nurt.2006.11.012
PMID:17199031
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7479689/
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。

相似文献

1
Retigabine.瑞替加滨
Neurotherapeutics. 2007 Jan;4(1):149-54. doi: 10.1016/j.nurt.2006.11.012.
2
Retigabine: chemical synthesis to clinical application.瑞替加滨:从化学合成到临床应用
CNS Drug Rev. 2005 Spring;11(1):1-20. doi: 10.1111/j.1527-3458.2005.tb00033.x.
3
Retigabine (ezogabine): in partial-onset seizures in adults with epilepsy.雷替加滨(依佐加滨):用于治疗成人癫痫部分发作。
CNS Drugs. 2011 Oct 1;25(10):887-900. doi: 10.2165/11205950-000000000-00000.
4
Retigabine: the newer potential antiepileptic drug.雷替加滨:一种较新的潜在抗癫痫药物。
Pharmacol Rep. 2010 Mar-Apr;62(2):211-9. doi: 10.1016/s1734-1140(10)70260-7.
5
The novel dual-mechanism Kv7 potassium channel/TSPO receptor activator GRT-X is more effective than the Kv7 channel opener retigabine in the 6-Hz refractory seizure mouse model.新型双重机制 Kv7 钾通道/TSPO 受体激动剂 GRT-X 在 6-Hz 难治性癫痫小鼠模型中的疗效优于 Kv7 通道开放剂瑞替加滨。
Neuropharmacology. 2022 Feb 1;203:108884. doi: 10.1016/j.neuropharm.2021.108884. Epub 2021 Nov 14.
6
Retigabine: in partial seizures.瑞替加滨:用于部分性癫痫发作。
CNS Drugs. 2006;20(7):601-8; discussion 609-10. doi: 10.2165/00023210-200620070-00005.
7
Potent KCNQ2/3-specific channel activator suppresses in vivo epileptic activity and prevents the development of tinnitus.强效KCNQ2/3特异性通道激活剂可抑制体内癫痫活动并预防耳鸣的发生。
J Neurosci. 2015 Jun 10;35(23):8829-42. doi: 10.1523/JNEUROSCI.5176-14.2015.
8
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。
Epilepsia. 2012 Mar;53(3):425-36. doi: 10.1111/j.1528-1167.2011.03364.x. Epub 2012 Jan 5.
9
Retigabine: fewer drug interactions.瑞替加滨:药物相互作用较少。
Prescrire Int. 2012 Mar;21(125):61.
10
Pharmacogenetics of KCNQ channel activation in 2 potassium channelopathy mouse models of epilepsy.KCNQ 通道激活的药物遗传学在 2 种癫痫钾通道病小鼠模型中的作用。
Epilepsia. 2018 Feb;59(2):358-368. doi: 10.1111/epi.13978. Epub 2017 Dec 19.

引用本文的文献

1
Insights into ion channels to identify drug target for neuropathic pain management.深入了解离子通道以确定用于治疗神经性疼痛的药物靶点。
Inflammopharmacology. 2025 Aug 12. doi: 10.1007/s10787-025-01899-4.
2
Identifying the mechanism of action of the Kv7 channel opener, retigabine in the treatment of epilepsy.确定钾离子通道开放剂瑞替加滨治疗癫痫的作用机制。
Neurol Sci. 2023 Nov;44(11):3819-3825. doi: 10.1007/s10072-023-06955-x. Epub 2023 Jul 13.
3
Application of Sensitivity Analysis to Discover Potential Molecular Drug Targets.敏感性分析在发现潜在分子药物靶标中的应用。
Int J Mol Sci. 2022 Jun 13;23(12):6604. doi: 10.3390/ijms23126604.
4
Alternative Targets for Modulators of Mitochondrial Potassium Channels.线粒体钾通道调节剂的替代靶标。
Molecules. 2022 Jan 4;27(1):299. doi: 10.3390/molecules27010299.
5
KCNQ Channels in the Mesolimbic Reward Circuit Regulate Nociception in Chronic Pain in Mice.中脑边缘奖赏回路中的 KCNQ 通道调节小鼠慢性痛觉过敏。
Neurosci Bull. 2021 May;37(5):597-610. doi: 10.1007/s12264-021-00668-x. Epub 2021 Apr 26.
6
Carbamate group as structural motif in drugs: a review of carbamate derivatives used as therapeutic agents.氨基甲酸酯基团作为药物中的结构基序:用作治疗剂的氨基甲酸酯衍生物综述。
Arh Hig Rada Toksikol. 2020 Dec 31;71(4):285-299. doi: 10.2478/aiht-2020-71-3466.
7
Copper mediated C-H amination with oximes: en route to primary anilines.铜介导的肟参与的C-H胺化反应:通往伯苯胺的途径。
Chem Sci. 2018 May 14;9(23):5160-5164. doi: 10.1039/c8sc01256c. eCollection 2018 Jun 21.
8
Antiepileptic drugs in development pipeline: A recent update.处于研发阶段的抗癫痫药物:近期进展
eNeurologicalSci. 2016 Jun 17;4:42-51. doi: 10.1016/j.ensci.2016.06.003. eCollection 2016 Sep.
9
Activation of KCNQ channels located on the skeletal muscle membrane by retigabine and its influence on the maximal muscle force in rat muscle strips.瑞替加滨对位于骨骼肌膜上的KCNQ通道的激活作用及其对大鼠肌条最大肌力的影响。
Naunyn Schmiedebergs Arch Pharmacol. 2016 Apr;389(4):439-46. doi: 10.1007/s00210-016-1211-0. Epub 2016 Jan 27.
10
The Sensorless Pore Module of Voltage-gated K+ Channel Family 7 Embodies the Target Site for the Anticonvulsant Retigabine.电压门控钾离子通道家族7的无传感器孔模块是抗惊厥药瑞替加滨的作用靶点。
J Biol Chem. 2016 Feb 5;291(6):2931-7. doi: 10.1074/jbc.M115.683185. Epub 2015 Dec 1.

本文引用的文献

1
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。
Naunyn Schmiedebergs Arch Pharmacol. 2004 Apr;369(4):382-90. doi: 10.1007/s00210-004-0881-1. Epub 2004 Mar 9.
2
The therapeutic potential of neuronal KCNQ channel modulators.神经元KCNQ通道调节剂的治疗潜力。
Expert Opin Ther Targets. 2003 Dec;7(6):737-48. doi: 10.1517/14728222.7.6.737.
3
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。
Eur J Pharmacol. 2003 Jan 24;460(2-3):109-16. doi: 10.1016/s0014-2999(02)02924-2.
4
Delayed sclerosis, neuroprotection, and limbic epileptogenesis after status epilepticus in the rat.大鼠癫痫持续状态后的迟发性硬化、神经保护和边缘叶癫痫发生
Epilepsia. 2002;43 Suppl 5:86-95. doi: 10.1046/j.1528-1157.43.s.5.39.x.
5
Effects of retigabine on rhythmic synchronous activity of human neocortical slices.
Epilepsy Res. 2001 May;44(2-3):155-65. doi: 10.1016/s0920-1211(01)00193-0.
6
Investigations into the mechanism of action of the new anticonvulsant retigabine. Interaction with GABAergic and glutamatergic neurotransmission and with voltage gated ion channels.新型抗惊厥药瑞替加滨的作用机制研究。与γ-氨基丁酸能和谷氨酸能神经传递以及电压门控离子通道的相互作用。
Arzneimittelforschung. 2000 Dec;50(12):1063-70. doi: 10.1055/s-0031-1300346.
7
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。
Proc Natl Acad Sci U S A. 2000 Apr 11;97(8):4333-8. doi: 10.1073/pnas.97.8.4333.
8
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。
Neurosci Lett. 2000 Mar 17;282(1-2):73-6. doi: 10.1016/s0304-3940(00)00866-1.
9
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。
Epilepsia. 2000 Jan;41(1):28-33. doi: 10.1111/j.1528-1157.2000.tb01501.x.
10
Characterization of the K+ channel opening effect of the anticonvulsant retigabine in PC12 cells.
Epilepsy Res. 1999 Jun;35(2):99-107. doi: 10.1016/s0920-1211(98)00131-4.