Characterization of organic anion transporting polypeptide (OATP)1B1 and OATP1B3 humanized rat as a translational model to study the pharmacokinetics of OATP1B substrate drugs [0.03%]
有机阴离子转运多肽（OATP）1B1和OATP1B3人源化大鼠作为研究OATP1B底物药物药代动力学的转化模型的特征分析
Yang Li,Jocelyn Yabut,Zuo Zhang et al.
Yang Li et al.
Organic anion transporting polypeptide (OATP)1B1 and OATP1B3 (OATP1B) are clinically important transporters that mediate active hepatic uptake for a broad range of drugs and endogenous compounds and play a pivotal role in hepatic dispositio...
Impact of the transcription factor nuclear factor 1 B T>C polymorphism on clozapine metabolism in vivo and expression of intestinal transporters in vitro [0.03%]
核转录因子1B多态性对氯氮平代谢及肠道转运体表达的影响
Maria Solbakk,Robert Løvsletten Smith,Birgit M Wollmann et al.
Maria Solbakk et al.
Clozapine's (CLZ) pharmacokinetics involves multiple enzymes and transporters, which may be influenced by genetic variability. A variant in the nuclear factor I B (NFIB) gene (rs28379954 T>C) has been associated with reduced CLZ serum conce...
Identification of human hepatic UDP-glucuronosyltransferases involved in the glucuronidation of temazepam [0.03%]
人肝UDP-葡萄糖醛酸转移酶介导的替马扎匹尔葡萄糖醛酸化的鉴定研究论文
Keti Bardhi,Shelby Coates,Mengqi Zhao et al.
Keti Bardhi et al.
Temazepam is a commonly used 1,4-benzodiazepine that exists as a racemic mixture of R and S enantiomers that are metabolized primarily by glucuronidation via the UDP-glucuronosyltransferases (UGT) enzymes. The goal of the present study was ...
Absorption, distribution, metabolism, and excretion of an antiviral drug-Fc conjugate CD388 following subcutaneous administration of 14C-CD388 in the rat [0.03%]
放射性碳-14标记的抗病毒药物-Fc融合蛋白CD388皮下注射后在大鼠体内的吸收、分布、代谢及排泄研究
Aline Laenen,Shawn Flanagan,Grayson Hough et al.
Aline Laenen et al.
CD388 is a novel drug-Fc conjugate designed to function as a long-acting antiviral drug by inhibiting proliferation of the influenza virus. This action results from a dimeric form of zanamivir, a neuraminidase inhibitor, conjugated to an Fc...
OATP1B1/1B3 deficiency exacerbates hyperbilirubinemia in erythropoietic protoporphyria [0.03%]
血红素合成酶缺陷症患者中OATP1B1/1B3缺乏加重高胆红素血症
Ruizhi Gu,Fu-Ying Qin,Luxuan Wang et al.
Ruizhi Gu et al.
Erythropoietic protoporphyria (EPP) is caused by loss-of-function mutations in ferrochelatase (FECH), leading to the accumulation of its substrate, protoporphyrin IX (PPIX). PPIX is primarily produced in the bone marrow and transported to t...
Novel role of serum albumin imidase activity in the formation of BI 761036 (M232), a major metabolite of iclepertin [0.03%]
人血清白蛋白对艾曲培定主要代谢产物BI 761036(M232)形成的作用研究
Klairynne G Raymond,Mitchell E Taub,Stefan Wölke et al.
Klairynne G Raymond et al.
Iclepertin was a promising drug candidate being developed for the treatment of cognitive impairment associated with schizophrenia. Interestingly, the predominant major metabolite in vivo in humans, BI 761036 (M232), was not observed after i...
Evaluation of dose linearity in the systemic availability and pharmacokinetics of topically administered diclofenac: A 14C-microdosing study in healthy volunteers [0.03%]
评价局部给药美洛昔康系统暴露量和药代动力学的剂量线性：健康志愿者中的碳14微剂量研究
Severin Mairinger,Mihye Kwon,Martin Bauer et al.
Severin Mairinger et al.
An important safety consideration for topically administered drugs is the extent of systemic exposure they achieve. The aim of this study was to evaluate whether a topically administered microdose of the model drug diclofenac can predict th...
A combination of dietary cholesterol and cholic acid induces hepatic expression of proinflammatory genes accompanied by changes in sterol metabolism and redox status [0.03%]
饮食胆固醇和胆酸的结合诱导肝炎性基因表达并伴有甾醇代谢和氧化还原状态的变化
Wakana Iwasaki,Hinata Soma,Hiromichi Yamazaki et al.
Wakana Iwasaki et al.
Oxidized sterols and redox status play an important role in the enhancement of lipid accumulation and exacerbation of symptoms in the liver. In this study, we examined whether the combination of dietary supplementation with cholesterol (Cho...
Taurodeoxycholic acid impairs the function and expression of organic anion transporter 2 through farnesoid X receptor activation during acute kidney injury to chronic kidney injury transition [0.03%]
鹅脱氧胆酸通过法尼醇X受体激活损伤有机阴离子转运多肽2功能及表达介导急性肾损伤向慢性肾损伤转变
Yingying Dong,Luyao Wu,Xiaoying Xu et al.
Yingying Dong et al.
Acute kidney injury (AKI) is a worldwide health issue with risk of progressing to chronic kidney disease (CKD). The kidney harbors various transporters that may be involved in certain disease processes, in addition to mediating drug transpo...
Characterization of the specific proteins to which HH-A, a drug that alleviates ischemic brain injury, binds in rat plasma [0.03%]
HH-A药物与大鼠血浆中特异性结合蛋白的表征研究HH-A是一种能够缓解脑缺血损伤的药物
Jie Zhao,Yuandong Zheng,Peng Lei et al.
Jie Zhao et al.
Stroke, a destructive and burdensome disease, continues to affect an increasing number of families. HH-A, also known as (S)-6-((3',5-diallyl-2,4'-dihydroxy-[1,1'-biphenyl]-3-yl)amino)-6-oxohexane-1,5-diaminium chloride, has attracted attent...