Literature DB >> 10322290

Novel procedure for rapid pharmacokinetic screening of discovery compounds in rats.

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Abstract

In therapeutic areas aimed at developing an orally administered drug, the pharmacokinetic profile of a drug candidate after oral administration in vivo is pivotal in evaluating its success. This can be done by monitoring the plasma concentration versus time after dosing and calculating the area under the curve (AUC). The authors describe a novel screening protocol in which an estimated AUC can be determined, allowing the rapid evaluation of large numbers of compounds and providing a rank order of estimated AUC values to prioritize compounds for further investigation.

Entities:  

Year:  1999        PMID: 10322290     DOI: 10.1016/s1359-6446(98)01299-9

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


  8 in total

1.  Application of parallel liquid chromatography/mass spectrometry for high throughput microsomal stability screening of compound libraries.

Authors:  Rongda Xu; Csaba Nemes; Kelly M Jenkins; Robyn A Rourick; Daniel B Kassel; Charles Z C Liu
Journal:  J Am Soc Mass Spectrom       Date:  2002-02       Impact factor: 3.109

2.  The use of the suicide CYP450 inhibitor ABT for distinguishing absorption and metabolism processes in in-vivo pharmacokinetic screens.

Authors:  Gary W Caldwell; David M Ritchie; John A Masucci; William Hageman; Carlos Cotto; Jeffrey Hall; Becki Hasting; William Jones
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2005 Jan-Jun       Impact factor: 2.441

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.  Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma.

Authors:  Xianhai Huang; Jason Brubaker; Wei Zhou; Purakkattle J Biju; Li Xiao; Ning Shao; Ying Huang; Li Dong; Zhidan Liu; Rema Bitar; Alexei Buevich; Joon Jung; Scott L Peterson; John W Butcher; Joshua Close; Michelle Martinez; Rachel N MacCoss; Hongjun Zhang; Scott Crawford; Kevin D McCormick; Robert Aslanian; Ravi Nargund; Craig Correll; Francois Gervais; Hongchen Qiu; Xiaoxin Yang; Charles Garlisi; Diane Rindgen; Kevin M Maloney; Phieng Siliphaivanh; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2018-06-23       Impact factor: 4.345

5.  Allometric scaling of pharmacokinetic parameters in drug discovery: can human CL, Vss and t1/2 be predicted from in-vivo rat data?

Authors:  Gary W Caldwell; John A Masucci; Zhengyin Yan; William Hageman
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2004 Apr-Jun       Impact factor: 2.441

Review 6.  Biology and therapeutic potential of cannabinoid CB2 receptor inverse agonists.

Authors:  C A Lunn; E-P Reich; J S Fine; B Lavey; J A Kozlowski; R W Hipkin; D J Lundell; L Bober
Journal:  Br J Pharmacol       Date:  2007-10-01       Impact factor: 8.739

7.  Survival-Assured Liver Injury Preconditioning (SALIC) Enables Robust Expansion of Human Hepatocytes in Fah-/- Rag2-/- IL2rg-/- Rats.

Authors:  Ludi Zhang; Jian-Yun Ge; Yun-Wen Zheng; Zhen Sun; Chenhua Wang; Zhaoliang Peng; Baihua Wu; Mei Fang; Kinji Furuya; Xiaolong Ma; Yanjiao Shao; Nobuhiro Ohkohchi; Tatsuya Oda; Jianglin Fan; Guoyu Pan; Dali Li; Lijian Hui
Journal:  Adv Sci (Weinh)       Date:  2021-08-11       Impact factor: 16.806

8.  Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.

Authors:  Vishal B Siramshetty; Pranav Shah; Edward Kerns; Kimloan Nguyen; Kyeong Ri Yu; Md Kabir; Jordan Williams; Jorge Neyra; Noel Southall; Ðắc-Trung Nguyễn; Xin Xu
Journal:  Sci Rep       Date:  2020-11-26       Impact factor: 4.996

  8 in total

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