Detalles de la búsqueda
1.
Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatment of osteoporosis.
Chem Res Toxicol
; 23(6): 1115-26, 2010 Jun 21.
Artículo
en Inglés
| MEDLINE | ID: mdl-20507089
2.
Can in vitro metabolism-dependent covalent binding data distinguish hepatotoxic from nonhepatotoxic drugs? An analysis using human hepatocytes and liver S-9 fraction.
Chem Res Toxicol
; 22(2): 332-40, 2009 Feb.
Artículo
en Inglés
| MEDLINE | ID: mdl-19161298
3.
High throughput ADME screening: practical considerations, impact on the portfolio and enabler of in silico ADME models.
Curr Drug Metab
; 9(9): 847-53, 2008 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-18991580
4.
Can in vitro metabolism-dependent covalent binding data in liver microsomes distinguish hepatotoxic from nonhepatotoxic drugs? An analysis of 18 drugs with consideration of intrinsic clearance and daily dose.
Chem Res Toxicol
; 21(9): 1814-22, 2008 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-18690722
5.
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation.
Bioorg Med Chem Lett
; 18(23): 6071-7, 2008 Dec 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-18951788
6.
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship.
J Med Chem
; 49(14): 4425-36, 2006 Jul 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-16821801
7.
Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4.
Chem Biol Interact
; 155(1-2): 10-20, 2005 Jun 30.
Artículo
en Inglés
| MEDLINE | ID: mdl-15978881
8.
Simple strategies for reducing sample loads in in vitro metabolic stability high-throughput screening experiments: a comparison between traditional, two-time-point and pooled sample analyses.
J Pharm Sci
; 94(1): 38-45, 2005 Jan.
Artículo
en Inglés
| MEDLINE | ID: mdl-15761928
9.
The development of a higher throughput reactive intermediate screening assay incorporating micro-bore liquid chromatography-micro-electrospray ionization-tandem mass spectrometry and glutathione ethyl ester as an in vitro conjugating agent.
J Pharm Biomed Anal
; 36(1): 105-16, 2004 Sep 21.
Artículo
en Inglés
| MEDLINE | ID: mdl-15351054
10.
Metabolism of a dopamine receptor partial agonist in rats, including an unusual N-dearylation reaction.
Drug Metab Pharmacokinet
; 26(3): 266-79, 2011 Jun.
Artículo
en Inglés
| MEDLINE | ID: mdl-21383524
11.
NADPH-dependent covalent binding of [3H]paroxetine to human liver microsomes and S-9 fractions: identification of an electrophilic quinone metabolite of paroxetine.
Chem Res Toxicol
; 20(11): 1649-57, 2007 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-17907785
12.
Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human.
Drug Metab Dispos
; 35(11): 2111-8, 2007 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-17686907
13.
A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif.
Chem Res Toxicol
; 20(12): 1954-65, 2007 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-17935300
14.
A 96-well efflux assay to identify ABCG2 substrates using a stably transfected MDCK II cell line.
Mol Pharm
; 3(1): 45-54, 2006.
Artículo
en Inglés
| MEDLINE | ID: mdl-16686368
15.
A semiquantitative method for the determination of reactive metabolite conjugate levels in vitro utilizing liquid chromatography-tandem mass spectrometry and novel quaternary ammonium glutathione analogues.
Chem Res Toxicol
; 19(3): 480-90, 2006 Mar.
Artículo
en Inglés
| MEDLINE | ID: mdl-16544956
16.
Bioactivation of the nontricyclic antidepressant nefazodone to a reactive quinone-imine species in human liver microsomes and recombinant cytochrome P450 3A4.
Drug Metab Dispos
; 33(2): 243-53, 2005 Feb.
Artículo
en Inglés
| MEDLINE | ID: mdl-15523046
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