Uptake and Permeability Studies to Delineate the Role of Efflux Transporters

2016 ◽  
pp. 69-74
Author(s):  
Ramya Krishna Vadlapatla ◽  
Dhananjay Pal ◽  
Ashim K. Mitra
Keyword(s):  
Efflux Transporters ◽  
Permeability Studies

Effect of Neuroinflammation on ABC Transporters: Possible Contribution to Refractory Epilepsy

2018 ◽  
Vol 17 (10) ◽  
pp. 728-735 ◽  
Author(s):  
Xiaolin Deng ◽  
Yangmei Xie ◽  
Yinghui Chen
Keyword(s):  
Antiepileptic Drugs ◽  
Abc Transporters ◽  
Refractory Epilepsy ◽  
Vascular Endothelial Cells ◽  
Efflux Transporters ◽  
Vascular Endothelial ◽  
Intracellular Signalling Pathways ◽  
The Brain ◽  
Transporter Expression

Background & Objective: Epilepsy is a common and serious chronic neurological disorder that is mainly treated with antiepileptic drugs. Although current antiepileptic drugs used in clinical practice have advanced to the third generation, approximately one-third of patients are refractory to these treatments. More efficacious treatments for refractory epilepsy are therefore needed. A better understanding of the mechanism underlying refractory epilepsy is likely to facilitate the development of a more effective therapy. The abnormal expression and/or dysfunction of efflux transporters, particularly ABC transporters, might contribute to certain cases of refractory epilepsy. Inflammation in the brain has recently been shown to regulate the expression and/or function of ABC transporters in the cerebral vascular endothelial cells and glia of the blood-brain barrier by activating intracellular signalling pathways. Conclusion: Therefore, in this review, we will briefly summarize recent research advances regarding the possible role of neuroinflammation in regulating ABC transporter expression in epilepsy.

scholarly journals Novel role of Acinetobacter baumannii RND efflux transporters in mediating decreased susceptibility to biocides

2009 ◽  
Vol 65 (2) ◽  
pp. 228-232 ◽  
Author(s):  
G. Rajamohan ◽  
V. B. Srinivasan ◽  
W. A. Gebreyes
Keyword(s):  
Acinetobacter Baumannii ◽  
Efflux Transporters

Evidence of stereoselective and segmental-dependant transport of chiral antidiabetic drug nateglinide along the rat small intestine: possible role of efflux transporters

2012 ◽  
Vol 22 (5) ◽  
pp. 2403-2410 ◽  
Author(s):  
Srinivas Maddi ◽  
Shravan Kumar Yamsani ◽  
Adukondalu Devandla ◽  
Gerhard Scriba ◽  
Madhusudan Rao Yamsani
Keyword(s):  
Small Intestine ◽  
Efflux Transporters ◽  
Rat Small Intestine ◽  
Antidiabetic Drug

Role of Hepatic Efflux Transporters in Regulating Systemic and Hepatocyte Exposure to Xenobiotics

2014 ◽  
Vol 54 (1) ◽  
pp. 509-535 ◽  
Author(s):  
Nathan D. Pfeifer ◽  
Rhiannon N. Hardwick ◽  
Kim L.R. Brouwer
Keyword(s):  
Efflux Transporters

The function of multidrug resistance-associated protein 3 in the transport of bile acids under normal physiological and lithocholic acid-induced cholestasis conditions

2021 ◽  
Vol 22 ◽  
Author(s):  
Wenyu Wang ◽  
Sijing Zeng ◽  
Ming Hu ◽  
Zhongqiu Liu ◽  
Lingzhi Gong
Keyword(s):  
Multidrug Resistance ◽  
Bile Acid ◽  
Bile Acids ◽  
Physiological Condition ◽  
Lithocholic Acid ◽  
Efflux Transporters ◽  
Valuable Insight ◽  
Wild Type ◽  
Normal Physiological Condition

Background: The role of multidrug resistance-associated protein 3 (Mrp3) in the transport of bile acid (BA) in drug-induced cholestasis have not been well studied. Objective: In this study, wild type and Mrp3 knockout (Mrp3-/- ) mice under normal physiological and lithocholic acid (LCA)-induced cholestatic conditions were employed to investigate the role of Mrp3 in BA transport. Method: The levels of BA in serum, liver, gallbladder, intestine, kidney, feces and urine were quantified in both wild type and Mrp3-/- mice via ultra-high performance liquid chromatography triple quadrupole mass spectrometry (UHPLC-MS/MS). Quantitative real time PCR (RT-PCR) analysis was used to measure the expression of genes related to the transport and synthesis of BA. Results: The results showed that the liver did not suffer more serious damage as a result of cholestasis when Mrp3 was depleted. The level of some individual bile acids changed apparently in the compartments of enterohepatic circulation (EHC) between the two control and model groups, respectively, but the level of serum total bile acid was only slightly reduced for Mrp3-/- groups. In addition, the level of BA-related efflux transporters and synthases increased significantly when Mrp3 was knocked out under normal physiological condition, but negligible alteration of them appeared under cholestatic condition. Conclusion: Our results indicated that Mrp3 could be responsible for the transport of some specific bile acids, and part of the Mrp3 role could be compensated for by other transporters. Moreover, Mrp3 deficiency has a direct effect on the expression of BA-related synthases and efflux transporters under normal physiological condition, but this effect could be less prominent under cholestatic condition. This study could provide much valuable insight into the physiological function of Mrp3 in the transport of bile acids.

Abstract 6322: The role of multidrug efflux transporters and CYP3A in the pharmacokinetics and tissue distribution of abemaciclib and its active metabolites

2020 ◽  
Author(s):  
Alejandra Martinez Chavez ◽  
Matthijs M. Tibben ◽  
Maria C. Lebre ◽  
Hilde Rosing ◽  
Jos H. Beijnen ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Efflux Transporters ◽  
Multidrug Efflux ◽  
Active Metabolites
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