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首页> 外文期刊>Journal of Pharmaceutical and Biomedical Analysis: An International Journal on All Drug-Related Topics in Pharmaceutical, Biomedical and Clinical Analysis >Dansyl azide as a selective fluorescence tagging probe for click chemistry reactions and its application to monitor rasagiline in pharmacokinetic studies
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Dansyl azide as a selective fluorescence tagging probe for click chemistry reactions and its application to monitor rasagiline in pharmacokinetic studies

机译：丹甘酰叠氮化物作为选择性荧光标记探针，用于点击化学反应及其在药代动力学研究中监测罗萨尼尼的应用

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摘要

Click chemistry has been widely used for bioorthogonal labeling of biomolecules for its high efficiency, regioselectivity and biocompatibility. In this study, dansyl azide (DNS-AZ) was introduced as a novel fluorescence labeling reagent for the determination of alkynes based on copper (I)-catalyzed azide alkyne cycloaddition (CuAAC) click chemistry reaction. Rasagiline mesylate (RSM) is an irreversible, selective monoamine oxidase B (MAO-B) inhibitor. It is used as a model example for drugs with terminal alkyne moiety that could be monitored in biological samples with CuAAC reaction. RSM reacts with DNS-AZ in the presence of copper (II) and sodium ascorbate as catalysts to form stable 1,2,3-triazole derivative determined by HPLC with fluorescence detection. The developed methodology was optimized for sensitive and selective determination of RSM in rat plasma. Selegiline (SLG) was used as internal standard. The developed method was validated according to US-FDA guidelines in order to confirm method suitability for the intended application. The method allowed accurate and precise determination of RSM in the linearity range 0.50-100 ng mL(-1) with a detection limit of 0.16 ng mL(-1) for RSM in rat plasma. To confirm method applicability in real sample analysis, the developed method was employed to quantify RSM in a pharmacokinetic study in rats after administration of a single oral dose of RSM tablet. (C) 2018 Elsevier B.V. All rights reserved.
机译：单击化学已被广泛用于生物分子的生物正交标记，其高效率，区域选择性和生物相容性。在该研究中，将丹氨酰叠氮化物（DNS-AZ）作为一种新的荧光标记试剂，用于基于铜（I）的炔烃（I） - 催化叠氮化物炔环加湿（CUAAC）点击化学反应。 Rasagiline甲磺酸盐（RSM）是一种不可逆的选择性单胺氧化酶B（MAO-B）抑制剂。它被用作具有末端炔烃部分的药物的模型实例，其可以在具有Cuaac反应中的生物样品中监测。 RSM在铜（II）的存在下与DNS-AZ反应，抗坏血酸钠作为催化剂，以形成通过HPLC测定的稳定的1,2,3-三唑衍生物，具有荧光检测。开发方法经过优化，用于大鼠等离子体中RSM的敏感和选择性测定。 Selegiline（SLG）用作内标。根据US-FDA指南验证开发的方法，以确认对预期应用的方法适用性。该方法允许在大鼠等离子体中具有0.50-100ng ml（-1）的线性度范围0.50-100ng ml（-1）的RSM的精确精确测定RSM。为了确认在真实样本分析中的适用性，研制方法用于量化在施用单一口服剂量的RSM片剂后大鼠药代动力学研究中的RSM。 （c）2018年elestvier b.v.保留所有权利。

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