Resolution of P-glycoprotein and non-P-glycoprotein effects on drug permeability using intestinal tissues from mdr1a (−/−) mice
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چکیده
منابع مشابه
Altered pharmacokinetics of vinblastine in Mdr1a P-glycoprotein-deficient Mice.
BACKGROUND P-glycoprotein (Pgp) is a membrane protein that acts as an extrusion pump for many cytotoxic drugs. Pgp is expressed in normal tissues, and its (over)expression in tumor cells contributes to their drug resistance. Human Pgp is encoded by the MDR1 gene, In mice, two Pgps (encoded by the mdr1a and mdr1b genes) appear to perform the same function as the single human protein. The simulta...
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The experiments described herein compared the extent of in vivo P-glycoprotein (P-gp)-mediated brain efflux between rats and mice for a set of known central nervous system compounds. With use of newly introduced genetically modified mdr1a-deficient rats and their gene-competent counterparts, the brain to plasma distribution was assessed and compared with the distribution pattern in mdr1a-defici...
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INTRODUCTION There are many factors that can affect the absorption process of orally administered drugs. Intestinal transporters play an important role in drug absorption. These transporters are divided into two major classes: the solute carriers and the ATP-binding cassette (ABC) transporters. P-glycoprotein (P-gp), belonging to the ABC transporter superfamily, flushes out the substrate drugs ...
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Drug-transporting P-glycoproteins are abundantly present in the liver and the intestinal wall. We have now investigated their role in the biliary and intestinal secretion of the anticancer drugs doxorubicin (unlabeled: 5 mg/kg) and vinblastine ((3)H-labeled: 1 mg/kg) i.v. administered to wild-type and mdr1a P-glycoprotein knockout [mdr1a(-/-)] mice. At 90 min after drug administration, levels o...
متن کاملThe role of P-glycoprotein in intestinal tumorigenesis: disruption of mdr1a suppresses polyp formation in Apc(Min/+) mice.
P-glycoprotein (P-gp) mediates the active transport of various substrates including xenobiotics, and it thus has a protective function in various cell types and tissues/organs including the intestinal epithelium. However, whether or not P-gp plays a positive role in the intestinal tumorigenesis is unclear. We have introduced disrupted alleles of the murine P-gp gene, mdr1a, into Apc(Min/+) mice...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2002
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0704668