Comparative transcriptomic profiling of drug-metabolizing enzymes and drug transporters in rabbit ocular subtissues, liver, and duodenum [0.03%]
兔眼亚组织、肝脏和十二指肠药物代谢酶和转运体的转录组分析
Mengyue Li,Brian J Sanderson,Jennifer Leigh Hackett et al.
Mengyue Li et al.
The increasing prevalence of diabetes and the aging population have led to a growing market for ophthalmic pharmaceutical drugs. However, the development of ophthalmic drugs is hampered by the poor understanding of drug-metabolizing enzymes...
Comparative metabolism of an N-acetylgalactosamine-conjugated small interfering RNA, inclisiran, among various in vitro systems and correlations with in vivo metabolism in rats [0.03%]
一种N-乙酰半乳糖胺连接的的小干扰RNA-inclisiran在各种体外系统中的代谢比较及其与大鼠体内代谢的相关性
Hong Zhang,Gengyao Qin,Liqi Shi et al.
Hong Zhang et al.
N-acetylgalactosamine-conjugated small interfering RNAs (siRNAs) have emerged as a promising new class of therapeutics, demonstrating potential across various disease areas. Metabolic stability is a critical factor in the development of siR...
The slow elimination of 1,4-bis [2-(3,5-dichloropyridyloxy)] benzene in mice leads to prolonged constitutive androstane receptor activation and hepatomegaly [0.03%]
1,4-双[2-(3,5-二氯吡啶氧基)]苯在小鼠中缓慢消除导致长时间的.constitutive和rostane受体激活和肝大
Yue Gao,Chenghui Cai,Wanyu Zheng et al.
Yue Gao et al.
Constitutive androstane receptor (CAR, NR1I3), a nuclear receptor superfamily member, plays a pivotal role in liver size regulation. Murine CAR agonist 1,4-bis [2-(3,5-dichloropyridyloxy)] benzene (TCPOBOP) was reported to induce hepatomega...
Effects of antihypertensive drugs on the metabolism of mobocertinib in rats both in vitro and in vivo [0.03%]
抗高血压药物对莫博赛替尼大鼠体内和体外代谢的影响
Dafa Yi,Jiazong Ye,Zebei Lu et al.
Dafa Yi et al.
This study investigates the potential drug-drug interactions between commonly prescribed antihypertensive drugs and mobocertinib in clinical practice to provide the scientific basis for the appropriate therapeutic application of drugs. The ...
Predicting in vivo cannabinoid-drug interactions mediated via inhibition of UDP-glucuronosyltransferases using in vitro studies and physiologically based pharmacokinetic modeling and simulations [0.03%]
基于体外研究和生理药代动力学模型与模拟预测由UDP葡萄糖醛酸转移酶介导的大麻素-药物体内相互作用
Sumit Bansal,Mary F Paine,Jashvant D Unadkat
Sumit Bansal
We previously reported the inhibitory potential of the most extensively studied cannabinoids, cannabidiol (CBD) and Δ9-tetrahydrocannabinol (THC), along with their respective circulating metabolites, against a panel of cytochrome P450 (CYP...
Bridging in vitro and clinical data: Experimental insights into the IC50 variability of dolutegravir as an organic cation transporter 2 inhibitor [0.03%]
从体外到临床数据的桥梁：作为有机阳离子转运蛋白2抑制剂时多替拉韦IC50变异性的实验见解
Tomoki Koishikawa,Yukana Tomoda,Toshiaki Tsuchitani et al.
Tomoki Koishikawa et al.
Dolutegravir is a clinically confirmed inhibitor of organic cation transporter 2 (OCT2)/SLC22A2; however, its in vitro IC50 varies widely across studies. Using OCT2-expressing human embryonic kidney 293 cells, we investigated experimental c...
Species difference in the excretion routes of Ciprofol (HSK3486) in rats and humans: Contribution of hepatic transporters and renal UDP-glucuronosyltransferase enzymes [0.03%]
动物与人匹鲁卡品（HSK3486）的排泄途径差异：肝转运体和肾UDP-葡萄糖醛酸转移酶的作用
Yufan Zhou,Zitao Guo,Jian Meng et al.
Yufan Zhou et al.
The primary metabolic pathways of the anesthetic Ciprofol in both humans and rats are glucuronidation (M4) and 4-hydroxylation, followed by glucuronidation (M5-1). However, there are significant interspecies differences in their excretion r...
Investigation of differentiation conditions for canine duodenum, upper jejunum, and ileum crypt-derived cells for drug transport and metabolism [0.03%]
犬十二指肠、上段空肠和回肠杯状细胞药物转运及代谢的分化条件研究
Hiroki Takezaki,Yoshiki Hashimoto,Ikuko Kaisaki et al.
Hiroki Takezaki et al.
Three-dimensional spheroid cultures of crypts from the duodenum, upper jejunum, and ileum of beagle dog were established to investigate species differences in drug transport and metabolism. Four differentiation conditions were tested using ...
Application of preclinical absorption, distribution, metabolism, elimination in vitro techniques for the characterization and compound library optimization of novel antibiotic gallium salophen [0.03%]
体外吸收、分布、代谢和排泄药代动力学技术在新型抗生素镓- salophen化合物库特征研究及优化中的应用
Samuel A Krug,Aziza Frank,Lucia Hwang et al.
Samuel A Krug et al.
Multidrug-resistant pathogens are an emerging threat to public health. Metal-based drugs have shown antimicrobial properties. As a result, metallotherapeutics have an untapped potential to combat antibiotic-resistant infections. Characteriz...
ABCC2 as a novel covariate influencing oxcarbazepine pharmacokinetics in pediatric epilepsy: Insights from population modeling [0.03%]
ABCC2作为影响儿童癫痫患者奥卡西平药代动力学的新协变量：人群建模的启示
Xianhuan Shen,Jiahao Zhu,Yaodong He et al.
Xianhuan Shen et al.
This study set out to establish a population pharmacokinetic (PPK) model of oxcarbazepine (OXC) in pediatric patients with epilepsy, with the goal of optimizing individualized dosage strategies. We collected steady-state trough plasma conce...