Literature DB >> 11241763

Cassette-accelerated rapid rat screen: a systematic procedure for the dosing and liquid chromatography/atmospheric pressure ionization tandem mass spectrometric analysis of new chemical entities as part of new drug discovery.

W A Korfmacher1, K A Cox, K J Ng, J Veals, Y Hsieh, S Wainhaus, L Broske, D Prelusky, A Nomeir, R E White.   

Abstract

This report addresses the continuing need for increased throughput in the evaluation of new chemical entities (NCEs) in terms of their pharmacokinetic (PK) parameters by describing an alternative procedure for increasing the throughput of the in vivo screening of NCEs in the oral rat PK model. The new approach is called "cassette-accelerated rapid rat screen" (CARRS). In this assay, NCEs are dosed individually (n = 2 rats/compound) in batches of six compounds per set. The assay makes use of a semi-automated protein precipitation procedure for sample preparation in a 96-well plate format. The liquid chromatography/atmospheric pressure ionization tandem mass spectrometry (LC/API-MS/MS) assay is also streamlined by analyzing the samples as "cassettes of six". Using this new approach, a threefold increase in throughput was achieved over the previously reported "rapid rat screen". Copyright 2001 John Wiley & Sons, Ltd.

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Year:  2001        PMID: 11241763     DOI: 10.1002/rcm.235

Source DB:  PubMed          Journal:  Rapid Commun Mass Spectrom        ISSN: 0951-4198            Impact factor:   2.419


  12 in total

1.  Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction.

Authors:  Andrew W Stamford; Jack D Scott; Sarah W Li; Suresh Babu; Dawit Tadesse; Rachael Hunter; Yusheng Wu; Jeffrey Misiaszek; Jared N Cumming; Eric J Gilbert; Chunli Huang; Brian A McKittrick; Liwu Hong; Tao Guo; Zhaoning Zhu; Corey Strickland; Peter Orth; Johannes H Voigt; Matthew E Kennedy; Xia Chen; Reshma Kuvelkar; Robert Hodgson; Lynn A Hyde; Kathleen Cox; Leonard Favreau; Eric M Parker; William J Greenlee
Journal:  ACS Med Chem Lett       Date:  2012-07-12       Impact factor: 4.345

Review 2.  Toward sensitive and accurate analysis of antibody biotherapeutics by liquid chromatography coupled with mass spectrometry.

Authors:  Bo An; Ming Zhang; Jun Qu
Journal:  Drug Metab Dispos       Date:  2014-09-02       Impact factor: 3.922

3.  Rapid in vivo oral screening in rats: reliability, acceptance criteria, and filtering efficiency.

Authors:  Hong Mei; Walter Korfmacher; Richard Morrison
Journal:  AAPS J       Date:  2006-07-28       Impact factor: 4.009

4.  Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.

Authors:  William T McElroy; Zheng Tan; Ginny Ho; Sunil Paliwal; Guoqing Li; W Michael Seganish; Deen Tulshian; James Tata; Thierry O Fischmann; Christopher Sondey; Hong Bian; Loretta Bober; James Jackson; Charles G Garlisi; Kristine Devito; James Fossetta; Daniel Lundell; Xiaoda Niu
Journal:  ACS Med Chem Lett       Date:  2015-05-12       Impact factor: 4.345

5.  Simultaneous analysis of multiple monoclonal antibody biotherapeutics by LC-MS/MS method in rat plasma following cassette-dosing.

Authors:  Hongyan Li; Robert Ortiz; Linh T B Tran; Hossein Salimi-Moosavi; Jennifer Malella; Christopher A James; Jean W Lee
Journal:  AAPS J       Date:  2012-12-12       Impact factor: 4.009

6.  The Discovery of Pyridone and Pyridazone Heterocycles as γ-Secretase Modulators.

Authors:  Xianhai Huang; Robert Aslanian; Wei Zhou; Xiaohong Zhu; Jun Qin; William Greenlee; Zhaoning Zhu; Lili Zhang; Lynn Hyde; Inhou Chu; Mary Cohen-Williams; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2010-05-24       Impact factor: 4.345

7.  Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.

Authors:  Xianhai Huang; Wei Zhou; Xiaoxiang Liu; Hongmei Li; George Sun; Mihirbaran Mandal; Monica Vicarel; Xiaohong Zhu; Chad Bennett; Troy McCraken; Dmitri Pissarnitski; Zhiqiang Zhao; David Cole; Gioconda Gallo; Zhaoning Zhu; Anandan Palani; Robert Aslanian; John Clader; Michael Czarniecki; William Greenlee; Duane Burnett; Mary Cohen-Williams; Lynn Hyde; Lixin Song; Lili Zhang; Inhou Chu; Alexei Buevich
Journal:  ACS Med Chem Lett       Date:  2012-09-04       Impact factor: 4.345

8.  Discovery of a potent nicotinic Acid receptor agonist for the treatment of dyslipidemia.

Authors:  Jun Qin; Ashwin Rao; Xiao Chen; Xiaohong Zhu; Zhidan Liu; Xianhai Huang; Sylvia Degrado; Ying Huang; Dong Xiao; Robert Aslanian; Boonlert Cheewatrakoolpong; Hongtao Zhang; Scott Greenfeder; Constance Farley; John Cook; Stan Kurowski; Qiu Li; Margaret van Heek; Madhu Chintala; Ganfeng Wang; Yunsheng Hsieh; Fangbiao Li; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2010-12-08       Impact factor: 4.345

9.  Discovery of a Potent Pyrazolopyridine Series of γ-Secretase Modulators.

Authors:  Jun Qin; Wei Zhou; Xianhai Huang; Pawan Dhondi; Anandan Palani; Robert Aslanian; Zhaoning Zhu; William Greenlee; Mary Cohen-Williams; Nicholas Jones; Lynn Hyde; Lili Zhang
Journal:  ACS Med Chem Lett       Date:  2011-03-29       Impact factor: 4.345

10.  In Vivo Rapid Assessment of Compound Exposure (RACE) for Profiling the Pharmacokinetics of Novel Chemical Probes.

Authors:  Danielle McAnally; Michael Vicchiarelli; Khandaker Siddiquee; Layton H Smith
Journal:  Curr Protoc Chem Biol       Date:  2012-12-01
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