| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 7802446 | European Journal of Medicinal Chemistry | 2012 | 8 Pages |
Abstract
⺠Mechanistic insights can be derived by comparing liver microsome and hepatocyte stability. ⺠Liver microsomes and hepatocytes give comparable intrinsic clearance for CYP mediated clearance. ⺠Liver microsomes give lower metabolic rate than hepatocytes for non-CYP mechanisms. âºÂ Comparison of intrinsic clearance from liver microsomes and hepatocytes cannot easily identify hepatic uptake or efflux transporter substrates. âºÂ Whether passive permeability will limit hepatocyte metabolism is dependent on the metabolic rate.
Keywords
SARuridine 5′-diphospho-glucuronosyltransferaseNa+-taurocholate cotransporting polypeptideUDPGAOCT1FMOOATP1B1P-gpNtcpOATP1B3BcrpMrp2MAOMWCOHEPESUGTCyPADMENADPHN-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acidP-glycoproteinaldehyde oxidaseuridine diphosphoglucuronic acidMetabolic stabilityabsorption, distribution, metabolism, and excretionorganic cation transporterStructure–activity relationshipREDCytochrome P450Molecular weight cutoffmonoamine oxidaseFlavin-containing monooxygenaseHuman Liver Microsomesnicotinamide adenine dinucleotide phosphateIVIVCHuman hepatocytesIntrinsic clearancebreast cancer resistance proteinDrug discovery
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Li Di, Christopher Keefer, Dennis O. Scott, Timothy J. Strelevitz, George Chang, Yi-An Bi, Yurong Lai, Jonathon Duckworth, Katherine Fenner, Matthew D. Troutman, R. Scott Obach,