Liquid chromatography-tandem mass spectrometry-based pharmacokinetic and metabolic analysis of 4-bromo-2,5-dimethoxyphenethylamine and its metabolites in human plasma [0.03%]
基于液相色谱-串联质谱法的人血浆中4-溴-2，5-二甲氧基苯乙胺及其代谢物的药代动力学和代谢分析
Jan Thomann,Deborah Rudin,Selina Kraus et al.
Jan Thomann et al.
4-Bromo-2,5-dimethoxyphenethylamine (2C-B) is widely used recreationally and has recently gained interest as a treatment for mental health disorders. In this study, a liquid chromatography-tandem mass spectrometry method to quantify 2C-B an...
Quantitative distribution of theobromine in mouse brain regions and its mitigation of nicotine withdrawal-induced anxiety and depression through neuroinflammation suppression [0.03%]
定量分布于小鼠脑区的茶碱及其通过抑制神经炎症来缓解尼古丁戒断引起的焦虑和抑郁作用研究
Shihua Xu,Yu Tian,Xiaofei Chen et al.
Shihua Xu et al.
Nicotine withdrawal is often accompanied by anxiety and depression-like behaviors, which are closely linked to neuroinflammation. Theobromine (TB), a bioactive compound found in cocoa, has demonstrated potential anti-inflammatory and neurop...
The impact of progressive chronic kidney disease on hepatic drug metabolism [0.03%]
慢性进行性肾病对肝脏药物代谢的影响
Emily D Hartjes,Yong Jin Lim,Thomas J Velenosi et al.
Emily D Hartjes et al.
Nonrenal clearance pathways such as drug metabolism are decreased in severe chronic kidney disease (CKD). The impact of progression of CKD on hepatic drug metabolism is unknown. We characterized the effect of progressive CKD on hepatic cyto...
Integrated strategy for biotransformation of antibody-drug conjugates and multidimensional interpretation via high-resolution mass spectrometry [0.03%]
基于高分辨质谱的抗体药物偶联物生物转化整合策略及多维解析方法
Ziyi Li,Jingxian Zhang,Yue Wu et al.
Ziyi Li et al.
The characterization of the release mechanism and stability in circulation for novel antibody-drug conjugates (ADCs) has become essential to address the complex variables (linker or payload selection, antibody, conjugating site). Understand...
Identification of selective inhibitors of uridine 5'-diphospho-glucuronosyltransferase (UGT) 1A3 and UGT1A8 and their application in UGT reaction phenotyping studies in human liver and intestinal microsomes [0.03%]
尿苷二磷酸-葡萄糖醛酸转移酶(UGT)1A3和UGT1A8的选择性抑制剂的鉴定及其在人肝和肠微粒体中的UGT反应表型研究中的应用
Ting Wang,Alyssa P Anderson,Andrew S Yu et al.
Ting Wang et al.
Uridine 5'-diphospho-glucuronosyltransferase (UGT) reaction phenotyping studies have posed significant challenges due to the limited availability of isoform-selective inhibitors. This recognized gap in reagent availability impedes the accur...
Coproporphyrin I as an in vitro fluorescent probe to measure OATP1B1 transport activity [0.03%]
以coproporphyrin I作为测量OATP1B1转运活性的体外荧光探针
Elizabeth R Hayden,Vivian Xu,Lisa Krotz et al.
Elizabeth R Hayden et al.
The organic anion transporting polypeptide 1B1 (OATP1B1) is a major pharmacologically relevant hepatic uptake transporter that mediates the clearance of many drugs. The OATP1B1 substrate coproporphyrin I (CPI) has been continually shown to ...
Characterization of intestinal transporters in human ileal spheroid-derived differentiated cells for the prediction of intestinal drug absorption [0.03%]
人回肠球状体分化细胞中肠道转运体的特征化以预测药物的肠道吸收性质
Kazuyoshi Michiba,Mana Namai,Yoshiki Hashimoto et al.
Kazuyoshi Michiba et al.
This study aimed to characterize the functional properties of human spheroid-derived differentiated cells for absorption, distribution, metabolism, and excretion studies. Three-dimensional human intestinal spheroids were successfully establ...
Substrate-specific inhibition of organic cation transporter 1 revealed using a multisubstrate drug cocktail [0.03%]
基于多种底物药物联合使用揭示有机阳离子转运体1的底物特异性抑制作用
Vincent Rönnpagel,Felix Morof,Sarah Römer et al.
Vincent Rönnpagel et al.
Transporters of the SLC22 family, such as organic cation transporter 1 (OCT1), possess very broad substrate specificity. It is unclear to what extent the inhibitory potencies of OCT1 depend on the substrate used. Here, we describe a multisu...
Chronic liver injury decreases levels of cerebral carnitine and acetylcarnitine in rats partly due to the downregulation of organic cation transporters OCT1/2 and OCTN2 at the blood-brain barrier [0.03%]
慢性肝损伤通过下调血脑屏障处的有机阳离子转运蛋白OCT1/2和OCTN2部分降低大鼠大脑 carnitine 和 acetylcarnitine 水平
Hao Zhi,Zhongyan Wang,Xinyue Zhu et al.
Hao Zhi et al.
Liver failure often causes hepatic encephalopathy, partly due to dysregulation in cerebral energy metabolism. Carnitine and acetylcarnitine play essential roles in energy metabolism by transporting fatty acids from the cytosol into mitochon...