Tolvaptan induces cholestasis in mice through altered expression and function of transporters and en

来源 :2015年第一届药代动力学朝阳论坛 | 被引量 : 0次 | 上传用户:iamup
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
  Drug-induced liver injury (DILI), responsible for many post-marketing withdrawal drugs, has become a serious issue in the practice of clinical medicine.Cholestasis is one of the predominant clinical manifestations of DILI in humans and plays an important role during the pathologic process.In many cholestasis cases, the main symptom is the disorder of bile acids (BAs) pool.In liver, specific BA transporters, such as sodium taurocholate co-transporting polypeptide (NTCP or SLC10A1) and bile salt export pump (BSEP or ABCB11), are indispensable in maintaining the BA homeostasis.Tolvaptan (TVP), a vasopressin Ⅱ receptor antagonist, was clinically used in the treatment of hypervolemic and euvolemic hyponatremia.Recently, TVP has been reported to show the potential risk of DILI.
其他文献
Tolcapone and entacapone, two potent catechol-O-methyltransferase COMT inhibitors, were commonly used as therapeutic drugs for treatment of Parkinsons disease.Tolcapone and entacapone share a common c
会议
Licochalcone A (LCA), a major bioactive compound isolated from the roots of Glycyrrhiza glabra, displays multiple bioactivities, such as anti-parasitic, anti-inflammatory and anti-cancer.The aim of th
会议
Carboxylesterases (CEs) catalyze hydrolytic and transesterification reactions with a vast number of endogenous and exogenous substrates including fatty acid esters, environmental toxins and ester-cont
会议
Licochalcone A (LCA) is a major bioactive compound isolated from traditional Chinese medicine liquorice which possesses multiple pharmacological effects including anti-inflammation, antiparasite, anti
会议
Nitidine chloride (NC), a benzophenanthridine alkaloid, h as many biological properties, such as anti-inflammatory and anti-cancer.However, its cytotoxicity was also reported.Our previous study demons
会议
Catechol-O-methyltransferase (COMT), one of the phase Ⅱ metabolizing enzymes, plays important roles in the metabolsim of endogenous and xenobiotic catechols.COMT is a metal ions-dependent intracellula
会议
Clopidogrel is a prodrug which requires the metabolic activation by cytochrome P450 to generate its active metabolite.The active metabolite of clopidogrel can decrease the platelet activation and aggr
会议
A sensitive, rapid and selective ultra liquid chromatography-tandem mass spectrometry (UPLC-MS-MS) method was developed and validated for the determination of baicalin in rat plasma.The oral administr
会议
Pyrrolizidine alkaloids (PAs) are a kind of hepatotoxic alkaloids, which widely exist in plants.Cytochrome P450 (CYP) 3A mediates metabolic activation of PAs, and the electrophilic products can cause
会议
Current antidepressant paroxetine therapies have an unsatisfactorily high failure rate with up to 60% of depressed patients suffering from treatment-resistant depression (TRD).The aim of this study wa
会议