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...
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...
ClinicalPharmacologyTherapeutics75,13-33(January2004)P-gptissuedistribution.EffluxactivityassociatedwithP-gpwouldreduceintestinaldrugabsorptionwhileenhancingdrugeliminationthroughtheliverandkidney.Atbarriersitessuchastheblood-brainbarrier,testes,orplacenta,P-gpwouldlimittissueexposuretopotentiallytoxicP-gpsubstrate...
10. Didziapetris, R.; Japertas, P.; Avdeef, A.; Petrauskas, A. Classification Analysis of P-Glycoprotein Substrate Specificity. J. Drug Target. 2003, 11, 391–406. 11. Zhang, H.; Xu, H.; Ashby, C. R. Jr.; Assaraf, Y. G.; Chen, Z.-S.; Liu, H.M. Chemical molecular-ba...
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...
In addition, no neurotoxic clinical signs were observed in either mouse type administered domperidone, a P-gp substrate with no reported neurotoxicity in ABCB1-1螖 Collies. Overall, neurotoxic signs displayed by model mice closely paralleled those observed in ivermectin-sensitive Collies. This model ...
P-gptissuedistribution.EffluxactivityassociatedwithP-gpwouldreduceintestinaldrugabsorptionwhileenhancingdrugeliminationthroughtheliverandkidney.Atbarriersitessuchastheblood-brainbarrier,testes,orplacenta,P-gpwouldlimittissueexposuretopotentiallytoxicP-gpsubstratecompounds.PolymorphismsinHumanMDR1(P-glycoprotein):Recent...
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...
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: ...
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 ...