ArticleBritish journal of pharmacology2000
Active transport of the angiotensin-II antagonist losartan and its main metabolite EXP 3174 across MDCK-MDR1 and caco-2 cell monolayers.
Article in British journal of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 105 citations in OpenAlex.
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- Prediction of CYP-mediated silybin A-losartan pharmacokinetic interactions using physiological based pharmacokinetic modeling.Journal of pharmacokinetics and pharmacodynamics · 2022Article
- Predictive Value of Microdose Pharmacokinetics.Clinical pharmacokinetics · 2019Review
- Cell Migration Related to MDR-Another Impediment to Effective Chemotherapy?Molecules (Basel, Switzerland) · 2018Review
- Neuroprotective effects of AT1 receptor antagonists after experimental ischemic stroke: what is important?Naunyn-Schmiedeberg's archives of pharmacology · 2017Article
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- Sucralose, a synthetic organochlorine sweetener: overview of biological issues.Journal of toxicology and environmental health. Part B, Critical reviews · 2013Review
- Screening candidate anticancer drugs for brain tumor chemotherapy: pharmacokinetic-driven approach for a series of (E)-N-(substituted aryl)-3-(substituted phenyl)propenamide analogues.Investigational new drugs · 2012Article
- In vitro interactions between aged garlic extract and drugs used for the treatment of cardiovascular and diabetic patients.European journal of nutrition · 2010Article
- Influence of intermittent hypoxia on myocardial and hepatic P-glycoprotein expression in a rodent model.Pharmacotherapy · 2009Article
- Expression of adenosine triphosphate-binding cassette (ABC) drug transporters in peripheral blood cells: relevance for physiology and pharmacotherapy.Clinical pharmacokinetics · 2007Review
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. We studied the functional interaction between transport and metabolism by comparing the transport of losartan and its active metabolite EXP 3174 (EXP) across cell monolayers. 2. Epithelial layers of Caco-2 cells as well as MDR1, MRP-1 and MRP-2 overexpressing cells, in comparison to the respective wildtypes, were used to characterize the transcellular transport of losartan and EXP. 3. Losartan transport in MDCK-MDR1 and Caco-2 cells was saturable and energy-dependent with a significantly greater basolateral-to-apical (B/A) than apical-to-basolateral (A/B) flux (ratio=31+/-1 in MDCK-MDR1 and ratio 4+/-1 in Caco-2 cells). The B/A flux of losartan was inhibited by cyclosporine and vinblastine, inhibitors of P-glycoprotein and MRP. In contrast, no active losartan transport was observed in MRP-1 or MRP-2 overexpressing cells. 4. The metabolite was only transported in Caco-2 cells with a B/A-to-A/B ratio of 5+/-1, while lacking active transport in the MDR1, MRP-1 or MRP-2 overexpressing cells. The B/A flux of EXP was significantly inhibited by cyclosporine and vinblastine. 5. In conclusion, losartan is transported by P-glycoprotein and other intestinal transporters, that do not include MRP-1 and MRP-2. In contrast, the carboxylic acid metabolite is not a P-glycoprotein substrate, but displays considerably higher affinity for other transporters than losartan, that again most probably do not include MRP-1 and MRP-2.
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