卵母细胞异体表达模型中选择性5-HT重摄取阻断剂的电生理特性比较

发布时间：2018-04-28 17:09

本文选题：-羟色胺转运体 + 选择性-羟色胺重摄取阻断剂　；参考：《上海交通大学学报(医学版)》2016年02期

【摘要】：目的观察和研究选择性5-羟色胺(5-HT)重摄取阻断剂(SSRIs)西酞普兰、氟西汀、帕罗西汀与非典型四环类抗抑郁药曲唑酮对人5-HT转运体(h SERTs)重摄取5-HT的抑制效应。方法在非洲爪蟾卵母细胞上异体表达h SERTs,采用双微电极电压钳技术记录在不同药物作用下5-HT转运电流的变化。结果在相同浓度下,帕罗西汀、西酞普兰、氟西汀和曲唑酮分别使5-HT诱导的初始转运电流抑制了(29.31±1.52)%、(47.17±3.38)%、(27.72±2.01)%和(43.30±2.83)%,但曲唑酮在其作用时间内未能有效逆转5-HT转运电流。采用指数衰减函数拟合电流曲线求取药物与h SERTs的结合时间常数以及药物与5-HT竞争转运体的时间常数,发现在3种SSRIs中,帕罗西汀的结合与竞争时间常数均最小,然后依次为氟西汀和西酞普兰。结论帕罗西汀对5-HT转运电流的初始抑制效果优于氟西汀和西酞普兰。
[Abstract]:Objective to observe and study the inhibitory effect of selective 5-HT reuptake blocker (SSRIs-citalopram, fluoxetine, paroxetine and atypical quadricyclic antidepressant trazodone) on the reuptake of 5-HT by human 5-HT transporter. Methods hSERTswere expressed in Xenopus oocytes. The changes of 5-HT transport current were recorded by double microelectrode voltage clamp technique. Results at the same concentration, paroxetine, citalopram, fluoxetine and trazodone inhibited the initial transport current induced by 5-HT by 29.31 卤1.52U and 27.72 卤2.01% and 43.30 卤2.83%, respectively, but trazodone could not effectively reverse the transport current of 5-HT. The binding time constant of h SERTs and the time constant of competing transporter between drugs and 5-HT were obtained by using exponential decay function fitting current curve. It was found that the combination and competition time constants of paroxetine were the smallest among the three SSRIs. Fluoxetine and citalopram were followed by fluoxetine and citalopram. Conclusion the initial inhibitory effect of paroxetine on 5-HT transport current is superior to fluoxetine and citalopram.
【作者单位】：上海健康医学院基础医学院生理教研室;上海交通大学基础医学院实验中心;上海交通大学基础医学院生理学教研室;
【基金】：上海市科委重点资助项目(06JC14045) 上海市教育委员会科研创新项目(13yz150) 上海医药高等专科学校教育科研基金(2014zr006FY)~~
【分类号】：R749.4

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