New Screening Criteria Setting on Evaluation of Cytochrome P450 Induction Using HepaRG Cells with Multiplex Branched DNA Technologies in Early Drug Discovery [0.03%]
基于HepaRG细胞的多重分支DNA技术在药物早期研发中用于评估CYP诱导的新筛选标准设定
Akira Ogasawara,Nao Torimoto,Naoki Tsuda et al.
Akira Ogasawara et al.
Background: Cytochrome P450 (CYP) enzymes are induced by some therapeutic drugs, leading to interactions reducing drug plasma concentrations. Recently, an assessment of CYP induction using messenger RNA (mRNA) levels has ...
Comparative Study
Drug metabolism letters. 2016;10(3):152-160. DOI:10.2174/1872312810666160822110011 2016
CYP2B6 and OPRM1 Receptor Polymorphisms at Methadone Clinics And Novel OPRM1 Haplotypes: A Cross-Sectional Study [0.03%]
阿片受体多态性和新型阿片受体基因型：横断面研究
Ahmad Abdulrahman AlMeman,Rusli Ismail,Markus Perola
Ahmad Abdulrahman AlMeman
Introduction: Methadone is accepted as an alternative therapy in opioid use disorders worldwide. Methadone responsiveness, however, is affected by a range of CYP450 enzymes and OPRM1 polymorphisms. ...
Multicenter Study
Drug metabolism letters. 2016;10(3):213-218. DOI:10.2174/1872312810666160810104040 2016
Intracellular Retention of Three Quinuclidine Derivatives in Caco-2 Permeation Experiments: Mechanisms and Impact on Estimating Permeability and Active Efflux Ratio [0.03%]
三种喹尼克立丁衍生物在Caco-2渗透实验中的胞内滞留：机制及对通透性和主动外排比率估算的影响
Hong Jin,Sudarshan Kapadnis,Ting Chen et al.
Hong Jin et al.
Background: Three quinuclidine derivatives (FRM-1, FRM-2 and FRM-3) were subject to significant mass loss to cellular retention in Caco-2 permeation experiments. The apparent permeability coefficient (Papp) calculated wit...
UHPLC Quantitation Method for New Thiazolidinedione LPSF/GQ-02 and In Vitro/In Vivo Kinetic Studies [0.03%]
新型环格列汀(LPSF/GQ-02)的UHPLC定量分析方法及其体内外动力学研究
Carla Monalizi Vieira,Michel Leandro de Campos,Elias Carvalho Padilha et al.
Carla Monalizi Vieira et al.
Background: LPSF/GQ-02 is a promising benzylidene thiazolidinedione that has demonstrated antidiabetic, antidyslipidemic, anti-atherosclerotic properties and can also treat non-alcoholic fatty liver disease. Despite all a...
Identification and Characterization of the Human Cytosolic Sulfotransferases Mediating the Sulfation of Clioquinol and Iodoquinol [0.03%]
人细胞质多聚泛素链特异性的硫酸转移酶的鉴定与特征分析：克利奥喹诺和碘喹诺的硫酸化作用
Akihiro Yamamoto,Maame Debrah-Pinamang,Nicholas J DiModica et al.
Akihiro Yamamoto et al.
Objective: The aim of the current study was to identify the human cytosolic sulfotransferases (SULTs) that are capable of sulfating clioquinol and iodoquinol, and to verify the presence of clioquinol/ iodoquinol-sulfating...
The Uremic Toxin Indoxyl-3-Sulfate Induces CYP1A2 In Primary Human Hepatocytes [0.03%]
尿毒症毒素吲哚硫酸盐诱导CYP1A2在人原代肝细胞中的表达
Hong Liu,Rangaraj Narayanan,Matthew Hoffmann et al.
Hong Liu et al.
Chronic kidney disease (CKD) generally impacts clearance of renally eliminated drugs but growing evidence shows that it can influence clearance of hepatically eliminated drugs and a complete mechanistic understanding of this phenomenon is s...
Comparative Study
Drug metabolism letters. 2016;10(3):195-199. DOI:10.2174/1872312810666160719143703 2016
The Uremic Toxin Indoxyl-3-Sulfate Induces CYP1A2 In Primary Human Hepatocytes [0.03%]
尿毒症毒素吲哚硫酸盐诱导CYP1A2在人原代肝细胞中的表达
Hong Liu,Rangaraj Narayanan,Matthew Hoffmann et al.
Hong Liu et al.
Chronic kidney disease (CKD) generally impacts clearance of renally eliminated drugs but growing evidence shows that it can influence clearance of hepatically eliminated drugs and a complete mechanistic understanding of this phenomenon is s...
Comparative Study
Drug metabolism letters. 2016;10(3):195-199. DOI:10.2174/1872312810666160719143703 2016
Suresh K Balani
Suresh K Balani
Inhibition of Procarcinogen Activating Enzyme CYP1A2 Activity and Free Radical Formation by Caffeic Acid and its Amide Analogues [0.03%]
咖啡酸及其酰胺类似物对前致癌激活酶CYP1A2活性和自由基形成的抑制作用
Paitoon Narongchai,Kanokporn Niwatananun,Siripun Narongchai et al.
Paitoon Narongchai et al.
Objectives: Caffeic acid (CAF) and its amide analogues, ethyl 1-(3',4'-dihydroxyphenyl) propen amide (EDPA), phenethyl 1-(3',4'-dihydroxyphenyl) propen amide (PEDPA), phenmethyl 1- (3',4'-dihydroxyphenyl) propen amide (PM...
Effect of Cardiovascular Injury on Catabolism of Adenosine and Adenosine 5-'Triphosphate in Systemic Blood in a Freely Moving Rat Model In Vivo [0.03%]
心血管损伤对活体自由活动大鼠全身血中腺苷和三磷酸腺苷降解的影响
Pollen K Yeung,Shyam S Kolathuru,Remigius U Agu
Pollen K Yeung
Background: Previous studies have shown that catabolism of adenosine 5'-triphosphate (ATP) in red blood cell (RBC) may be a key factor for cardiovascular protection and maintaining cardiovascular homeostasis. ...