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Showing 1 to 12 of 20 entries
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Kinetics of cytochrome P450 enzymes for metabolism of sodium tanshinone IIA sulfonate in vitro.

Chinese medicine

Ouyang DS, Huang WH, Chen D, Zhang W, Tan ZR, Peng JB, Wang YC, Guo Y, Hu DL, Xiao J, Chen Y.
PMID: 27006687
Chin Med. 2016 Mar 22;11:11. doi: 10.1186/s13020-016-0083-z. eCollection 2016.

BACKGROUND: Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA for treating cardiovascular disorders. The roles of cytochrome P450 enzymes (CYPs) in the metabolism of STS have remained unclear. This study aims to screen the main...

Optical purity determination and (1)H NMR spectral simplification with lanthanide shift reagents - V. Mephenytoin, 5-ethyl-3-methyl-5-phenyl-2,4-imidazolidinedione.

Journal of pharmaceutical and biomedical analysis

Avolio J, Rothchild R.
PMID: 16867720
J Pharm Biomed Anal. 1984;2(3):403-8. doi: 10.1016/0731-7085(84)80043-6.

The 60-MHz 1H NMR spectra of racemic mephenytoin, I, have been studied with the achiral shift reagent, tris(6,6,7,7,8,8,8-heptafluoro-2,2-dimethyl-3,5-octane-dionato) europium (III), II, and the chiral reagent, tris[3-(trifluoromethylhydroxy-methylene)-d-camphorato] europium (III), III. Moderate values of the enantiomeric shift differences, Delta, were clearly...

An in-vitro cocktail assay for assessing compound-mediated inhibition of six major cytochrome P450 enzymes.

Journal of pharmaceutical analysis

Wang JJ, Guo JJ, Zhan J, Bu HZ, Lin JH.
PMID: 29403890
J Pharm Anal. 2014 Aug;4(4):270-278. doi: 10.1016/j.jpha.2014.01.001. Epub 2014 Feb 14.

An efficient screening assay was developed and validated for simultaneous assessment of compound-mediated inhibition of six major human cytochrome P450 (CYP) enzymes. This method employed a cocktail of six probe substrates (i.e., phenacetin, amodiaquine, diclofenac, S-mephenytoin, dextromethorphan and midazolam...

Impact of P450 genetic polymorphism on the first-pass extraction of cardiovascular and neuroactive drugs.

Advanced drug delivery reviews

Eichelbaum M, Kroemer HK, Fromm MF.
PMID: 10837557
Adv Drug Deliv Rev. 1997 Sep 15;27(2):171-199. doi: 10.1016/s0169-409x(97)00042-2.

This review highlights the present knowledge on the CYP2D6 (sparteine/debrisoquine) and the CYP2C19 (mephenytoin) polymorphisms. The relevant mutations at genomic level affecting protein expression and function and consequences for first-pass metabolism and effects of cardiovascular and neuroactive drugs are...

In vitro inhibitory effect of 1-aminobenzotriazole on drug oxidations catalyzed by human cytochrome P450 enzymes: a comparison with SKF-525A and ketoconazole.

Drug metabolism and pharmacokinetics

Emoto C, Murase S, Sawada Y, Jones BC, Iwasaki K.
PMID: 15618748
Drug Metab Pharmacokinet. 2003;18(5):287-95. doi: 10.2133/dmpk.18.287.

1-Aminobenzotriazole (ABT) is widely used as a non-specific inhibitor of animal cytochrome P450 (CYP). In the present study, the inhibitory effect of ABT was investigated on drug oxidations catalyzed by human CYP isoforms. This inhibitory effect was compared with...

Molecular cloning of monkey CYP2C43 cDNA and expression in yeast.

Drug metabolism and pharmacokinetics

Matsunaga T, Ohmori S, Ishida M, Sakamoto Y, Nakasa H, Kitada M.
PMID: 15618659
Drug Metab Pharmacokinet. 2002;17(2):117-24. doi: 10.2133/dmpk.17.117.

A cDNA clone designated as CYP2C43 was isolated from the rhesus monkey liver cDNA library. The first 16 amino acid residues at the N-terminal region of this cDNA product were identical with those of P450 CMLd which have been...

Application of microtiter plate assay to evaluate inhibitory effects of various compounds on nine cytochrome P450 isoforms and to estimate their inhibition patterns.

Drug metabolism and pharmacokinetics

Yamamoto T, Suzuki A, Kohno Y.
PMID: 15618695
Drug Metab Pharmacokinet. 2002;17(5):437-48. doi: 10.2133/dmpk.17.437.

Using a microtiter plate (MTP) assay consists of recombinant cytochromes P450 and fluorescent probes, we evaluated inhibitory effects of commercially available model-compounds, 18 typical substrates and 8 selective inhibitors, on nine cytochromes P450 (CYPs) activities. The IC(50) values obtained...

A Physiologically-Based Pharmacokinetic (PBPK) Model Network for the Prediction of CYP1A2 and CYP2C19 Drug-Drug-Gene Interactions with Fluvoxamine, Omeprazole, S-mephenytoin, Moclobemide, Tizanidine, Mexiletine, Ethinylestradiol, and Caffeine.

Pharmaceutics

Kanacher T, Lindauer A, Mezzalana E, Michon I, Veau C, Mantilla JDG, Nock V, Fleury A.
PMID: 33302490
Pharmaceutics. 2020 Dec 08;12(12). doi: 10.3390/pharmaceutics12121191.

Physiologically-based pharmacokinetic (PBPK) modeling is a well-recognized method for quantitatively predicting the effect of intrinsic/extrinsic factors on drug exposure. However, there are only few verified, freely accessible, modifiable, and comprehensive drug-drug interaction (DDI) PBPK models. We developed a qualified...

Metabolism of selegiline hydrochloride, a selective monoamine b-type inhibitor, in human liver microsomes.

Drug metabolism and pharmacokinetics

Kamada T, Chow T, Hiroi T, Imaoka S, Morimoto K, Ohde H, Funae Y.
PMID: 15618670
Drug Metab Pharmacokinet. 2002;17(3):199-206. doi: 10.2133/dmpk.17.199.

The participation of cytochrome P-450 (CYP) isoforms in the metabolism of selegiline was investigated. Experiments using recombinant CYP isoforms expressed in human lymphoblastoid cells showed CYP2B6 to be the major CYP isoform involved with the metabolism of selegiline. CYP1A2...

High Expression of Human CYP2C in Immortalized Human Liver Epithelial Cells.

Toxicology in vitro : an international journal published in association with BIBRA

Bort R, Castell JV, Pfeifer A, Gómez-Lechón MJ, Macé K.
PMID: 20654527
Toxicol In Vitro. 1999 Aug-Oct;13(4):633-8. doi: 10.1016/s0887-2333(99)00069-7.

Cell lines stably expressing high levels of single isozymes of human CYP2C genes (CYP2C8, CYP2C9, CYP2C18 and CYP2C19) have been successfully generated by transfecting liver epithelial human cells (THLE) with an appropriate expression vector. To this aim, cDNAs encoding...

High-Throughput, 384-Well, LC-MS/MS CYP Inhibition Assay Using Automation, Cassette-Analysis Technique, and Streamlined Data Analysi.

Drug metabolism letters

Halladay JS, Delarosa EM, Tran D, Wang L, Wong S, Khojasteh SC.
PMID: 21824084
Drug Metab Lett. 2011 Aug 09; Epub 2011 Aug 09.

Here we describe a high capacity and high-throughput, automated, 384-well CYP inhibition assay using well-known HLM-based MS probes. We provide consistently robust IC(50) values at the lead optimization stage of the drug discovery process. Our method uses the Agilent...

In Vitro Assessment of Cytochrome P450 2C19 Potential of Naoxintong.

Evidence-based complementary and alternative medicine : eCAM

Chen H, Zhang Y, Wu X, Li C, Wang H.
PMID: 22454664
Evid Based Complement Alternat Med. 2012;2012:430262. doi: 10.1155/2012/430262. Epub 2012 Feb 16.

The effects of Buchang Naoxintong Capsules (BNCs) on S-mephenytoin 4'-hydroxylation activities in human liver microsomes in vitro were assessed. Human liver microsome was prepared by different ultracentrifugation. Human liver microsome incubation experiment was carried out to assay BNC on...

Showing 1 to 12 of 20 entries