Substrate (in vitro transport assay)– -药物通过表达P-gp的细胞单层极化运输或在MDR细胞中的减少药物积累减少 Substrate (in vivo BBB models)- 在P-gp基因缺乏(mdr1a/b(-/-))的小鼠中药物向大脑的分布增加 P-gp mediated resistance- P-gp过表达(MDR)细胞中表现...
P-GP SUbSTrATe DeTerMINATION - cerep.fr APPLICATION NOTE - July 2013The P-glycoprotein (P-gp), is an efflux pump located in the intestine and blood-brain barrier among other tissues. Compounds that are substrates for the P-gp may be secreted back into the lumen of the intestine, resulting ...
However, when substrate drugs of both CYPs and P-gp are involved in DDIs, it remains that the mechanisms of DDIs will be quite ambiguous in assessing how much the CYPs and/or drug transporters partially contribute to DDIs.Akamine, Yumiko...
Tetracyclic compound27is a chemotherapy plagued with cytotoxic drug resistance as a consequence of being a P-gp substrate. A Mannich reaction of27offered the corresponding 3-aminomethyl derivatives28and29, respectively. The maneuver co...
发光底物B液Substrate Reagent B1瓶 5mL4℃(避光) 封板覆膜Plate Sealer5 张 产品说明书Manual1 份 质检报告Certificate of Analysis1 份 特别说明: #: 一周内使用可存于4℃,需长时间存放或多次使用建议存于-20℃. 人P糖蛋白/渗透性糖蛋白(P-GP)化学发光**分析试剂盒操作步骤: ...
P-gp belongs to a class of ATP-binding cassette transporters. Roughly, a drug is a P-gp efflux substrate if more of the drug is transported out than going in. Basically, P-gp substrates are defined as compounds transported by the P-gp. If the P-gp efflux ratio [ER= Papp(B→A)/Pa...
dependent permeability of verapamil, quinidine, and vinblastine in MDR1-MDCKII, P-gp-highly induced Caco-2, P-gp-induced Caco-2, normal Caco-2, and MDR1-knockdown Caco-2 cells data were analyzed using a model in which the Km value was defined for the intracellular substrate concentration....
A model to identify P-glycoprotein(P-gp) substrate was constructed with a random forest method based on open source software CDK(Chemistry Development Kit) descriptors and a training data set which contained 170 compounds(96 P-gp substrates). 应用随机森林方法、开放源代码软件-CDK(Chemistry Developme...
ClinicalPharmacologyTherapeutics75,13-33(January2004)P-gptissuedistribution.EffluxactivityassociatedwithP-gpwouldreduceintestinaldrugabsorptionwhileenhancingdrugeliminationthroughtheliverandkidney.Atbarriersitessuchastheblood-brainbarrier,testes,orplacenta,P-gpwouldlimittissueexposuretopotentiallytoxicP-gpsubstrate...
This mini-review aims at summarizing the role of P-gp in the drugs oral absorption and correlating some of the most used permeability methods to determine the drug condition as P-gp substrate. Studies about P-gp have shown that it is a dynamic protein, facilitating secretion of endogenous ...