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用于肝微粒体孵育样品定量分析的自动化质谱系统的开发:一种用于快速筛选新化合物代谢稳定性的工具。

Development of an automated mass spectrometry system for the quantitative analysis of liver microsomal incubation samples: a tool for rapid screening of new compounds for metabolic stability.

作者信息

Korfmacher W A, Palmer C A, Nardo C, Dunn-Meynell K, Grotz D, Cox K, Lin C C, Elicone C, Liu C, Duchoslav E

机构信息

Department of Drug Metabolism and Pharmacokinetics, Schering-Plough Research Institute, Kenilworth, NJ 07033, USA.

出版信息

Rapid Commun Mass Spectrom. 1999;13(10):901-7. doi: 10.1002/(SICI)1097-0231(19990530)13:10<901::AID-RCM583>3.0.CO;2-5.

DOI:10.1002/(SICI)1097-0231(19990530)13:10<901::AID-RCM583>3.0.CO;2-5
PMID:10353225
Abstract

There is a continuing need for increased throughput in the evaluation of new drug entities in terms of their pharmacokinetic parameters. One useful parameter that can be measured in vitro using liver microsomal preparations is metabolic stability. In this report, we describe an automated system that can be used for unattended quantitative analysis of liver microsomal samples for a series of compounds. This system is based on the Sciex API 150 (single quadrupole) liquid chromatography/mass spectrometry system and utilizes 96-well plate autosampler technology as well as a custom-designed AppleScript which executes the on-line data processing and report generation. It has the capability of analyzing at least 75 compounds per week or 300 compounds per month in an automated fashion.

摘要

在新药实体的药代动力学参数评估方面,持续需要提高通量。代谢稳定性是一个可以使用肝微粒体制剂在体外测量的有用参数。在本报告中,我们描述了一种自动化系统,可用于对一系列化合物的肝微粒体样品进行无人值守的定量分析。该系统基于Sciex API 150(单四极杆)液相色谱/质谱系统,采用96孔板自动进样器技术以及定制设计的AppleScript,该脚本执行在线数据处理和报告生成。它能够以自动化方式每周分析至少75种化合物,或每月分析300种化合物。

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An Automated High-Throughput Metabolic Stability Assay Using an Integrated High-Resolution Accurate Mass Method and Automated Data Analysis Software.一种使用集成高分辨率精确质量法和自动化数据分析软件的自动化高通量代谢稳定性测定方法。
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Application of parallel liquid chromatography/mass spectrometry for high throughput microsomal stability screening of compound libraries.
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Mass spectrometry innovations in drug discovery and development.药物发现与开发中的质谱创新
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