New Perspectives on Acyl Glucuronide Risk Assessment in Drug Discovery: Investigation of In vitro Stability, In situ Reactivity, and Bioactivation [0.03%]
药物发现中酰基葡萄糖醛酸酯风险评估的新视角：体外稳定性、原位反应性及生物活化作用的考察
Mithat Gunduz,Upendra A Argikar,Amanda L Cirello et al.
Mithat Gunduz et al.
Background: Acyl glucuronides of xenobiotics have been a subject of wide interest from the pharmaceutical industry with respect to biochemical reactivity, hepatic disposition, and enterohepatic circulation. The reactivity...
Effects of Tobacco Nicotine-Derived Nitrosamine Ketone (NNK) Exposures on Brain Alcohol Metabolizing Enzyme Activities [0.03%]
尼古丁亚硝胺酮对脑内酒精代谢酶活性的影响
Emine B Yalcin,Ming Tong,Gina Gallucci et al.
Emine B Yalcin et al.
Background: The high levels of blood alcohol achieved with chronic plus binge alcohol exposures are somewhat reduced by co-administration of tobacco-specific Nicotine-Derived Nitrosamine Ketone (NNK) suggesting that NNK m...
Effect of CYP2D6 Poor Metabolizer Phenotype on Stereoselective Nebivolol Pharmacokinetics [0.03%]
CYP2D6慢代谢表型对奈必洛尔手性异构体药代动力学的影响
Carolina P Vieira,Daniel V Neves,Eduardo B Coelho et al.
Carolina P Vieira et al.
Background: Nebivolol is a drug available as a racemate of d-nebivolol (SRRR) and lnebivolol (RSSS). In human liver microsomes, CYP2D6 mainly catalyses the metabolism of lnebivolol, while CYP2C19 catalyses the metabolism ...
In vitro Drug Metabolism Investigation of 7-Ethoxycoumarin in Human, Monkey, Dog and Rat Hepatocytes by High Resolution LC-MS/MS [0.03%]
高效液相色谱质谱联用技术在四种物种肝细胞体外代谢研究中的应用
Wan-Yong Feng,Jenny Wen,Kathe Stauber
Wan-Yong Feng
Background: Recently, it has been an increasing concern on the bioactivation and adverse reactions associated with consumption of herbal and nature products. 7-Ethoxycoumarin is one of coumarin family compounds, but littl...
Evaluation of the Effect of Uremic Serum on Hepatic Reductase Functional Expression [0.03%]
尿毒症血清对肝细胞还原酶功能表达影响的评估研究
Osama Y Alshogran,Esra A F Al-Obaidi,Belal A Al-Husein et al.
Osama Y Alshogran et al.
Background: The nonrenal clearance of drugs mediated by hepatic reduction is selectively altered by kidney disease. This study evaluated the influence of uremic serum on the expression and activity of reductase enzymes. ...
Cytochrome P450 3A4 Induction: Lumacaftor versus Ivacaftor Potentially Resulting in Significantly Reduced Plasma Concentration of Ivacaftor [0.03%]
细胞色素P450 3A4诱导作用：Lumacaftor与Ivacaftor联用可能会显著降低后者的血浆浓度
Elena K Schneider
Elena K Schneider
Background & objective: Since the release of ivacaftor-lumacaftor, several red-flags have been raised that highlight the clinical efficacy of this combination strategy that may be limited due to antagonistic drug-drug int...
Characterization of Liver- and Cancer-type-Organic Anion Transporting Polypeptide (OATP) 1B3 Messenger RNA Expression in Normal and Cancerous Human Tissues [0.03%]
人正常和肿瘤组织肝脏及癌症型有机阴离子转运多肽(OATP)1B3信使核糖核酸表达的特征研究
Khondoker Alam,Taleah Farasyn,Kai Ding et al.
Khondoker Alam et al.
Background: Membrane transport protein organic anion transporting polypeptide (OATP) 1B3 mediates the cellular uptake of many clinically important drugs including anti-cancer drugs (e.g., paclitaxel). In addition to the w...
Evaluation of Herb-Drug Interaction of Synacinn™ and Individual Biomarker through Cytochrome 450 Inhibition Assay [0.03%]
Synacinn™及个体生物标志物的 herbal-drug相互作用评价与细胞色素450抑制试验
Nur Syukriah Ab Rahman,Fadzilah Adibah Abd Majid,Mohd Effendy Abd Wahid et al.
Nur Syukriah Ab Rahman et al.
Background: SynacinnTM contains five standardized herbal extracts of Orthosiphon Stamineus (OS), Syzygium polyanthum (SZ), Curcuma xantorrizza (CX), Cinnamomum zeylanicum (CZ) and Andrographis paniculata (AP) and is stand...
LC-MS/MS Identification and Structural Characterization of Main Biodegradation Products of Nitroproston - A Novel Prostaglandin-based Pharmaceutical Compound [0.03%]
新型前列腺素类药物硝基普罗松龙的主要降解产物的鉴定及结构表征
Natalia V Mesonzhnik,Natalia E Moskaleva,Ksenia M Shestakova et al.
Natalia V Mesonzhnik et al.
Background: Nitroproston is a novel prostaglandin-based compound modified by NOdonating groups with potential application in obstructive respiratory diseases such as asthma and obstructive bronchitis. Nitroproston has bee...
Cytochrome P450 1A2 Messenger RNA is a More Reliable Marker than Cytochrome P450 1A2 Activity, Phenacetin O-Deethylation, for Assessment of Induction Potential of Drug-Metabolizing Enzymes Using HepaRG Cells [0.03%]
他达拉非用药过程中发生药物相互作用的潜在风险：与细胞色素P450酶诱导相关的体外和临床数据
Akira Ogasawara,Nozomu Kato,Nao Torimoto et al.
Akira Ogasawara et al.
Background: The HepaRG cells have key drug metabolism functionalities comparable to those of primary human hepatocytes. Many studies have reported that this cell line can be used as a reliable in vitro model for human dru...