The quaternary lidocaine derivative QX-314 produces long-lasting intravenous regional anesthesia in rats.
The quaternary lidocaine derivative QX-314 produces long-lasting intravenous regional anesthesia in rats.
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四元利多卡因衍生物 QX-314 对大鼠产生持久的静脉局部麻醉
DOI：
10.1371/journal.pone.0099704
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发表时间：
2014
期刊：
影响因子：
3.7
通讯作者：
Chen X
中科院分区：
文献类型：
--
作者：
Zhao Y;Zhou C;Liu J;Liang P;Liao D;Chen Y;Chen X
利多卡因衍生物QX-314在多种动物模型中产生持久的区域麻醉。我们设计了这项研究，以检验QX-314是否能在大鼠模型中产生持久的静脉区域麻醉（IVRA）。方法对大鼠尾部进行IVRA。采用上下法测定QX-314在IVRA中的中位有效浓度（EC50）。采用甩尾法和夹尾法评价大鼠尾部的IVRA。为比较QX-314与利多卡因的作用，将60只sd大鼠随机分为6组（n = 10/组），分别给予0.5%利多卡因0.5 ml、0.25% QX-314、0.5% QX-314、1.0% QX-314、2.0% QX-314和生理盐水。为探讨TRPV1通道在QX-314 IVRA中的作用，将20只大鼠随机分为2组（n = 10/组），分别给予1% QX-314 0.5 ml和1% QX-314+75µg/ml辣椒平。采用拉辛惊厥评分法和心电图法分别测定QX-314对大鼠中枢神经系统和心脏系统的毒性。结果QX-314能产生长效IVRA，且呈浓度依赖性。QX-314在大鼠尾IVRA中的EC50为0.15±0.02%。在0.5%浓度下，QX-314的IVRA持续时间（2.5±0.7小时）明显长于0.5%利多卡因（0.3±0.2小时，P<0.001）。TRPV1通道拮抗剂（capsazepine）可显著降低QX-314的作用。为了评估毒性，QX-314剂量为5或10 mg/kg时未引起任何严重并发症。然而，QX-314剂量为20 mg/kg（体重250 g大鼠为1% QX-314 0.5 ml）时，6/10大鼠死亡。结论QX-314具有浓度依赖性，可产生长效IVRA。这种持久的IVRA是通过激活TRPV1通道介导的。对QX-314毒性并发症的评估证实，低剂量但相关的QX-314没有导致任何可测量的毒性。
Background The lidocaine derivative, QX-314, produces long-lasting regional anesthesia in various animal models. We designed this study to examine whether QX-314 could produce long-lasting intravenous regional anesthesia (IVRA) in a rat model. Methods IVRA was performed on tail of rats. EC50 (median effective concentration) of QX-314 in IVRA was determined by up-and-down method. IVRA on tail of rats was evaluated by tail-flick and tail-clamping tests. For comparison between QX-314 and lidocaine, 60 Sprague-Dawley rats were randomly divided into 6 groups (n = 10/group), respectively receiving 0.5 ml of 0.5% lidocaine, 0.25% QX-314, 0.5% QX-314, 1.0% QX-314, 2.0% QX-314 and normal saline. To explore the role of TRPV1 channel in IVRA of QX-314, 20 rats were randomly divided into 2 groups (n = 10/group), respectively receiving 0.5 ml of 1% QX-314 and 1% QX-314+75 µg/ml capsazepine. Toxicities of QX-314 on central nervous system and cardiac system were measured in rats according to Racine's convulsive scale and by electrocardiogram, respectively. Results QX-314 could produce long-lasting IVRA in a concentration-dependent manner. EC50 of QX-314 in rat tail IVRA was 0.15±0.02%. At concentration of 0.5%, IVRA duration of QX-314 (2.5±0.7 hour) was significantly longer than that of 0.5% lidocaine (0.3±0.2 hour, P<0.001). TRPV1 channel antagonist (capsazepine) could significantly reduce the effect of QX-314. For evaluation of toxicities, QX-314 at doses of 5 or 10 mg/kg did not induce any serious complications. However, QX-314 at dose of 20 mg/kg (1% QX-314 0.5 ml for a rat weighing 250 g) induced death in 6/10 rats. Conclusions QX-314 could produce long-lasting IVRA in a concentration-dependent manner. This long-lasting IVRA was mediated by activation of TRPV1 channels. Evaluation of toxic complications of QX-314 confirmed that low but relevant doses of QX-314 did not result in any measurable toxicity.
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影响因子：
2.5
作者：
Bern, Sarah;Weinberg, Guy
通讯作者：
Weinberg, Guy
辣椒素结合局部麻醉剂优先延长大鼠坐骨神经中的感觉/伤害性阻滞。
影响因子：
8.8
作者：
Gerner P;Binshtok AM;Wang CF;Hevelone ND;Bean BP;Woolf CJ;Wang GK
通讯作者：
Wang GK
DOI：
10.1007/bf03020416
发表时间：
2002-01-01
期刊：
CANADIAN JOURNAL OF ANAESTHESIA-JOURNAL CANADIEN D ANESTHESIE
影响因子：
--
作者：
Choyce, A;Peng, P
通讯作者：
Peng, P
影响因子：
7.4
作者：
Kawamata, Mikito;Sugino, Shigekazu;Namiki, Akiyoshi
通讯作者：
Namiki, Akiyoshi
影响因子：
5.7
作者：
Sawyer, RJ;von Schroeder, H
通讯作者：
von Schroeder, H