Drug Metabolism in Drug Design and Development Basic Concepts and Practice

Therefore, the oral clearance or the plasma-concentration-time curve for an oral administration (AUCpo) can be directly estimate ...

CYP2C9-mediated celecoxib hydroxylation was reduced by the amino acid substitutions of Ile^359 to Leu^359 and Arg^144 to Cys^144 ...

AUCpo the plasma-concentration-time curve of following an oral administration CLh hepatic clearance CLint intrinsic clearance CL ...

UDPGA uridine 5 0 -diphosphate glucuronic acid UGT UDP-glucuronosyltransferase UV ultraviolet Vmax the maximal rate REFERENCES A ...

Davies B, Morris T. Physiological parameters in laboratory animals and humans. Pharm Res 1993;10:1093–1095. Dordal A, Lipkin M, ...

Kalvass JC, Tess DA, Giragossian C, Linhares MC, Maurer TS. Influence of microsomal concentration on apparent intrinsic clearanc ...

Naritomi Y, Terashita S, Kimura S, Suzuki A, Kagayama A, Sugiyama Y. Prediction of human hepatic clearance fromin vivoanimal exp ...

Roberts MS, Rowland M.A dispersion model of hepatic elimination: 3. Application to metabolite formation and elimination kinetics ...

human plasma and 7-hydroxywarfarin in human urine by chiral stationary-phase liquid chromatography with ultraviolet or fluoresce ...

14 PROTOCOLS FOR ASSESSMENT OF IN VITRO AND IN VIVO BIOACTIVATION POTENTIAL OF DRUG CANDIDATES ZHOUPENGZHANG ANDJINPINGGAN Xenob ...

Bioactivation, or metabolic activation, is a process where xenobiotics are metabolized to proximate and ultimate reactive interm ...

OH O O NH NH 2 H S O N H OH O H R O HNH S O R OH O HO S O N OH O HO S OH O N O HO S O N OH NC CN HO S OH O N H OH S HN O OH O OH ...

GSH and NAc are complementary to covalent protein binding studies because trapping studies are easily implemented and amenable t ...

spectra of NAc adducts may provide more structural information of modification site on the drug moiety. Even though fragmentatio ...

resulting in covalent protein binding in vivo may not be detected in incubations with common trapping agentsin vitro(Zhang et al ...

are recorded by collision-induced dissociation (CID) of molecular ion of the test compound (MH+) species. Several approaches mig ...

In trapping studies of (2S,3R)-(+)-3-(3-hydroxyphenyl)-2-[4-(2-pyrrolidin- 1-ylethoxy)-phenyl]-2,3-dihydro-1,4-benzoxathiin-6-ol ...

and 14.4b), consistent with the addition of the element ofN-acetylcysteine to the parent molecule. The MS^2 spectrum ofm/z611 re ...

are the same as that described in Section 14.1.2 (the protocol for detection of glutathione/N-acetylcysteine or cyano adducts us ...

an HPLC system consisting of a Perkin-Elmer Series 200 quaternary pump and a Series 200 autosampler (Norwark, CT). A Turbo IonSp ...