A5087074582- Pharmacogenetics and Drug Metabolism
- Analytical Chemistry and Chromatography
- Mass Spectrometry Techniques and Applications
- Drug Transport and Resistance Mechanisms
- Synthesis and Biological Evaluation
- Analytical Methods in Pharmaceuticals
- Antibiotics Pharmacokinetics and Efficacy
- Porphyrin and Phthalocyanine Chemistry
- Phenothiazines and Benzothiazines Synthesis and Activities
- Renal Transplantation Outcomes and Treatments
- Pesticide Residue Analysis and Safety
- DNA and Nucleic Acid Chemistry
- Metabolomics and Mass Spectrometry Studies
- Pharmacological Effects and Toxicity Studies
- Analytical chemistry methods development
- Drug-Induced Hepatotoxicity and Protection
- Asymmetric Synthesis and Catalysis
- Pharmaceutical studies and practices
- Computational Drug Discovery Methods
- Hormonal and reproductive studies
- Pharmacological Effects of Natural Compounds
- Chemical Reaction Mechanisms
- Diet and metabolism studies
- Cancer therapeutics and mechanisms
- Advanced NMR Techniques and Applications
Osaka University
1972-2018
Shimadzu (Japan)
2018
Sekisui Medical (Japan)
2010-2013
BioAssay Systems (United States)
2009
Daiichi-Sankyo (Japan)
2007
Daiwa Pharmaceutical Co. (Japan)
1982-2005
Osaka Red Cross Hospital
2004
Mochida Pharmaceutical (Japan)
1995-1996
Osaka University of Pharmaceutical Sciences
1985
Fujisawa City Hospital
1982-1983
Abstract A series of multilayered cyclophanes up to sixfold were synthesized by 1,6-Hofmann elimination method. Odd layered and some dissymmetric ones derived means cross-breeding pyrolysis mixed quaternary ammonium hydroxides. The electronic spectra, absorption, emission, CT absorption charge-transfer complexes, these exhibited remarkable transannular π-electronic interaction among chromophores closely stacked methylene bridges. is increased eminently when the layer varied from single...
To characterize structures and biological activities of FK506 metabolites, was incubated with liver microsomes prepared from phenobarbital-treated rats in the presence NADPH generating system under aerobic condition. Oxidative metabolites formed reaction medium were isolated identified. Purified samples analyzed by HPLC, mass spectrometry, NMR spectroscopy. M-I, M-II, M-III O-demethylated at 13-, 31-, 15-positions FK506, respectively, M-IV monohydroxylated metabolite 12-position. M-I...
A study of the pharmacokinetics (14)C-labeled acetaminophen (AAP) was performed in healthy Japanese subjects receiving an oral microdose drug. After separation by high-performance liquid chromatography (HPLC), levels AAP and its metabolites pooled plasma specimens were quantified using accelerator mass spectrometry (AMS). The total body clearance (CL(tot))/bioavailability (F) within variation reported values at therapeutic doses, indicating linearity pharmacokinetics. AAP-glucuronide (Glu)...
Covalent binding of reactive metabolites to cytochrome P450s (P450s) often causes their mechanism-based inactivation (MBI), resulting in drug-drug interactions or toxicity. The detection and identification the P450 sites which bind would elucidate MBI mechanisms. We describe a proteomic approach using nano-LC/linear ion trap-Fourier transform cyclotron resonance (FTICR) mass spectrometry characterize metabolite raloxifene, is known 3A4 inhibitor, isozyme. LTQ-FT analyses revealed that...
Fexofenadine is a P-glycoprotein substrate of low bioavailability. It primarily excreted into faeces as parent drug via biliary excretion. The predictability from microdose data for the absorbed transporters such not known. Therefore, this study assessed therapeutic-dose pharmacokinetics fexofenadine microdosing using non-radioisotope-labelled and liquid chromatography/electrospray ionization tandem mass spectrometry (LC/ESI-MS/MS).In single dose, randomized, two-way crossover study, eight...
Null mutation of glutathione transferase (<i>GST</i>) <i>M1</i> and <i>GSTT1</i> was reported to correlate statistically with an abnormal increase in the plasma levels alanine aminotransferase or aspartate caused by troglitazone diabetic patients (<i>Clin Pharmacol Ther</i>, 73:435–455, 2003). This clinical evidence leads hypothesis that GSH conjugation catalyzed GSTT1 GSTM1 has a role elimination reactive metabolites troglitazone. However, contribution GST isoforms expressed human liver...
FK228 (FR901228, depsipeptide) is a potent histone deacetylase inhibitor currently in phase II clinical trials for cancer treatment. In the present study, cytochrome P450 (P450) enzymes responsible metabolism human liver microsomes were investigated. Incubation with presence of an NADPH-generating system revealed that metabolized to at least 10 different metabolites. Km and Vmax values disappearance 20.3 microM 561.9 pmol/min/mg protein, respectively. Further studies performed substrate...
The purpose of this study was to develop quantitative liquid chromatography-tandem mass spectrometry (LC-MS/MS) methods for the analysis proteins involved in metastasis breast cancer diagnosis and determining disease prognosis, as well further our understand metastatic mechanisms. We have previously demonstrated that protein type XIV collagen may be specifically expressed tissues by two dimensional LC-MS/MS. In study, we developed LC-MS/MS collagen. Type quantified analyzing 2 peptides...
1. Studies using human liver microsomes and recombinant cytochrome P450 (P450) enzymes flavin-containing monooxygenase (FMO) were performed to identify the responsible for formation of zotepine metabolites in man. 2. Human produced four a tentative order importance was: norzotepine, 3-hydroxyzotepine, S-oxide 2-hydroxyzotepine. Zotepine N-oxide was also detected, but it could not be quantified. 3. The rates major metabolite, (at substrate concentration 20 microM) significantly correlated...
1. Species and sex differences in testosterone hydroxylation nifedipine oxidation liver microsomes from rat, dog monkey have been investigated.2. The formation of 2α-, 2β-, 6β-, 16α-hydroxytestosterone androstenedione the male rat was higher than that female rat. Microsomes prepared oxidized about eight times faster did those In contrast, marked sex-related were not seen monkey.3. Nifedipine oxidase activity correlated significantly with activities for both 2β-hydroxylation 6β-hydroxylation,...
A new condensing reagent 1 -(2,4,6-triisoprophylbenzenesulfonyl)-5-(pyridin-2-y1)tetrazolide (TPSPy) was found to give one diastereoisomer of dinucleoside monophosphate aryl esters. Several oligodeoxynucleotide blocks were prepared using this reagent. heptadecanucleotide .dTATCCCTTGCGGTGATA, which had the same sequence as λ cro binding DNA synthesized by mono-, tri- and dodecanucleotide on a polystyrene support.