Possibility of QX-314 as a novel therapeutic drug for neuropathic pain

QX-314作为神经病理性疼痛新型治疗药物的可能性

• 批准号: 22659367
• 负责人: SEO Kenji
• 金额: $ 2.06万
• 依托单位: Niigata University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Challenging Exploratory Research
• 财政年份: 2010
• 资助国家: 日本
• 起止时间: 2010 至 2012
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-22659367/
• 关键词: QX-314, リドカイン; ニューロパチー; TRPV1; PAIN; 三叉神経; QX-314; カプサイシン; 末梢神経; 知覚; 神経因性疼痛; 下歯槽神経; 神経切断; TRPV1チャネル; ラット; 触覚; 三叉神経脊髄路核; 侵害刺激; 膜電位; C-繊維

A novel local anesthetic, QX-314 is known to have an effect of Na+ channel blockade.This action requires it to enter through TRIPV1 channel on the surface of the neuron and make a blockade action inside the neuron. Thus, we aimed to study the possibility of QX-314 in anti-nociceptive effect and investigated the effects of QX-314 on the withdraw threshold which was decreased by a resection of inferior alveolar nerve in the rats. The results were that QX-314 using together with capsaicin, the threshold became to be elevated. This was consistent with histological findings that TRIPV1channels increased in the injured trigeminal nerve. These suggested that QX-314 has a potential to be used as a therapeutic tool for neuropathic pain.

已知一种新型的局部麻醉QX-314具有Na+通道封锁的作用。此动作要求它通过神经元表面的TripV1通道进入，并在神经元内进行阻断动作。因此，我们旨在研究QX-314在抗伤害感受效应中的可能性，并研究了QX-314对大鼠下肺泡神经的切除降低的撤离阈值的影响。结果是QX-314与辣椒素一起使用，阈值升高。这与组织学发现一致，即受伤的三叉神经中TRIPV1频道增加。这些表明QX-314有可能用作神经性疼痛的治疗工具。

项目成果

Expression of TRPV1 channels after nerve injury provides an essential delivery tool for neuropathic pain attenuation.

• DOI: 10.1371/journal.pone.0044023
• 发表时间: 2012
• 期刊: PloS one
• 影响因子: 3.7
• 作者: Zakir HM;Mostafeezur RM;Suzuki A;Hitomi S;Suzuki I;Maeda T;Seo K;Yamada Y;Yamamura K;Lev S;Binshtok AM;Iwata K;Kitagawa J
• 通讯作者: Kitagawa J