The Metabolism of Methazolamide in Immortalized Human Keratinocytes, HaCaT Cells [0.03%]
甲氯芬酯在人永生化角质细胞系HaCaT细胞中的代谢研究
Tetsuo Sasabe,Shinichiro Maeda,Kenichi Kishida et al.
Tetsuo Sasabe et al.
Objective: Drug therapy is occasionally accompanied by an idiosyncratic severe toxicity, which occurs very rarely, but can lead to patient mortality. Methazolamide, an anti-glaucomatous agent, could cause severe skin erup...
Pharmacokinetics, Metabolism and Disposition of [14C]XQ-1H After Intravenous Administration to Male Rats [0.03%]
静脉注射XQ-1H后大鼠的药代动力学、代谢及排泄研究
Yinlin Qin,Tao Chen,Qiu Jin et al.
Yinlin Qin et al.
Objective: This study describes the in vivo pharmacokinetics and metabolism of [14C]labeled XQ-1H in male rats. Methods: XQ-1H is a met...
Quantification of Etodolac in Human Plasma for Pharmacokinetics and Bioequivalence Studies in 27 Korean Subjects [0.03%]
一种测定乙基多炎凯的人血浆中浓度的方法用于药代动力学及生物等效性研究(Korean subjects)
Il-Dong Song,Ju-Seop Kang,Hyun-Jin Kim et al.
Il-Dong Song et al.
Objective: We developed a simple and validated liquid chromatography tandem mass spectrometry( LC-MS/MS) for quantification of etodolac using pioglitazone as an internal standard (IS) to assess pharmacokinetics and to app...
Variability of Zaleplon 5-Oxidase Activity in Mice and Humans, and Inhibition by Raloxifene [0.03%]
唑吡坦5-氧化酶活性的种间差异及雷洛昔芬对其的抑制作用
Chiaki Tanoue,Kazumi Sugihara,Yoshitaka Tayama et al.
Chiaki Tanoue et al.
Background: Zaleplon (ZAL) is a sedative-hypnotic agent, which is mainly metabolized to inactive 5-oxidized zaleplon (5-oxo-ZAL) and N-des-ethylated ZAL (des-ethyl-ZAL) in mice and humans. The former reaction is considere...
Ortho-Methylarylamines as Time-Dependent Inhibitors of Cytochrome P450 1A1 Enzyme [0.03%]
ortho-甲基芳氨化合物作为时间依赖性的细胞色素P450 1A1抑制剂
Jayalakshmi Sridhar,Jiawang Liu,Rajesh Komati et al.
Jayalakshmi Sridhar et al.
Background: Members of the cytochrome P450 1A family metabolize many procarcinogens such as polycyclicaromatic hydrocarbons and heterocyclic amines. Inactivation of these enzymes is a prerequisite for cancer prevention an...
A Novel Liquid Chromatography Tandem Mass Spectrometry Method for the Estimation of Bilirubin Glucuronides and its Application to In Vitro Enzyme Assays [0.03%]
一种新型液相色谱-串联质谱法用于测定胆红素葡萄糖醛酸酯及其在体外酶分析中的应用
Siva P Putluru,Murali K Matta,Deepak Ahire et al.
Siva P Putluru et al.
Background: Bilirubin is a toxic waste product of metabolism, eliminated mainly through UGT1A1 mediated conjugation to mono- and di-glucuronides. Due to the potentially low Km value of bilirubin glucuronidation, the quant...
Cytochrome P450 2A6 Phenotyping Using Dietary Caffeine Salivary Metabolite Ratios and Genotyping Using Blood on Storage Cards in Non-smoking Japanese Volunteers [0.03%]
利用储藏卡血液基因型和非吸烟日本志愿者饮食咖啡因测定细胞色素P450 2A6表型的比例唾液代谢物比率
Norie Murayama,Makiko Shimizu,Kenta Kobayashi et al.
Norie Murayama et al.
Background: A simple method of genotyping and phenotyping cytochrome P450 2A6 (CYP2A6) was previously reported using individual blood samples and urinary caffeine metabolite ratios of 1,7-dimethyluric acid (17U) to 1-meth...
Strong Induction of Cytochrome P450 1A/3A, But not P450 2B, in Cultured Hepatocytes from Common Marmosets and Cynomolgus Monkeys by Typical Human P450 Inducing Agents [0.03%]
典型的人体P450诱导剂对常见狨猴和食蟹猕猴原代肝细胞中CYP1A/3A但不是CYP2B的强诱导作用
Shotaro Uehara,Yasuhiro Uno,Takako Suzuki et al.
Shotaro Uehara et al.
Background: Common marmosets (Callithrix jacchus) and cynomolgus monkeys (Macaca fascicularis) are used as non-human primate models in preclinical studies for drug development. ...
Genipin Inhibits the Induction of Inducible Nitric Oxide Synthase Through the Inhibition of NF-κB Activation in Rat Hepatocytes [0.03%]
绞股蓝明矾抑制NF-κB活化从而抑制诱导型一氧化氮合酶的诱导作用
Richi Nakatake,Takumi Tsuda,Takashi Matsuura et al.
Richi Nakatake et al.
Background/aims: Genipin is a component of Japanese traditional herbal medicine (Kampo), inchinkoto, and is used for the treatment of various liver injuries. However, there are few scientific evidence for its anti-inflamm...
Application of a "Fit for Purpose" PBPK Model to Investigate the CYP3A4 Induction Potential of Enzalutamide [0.03%]
用于评估恩扎卢胺CYP3A4诱导潜能的“适合目的”的PBPK模型应用研究
Rangaraj Narayanan,Matthew Hoffmann,Gondi Kumar et al.
Rangaraj Narayanan et al.
Background: Oncology therapy typically involves drug combinations since monotherapy seldom provides the desired outcome. But combination therapy presents the potential for drug-drug interactions (DDIs). Due to the narrow ...