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A novel psychoanalytical approach: An electrochemical ligand-binding assay to screen antipsychotics
Biosensors and Bioelectronics ( IF 12.6 ) Pub Date : 2017-08-30 , DOI: 10.1016/j.bios.2017.08.059
Tugba Kilic , Valerie Brunner , Laurent Audoly , Sandro Carrara

Schizophrenia treatment may see a paradigm shift due to development of new atypical antipsychotic drugs (APDs), with better tolerability due to more selective dopamine (DA) receptor blockade. Monitoring of these APD candidates in biological fluids is of great importance to reduce the development cost, to clarify the mechanism of action and ultimately to support the demonstration of efficacy of these molecules. Electrochemical approaches have attracted great attention for monitoring DA and APD levels but none of the methods developed so far aimed to screen APD candidates. Herein, by this work, we propose for the first time an electrochemical ligand-binding approach for antipsychotic drug screening where competitive binding of a novel APD and DA to a dopamine D3 receptor (D3R) was investigated by looking at electrochemical signals of DA and drug before and after D3R interaction. D3R peptide was incubated with DA and/or drug first and then changes in electrochemical oxidation signals of free DA and the drug was measured by cyclic voltammetry (CV) and differential pulse voltammetry (DPV). Circular Dichroism spectroscopy was used to investigate the secondary structure of the peptide upon binding with either drug and/or DA.



中文翻译:

一种新颖的心理分析方法:电化学配体结合测定法筛选抗精神病药

由于新的非典型抗精神病药(APDs)的发展,精神分裂症的治疗可能会发生范式转变,而由于对多巴胺(DA)受体的选择性更高,对精神分裂症的耐受性也更好。监测生物流体中这些APD候选物对于降低开发成本,阐明作用机理并最终支持这些分子功效的证明非常重要。电化学方法已经引起了监测DA和APD水平的极大关注,但是迄今为止,尚未开发出任何旨在筛选APD候选物的方法。在这里,通过这项工作,我们首次提出了一种用于抗精神病药物筛选的电化学配体结合方法,该方法通过观察DA和药物在D3R相互作用之前和之后的电化学信号来研究新型APD和DA与多巴胺D3受体(D3R)的竞争结合。首先将D3R肽与DA和/或药物孵育,然后再通过游离伏安法(CV)和差动脉冲伏安法(DPV)测定游离DA的电化学氧化信号的变化。圆二色谱法用于研究与药物和/或DA结合后的肽的二级结构。首先将D3R肽与DA和/或药物孵育,然后再通过游离伏安法(CV)和差动脉冲伏安法(DPV)测定游离DA的电化学氧化信号的变化。圆二色谱法用于研究与药物和/或DA结合后的肽的二级结构。首先将D3R肽与DA和/或药物孵育,然后再通过游离伏安法(CV)和微分脉冲伏安法(DPV)测定游离DA的电化学氧化信号的变化。圆二色谱法用于研究与药物和/或DA结合后的肽的二级结构。

更新日期:2017-08-30
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