retigabine anti-hyperalgesic活动是由KCNQ钾通道激活。
文章的细节
-
引用
复制到剪贴板 -
难道R,罗斯托克,Rundfeldt C
retigabine anti-hyperalgesic活动是由KCNQ钾通道激活。
Naunyn Schmiedebergs拱杂志。2004年4月,369 (4):382 - 90。Epub 2004年3月9日。
- PubMed ID
-
15007538 (在PubMed]
- 文摘
-
Retigabine (N - (2-amino-4 (4-fluorobenzylamino)苯基)氨基甲酸乙酯)有广泛的抗惊厥的频谱和目前用于癫痫的临床研究。复合开放影响神经元KCNQ频道。在更高浓度的增强γ-氨基丁酸(GABA)诱导电流以及弱阻塞对钠和钙电流的影响被观察到。本研究的目的是描述的活动retigabine模型的急性和神经性疼痛和调查如果钾通道开放retigabine有助于其活性的影响。Retigabine测试在小鼠和大鼠的尾巴轻轻模型的急性疼痛和神经结扎模型用严格的第五脊神经结扎(L5)使用热和触觉刺激。虽然retigabine像加巴喷丁几乎没有小鼠的镇痛效果显示,老鼠的尾巴轻轻一些镇痛效果模型。这些影响与linopirdine不能得罪,选择性KCNQ钾通道阻滞剂,表明不同的行动模式这一活动。L5-ligated老鼠retigabine显著剂量依赖性升高痛阈和长时间延迟撤军的触觉和热刺激后,分别。在L5结扎模型与热刺激retigabine 10毫克/公斤汇票是100毫克/公斤加巴喷丁或有效10毫克/公斤曲马多。触觉刺激的L5模型是用来测试的角色KCNQ钾通道开放retigabine的效果。 If retigabine 10 mg/kg p.o. was administered alone it was as effective as tramadol 10 mg/kg p.o. in elevating the pain threshold. Linopirdine (1 and 3 mg/kg i.p.) had nearly no influence on neuropathic pain response. If we administered both retigabine and linopirdine the effect of retigabine was abolished or diminished depending on the dose of linopirdine used.In summary, retigabine is effective in predictive models for neuropathic pain. The activity is comparable to tramadol and is present at lower doses compared with gabapentin. Since the anti-allodynic effect can be inhibited by linopirdine we can conclude that the potassium channel opening properties of retigabine are critically involved in its ability to reduce neuropathic pain response.
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物