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-GPSUbSTrATeDeTerMINATION-cerep46fr 系统标签: substratedeterminationeffluxverapamilpermeabilitysubstrates APPLICATIONNOTE-July2013 TheP-glycoprotein(P-gp),isaneffluxpumplocatedintheintestineandblood-brainbarrieramongothertissues.Compoundsthataresubstrates fortheP-gpmaybesecretedbackintothelumenoftheintestine,resultingin...
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...
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...
gp inducers that reduce total bioavailability with a minor impact on renal clearance. Rifampin is the most potent P-gp inducer, resulting in an average reduction in substrate exposure ranging between 20 and 67%. For other inducer...
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). ...
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 ...
ClinicalPharmacologyTherapeutics75,13-33(January2004)P-gptissuedistribution.EffluxactivityassociatedwithP-gpwouldreduceintestinaldrugabsorptionwhileenhancingdrugeliminationthroughtheliverandkidney.Atbarriersitessuchastheblood-brainbarrier,testes,orplacenta,P-gpwouldlimittissueexposuretopotentiallytoxicP-gpsubstrate...
Experience in oncology indicates that repeated exposure to P-gp substrate cytotoxic drugs leads to the selection of drug-resistant tumor cells that overexpress P-gp. Since immunosuppressive agents such as cyclosporine, tacrolimus, sirolimus and corticosteroids are substrates for P-gp and since T-cells...