An integrated platform for fully automated high-throughput LC–MS/MS analysis of in vitro metabolic stability assay samples

2010 ◽  
Vol 296 (1-3) ◽  
pp. 1-9 ◽  
Author(s):  
Andreas H. Luippold ◽  
Thomas Arnhold ◽  
Wolfgang Jörg ◽  
Roderich D. Süssmuth
Keyword(s):  
High Throughput ◽  
Metabolic Stability ◽  
Ms Analysis ◽  
Integrated Platform

An integrated platform for a high-throughput pharmacokinetic study of glycosides using a boronic acid-functionalized 96-well glass plate

2019 ◽  
Vol 55 (64) ◽  
pp. 9543-9546
Author(s):  
Ningning Zhao ◽  
Qianqian Gu ◽  
Zhiqiang Liu ◽  
Fengrui Song ◽  
Zifeng Pi ◽  
...  
Keyword(s):  
High Throughput ◽  
Pharmacokinetic Study ◽  
Boronic Acid ◽  
Large Scale ◽  
Glass Plate ◽  
The Novel ◽  
Ms Analysis ◽  
Integrated Platform

The novel Vial@FPBA strategy was established for a large-scale pharmacokinetic study of glycosides, during which glycosides were absorbed into a boronic acid-functionalized 96-well glass plate and directly desorbed for UHPLC-MS/MS analysis.

scholarly journals Examination of the Utility of the High Throughput In Vitro Metabolic Stability Assay to Estimate In Vivo Clearance in the Mouse

2009 ◽  
Vol 3 ◽  
pp. 31-42 ◽  
Author(s):  
S Sarawek ◽  
L Li ◽  
X.Q Yu ◽  
S Rooney ◽  
A Nouraldeen ◽  
...  
Keyword(s):  
High Throughput ◽  
Metabolic Stability

scholarly journals A High-Throughput Method for Enzyme Kinetic Studies

2003 ◽  
Vol 8 (5) ◽  
pp. 544-554 ◽  
Author(s):  
Lakshmi D. Saraswat ◽  
Kimberley A. Caserta ◽  
Kathy Laws ◽  
Darren Wei ◽  
Simon S. Jones ◽  
...  
Keyword(s):  
Drug Metabolism ◽  
High Throughput ◽  
Kinetic Studies ◽  
Metabolic Stability ◽  
Metabolic Parameter ◽  
High Throughput Method ◽  
Multiple Samples ◽  
Parameter Values

A simple and flexible setup for conducting drug metabolism studies is described in this report. A heating block was designed for the Multimek liquid handler platform for incubation of multiple samples at 37 °C in a 96-well format. This setup enables the rapid performance of drug metabolism experiments on a large number of samples. In this report, the authors present the validation of the system by 1) showing reproducible and consistent determination of the in vitro half-life of midazolam in every well across the entire plate and 2) determination of metabolic parameter values of midazolam, testosterone, diclofenac, warfarin, and dextromethorphan and inhibition parameter values of quinidine and ketoconazole, all comparable to literature values. In addition, the authors demonstrate the application of the setup to determining the metabolic stability of a set of proprietary compounds, the inhibition of activity of cytochrome P450 (CYP) enzymes, and the conduct of a single combination experiment that can simultaneously determine the metabolic stability and CYP inhibition activity. Overall, the system represents a simple, high-throughput and useful tool for drug metabolism screening in drug discovery. ( Journal of Biomolecular Screening 2003:544-554)

scholarly journals RapidFire BLAZE-Mode Is Boosting ESI-MS Toward High-Throughput-Screening

2019 ◽  
Vol 24 (4) ◽  
pp. 386-393 ◽  
Author(s):  
Tom Bretschneider ◽  
Can Ozbal ◽  
Markus Holstein ◽  
Martin Winter ◽  
Frank H. Buettner ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Technological Advancement ◽  
Label Free ◽  
Mass Spectrometers ◽  
Esi Ms ◽  
Compound Libraries ◽  
Ms Analysis ◽  
Long Time

Label-free in vitro potency assays are an emerging field in drug discovery to enable more physiological conditions, to improve the readout quality, and to save time. For this approach mass spectrometry (MS) is a powerful technology to directly follow physiological processes. The speed of this methodology, however, was for a long time not compatible with chemiluminescence- or fluorescence-based assays. Recent advances in matrix-assisted laser desorption/ionization (MALDI) instrumentation paved the way for high-throughput MS analysis of label-free assays for large compound libraries, whereas electrospray ionization (ESI)-based mass spectrometers equipped with RapidFire autosamplers were limited to medium throughput. Here we present a technological advancement of the RapidFire device to enable cycle times of 2.5 s per sample. This newly developed BLAZE-mode substantially boosted the ESI-MS analysis speed, providing an alternative technology for label-free high-throughput screening.

New Imidazole Inhibitors of Mycobacterial FtsZ: the Way from High-Throughput Molecular Screening in Grid up to in vitro Verification

2016 ◽  
Vol 12 (3) ◽  
pp. 43-55 ◽  
Author(s):  
P.A. Karpov ◽  
◽  
O.M. Demchuk ◽  
V.M. Britsun ◽  
D.I. Lytvyn ◽  
...  
Keyword(s):  
High Throughput ◽  
Molecular Screening ◽  
The Way
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