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首页> 外文期刊>Brain research >Brain penetration of the novel free radical trapping neuroprotectant NXY-059 in rats subjected to permanent focal ischemia.
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Brain penetration of the novel free radical trapping neuroprotectant NXY-059 in rats subjected to permanent focal ischemia.

机译：新型自由基捕获神经保护剂NXY-059在永久性局灶性局部缺血大鼠的脑部渗透。

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摘要

The penetration of the free radical trapping neuroprotectant NXY-059 into the brain has been examined in rats subjected to permanent middle cerebral artery occlusion (pMCAO). NXY-059 (125 mg/kg bolus followed by 125 mg/kg/h) was infused for 4 h 45 min starting 15 min after right pMCAO or sham operation. At 5 h, there was a similar plasma total NXY-059 concentration (micromol/L) in both groups [sham: 623 +/- 44 (6); pMCAO: 605 +/- 43 (5)] and a similar drug concentration (nmol/g) in the right cortex [sham: 6.92 +/- 1.05 (6); pMCAO: 6.14 +/- 2.18 (6)]. A subsequent experiment in normal rats, infusing NXY-059 at both a similar and higher concentration (252 mg/kg bolus and 252 mg/kg/h), demonstrated that the concentration of NXY-059 in cortex increased linearly with respect to the plasma concentration. These data demonstrate that NXY-059 does penetrate brain tissue in control animals and ischemic tissue of animals subjected to pMCAO.
机译：自由基捕获的神经保护剂NXY-059在大脑中的渗透已在遭受永久性大脑中动脉阻塞（pMCAO）的大鼠中进行了检查。在正确的pMCAO或假手术后15分钟开始，将NXY-059（125 mg / kg推注，然后125 mg / kg / h）输注4 h 45 min。在5 h时，两组血浆总NXY-059浓度（微摩尔/升）相似​​[假手术：623 +/- 44（6）; pMCAO：605 +/- 43（5）]和右侧皮质中相似的药物浓度（nmol / g）[假手术：6.92 +/- 1.05（6）; pMCAO：6.14 +/- 2.18（6）]。随后在正常大鼠中进行的实验，以相似和更高的浓度（252毫克/千克大剂量和252毫克/千克/小时）注入NXY-059，表明皮质中NXY-059的浓度相对于血浆呈线性增加浓度。这些数据表明，NXY-059确实渗透了对照动物的脑组织和经过pMCAO的动物的缺血组织。

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