نتایج جستجو برای: cyp1a2

تعداد نتایج: 1781  

2012

Phenacetin is widely used as an in vitro probe to measure CYP1A2 activity across species. To investigate whether phenacetin can be used as an in vivo probe substrate to phenotype CYP1A2 activity in dogs, beagle dogs previously genotyped for a single nucleotide polymorphism that yields an inactive CYP1A2 protein were selected and placed into one of three groups: CC (wild-type), CT (heterozygous)...

2016
Paul Quehl Joel Hollender Jan Schüürmann Tatjana Brossette Ruth Maas Joachim Jose

BACKGROUND Human cytochrome P450 (CYP) enzymes mediate the first step in the breakdown of most drugs and are strongly involved in drug-drug interactions, drug clearance and activation of prodrugs. Their biocatalytic behavior is a key parameter during drug development which requires preparative synthesis of CYP related drug metabolites. However, recombinant expression of CYP enzymes is a challen...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2000
J S Wang J T Backman P Taavitsainen P J Neuvonen K T Kivistö

The roles of cytochrome P-450 (CYP) enzymes in the N-deethylation, i.e., formation of monoethylglycinexylidide (MEGX), and 3-hydroxylation of lidocaine were studied with human liver microsomes and recombinant human CYP isoforms. Both CYP1A2 and CYP3A4 were found to be capable of catalyzing the formation of MEGX and 3-OH-lidocaine. Lidocaine N-deethylation by liver microsomes was strongly inhibi...

Journal: :Cancer science 2010
Xiang-Rui Wang Zeng-Qiang Qu Xiao-Dong Li Hai-Lin Liu Ping He Bei-Xiong Fang Jie Xiao Wei Huang Meng-Chao Wu

The phase I metabolizing enzyme and phase II metabolizing enzyme play vital roles in carcinogenesis, but little is known about the changes of their activities in patients with hepatocellular carcinoma (HCC) secondary to chronic hepatitis B virus (HBV) infection. In this study phenacetin, a probe drug (1 g for men and 0.85 g for women orally), was applied for the detection of sulfotransferase 1A...

Journal: :Carcinogenesis 1998
F G Crofts T R Sutter P T Strickland

While the metabolic activation of 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) by N-hydroxylation has been well documented, the relative roles of the human cytochrome P450 (CYP) enzymes that catalyze this reaction have not been established. Previous studies indicated that the mutagenic activation product, 2-hydroxyamino-PhIP (N2-OH-PhIP), is produced primarily by CYP1A2, and to a less...

Journal: :Evidence-based complementary and alternative medicine : eCAM 2016
Zhongnv Ma Xianbao Shi Gang Zhang Feng Guo Lina Shan Jiqun Cai

Cytochrome p450 (CYP450) enzymes are predominantly involved in Phase I metabolism of xenobiotics. In this study, the CYP450 isoforms involved in xanthotoxol metabolism were identified using recombinant CYP450s. In addition, the inhibitory effects of xanthotoxol on eight CYP450 isoforms and its pharmacokinetic parameters were determined using human liver microsomes. CYP1A2, one of CYP450s, playe...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2000
S i Kuriya S Ohmori M Hino I Ishii H Nakamura C Senda T Igarashi M Kiuchi M Kitada

Pimobendan, 4, 5-dihydro-6-(2-(4-methoxyphenyl)-1H-benzimidazol-5-yl)-5-methyl-3( 2-H )-pyridazinone, is a new inotropic drug that augments Ca(2+) sensitivity and inhibits phosphodiesterase in cardiomyocytes. Pimobendan is well absorbed after oral administration and is metabolized in the liver to the O-demethyl metabolite, which is also active. This study was conducted to identify the cytochrom...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2012
Kaori Yasuda Shinichi Ikushiro Shuto Wakayama Toshimasa Itoh Keiko Yamamoto Masaki Kamakura Eiji Munetsuna Miho Ohta Toshiyuki Sakaki

Sesamin and episesamin are two epimeric lignans that are found in refined sesame oil. Commercially available sesamin supplements contain both sesamin and episesamin at an approximate 1:1 ratio. Our previous study clarified the sequential metabolism of sesamin by cytochrome P450 (P450) and UDP-glucuronosyltransferase in human liver. In addition, we revealed that sesamin caused a mechanism-based ...

Journal: :Journal of occupational health 2004
Ana Fanlo Blanca Sinuès Esteban Mayayo Luisa Bernal Antonia Soriano Begoña Martínez-Jarreta Enrique Martínez-Ballarín

The two major causes of bladder cancer have been recognised to be cigarette smoke and occupational exposure to arylamines. These compounds are present both in tobacco smoke and in the dyes used in textile production. Aromatic amines suffer oxidative metabolism via P450 cytochrome CYP1A2, and detoxification by the polymorphic NAT2. The aim of the present work was to assess the association betwee...

1997
A. DAVID RODRIGUES BRUCE W. SURBER YE YAO SHEKMAN L. WONG ELLEN M. ROBERTS

The activity of human liver microsomal cytochrome P450 1A2 (CYP1A2) is readily estimated by following the O-deethylation of [O-ethyl C]phenacetin (PODase). The basis of the assay is the quantitative measurement of [C]acetaldehyde, remaining in the supernatant of assay incubates, after extraction of unmetabolized [O-ethyl C]phenacetin with charcoal. In the presence of native human liver microsom...

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