ArticlePharmaceutical research2002
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
Article in Pharmaceutical research, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
18 citing papers in PubMed, 107 citations in OpenAlex.
- Cytochrome P450 mRNA expression in peripheral blood lymphocytes as a predictor of enzyme induction.European journal of clinical pharmacology · 2005Trial
- Use of In Vivo Imaging and Physiologically-Based Kinetic Modelling to Predict Hepatic Transporter Mediated Drug-Drug Interactions in Rats.Pharmaceutics · 2023Article
- Physiological Characterization of the Transporter-Mediated Uptake of the Reversible Male Contraceptive H2-Gamendazole Across the Blood-Testis Barrier.The Journal of pharmacology and experimental therapeutics · 2022Article
- Impact of rifampicin-inhibitable transport on the liver distribution and tissue kinetics of erlotinib assessed with PET imaging in rats.EJNMMI research · 2018Article
- Role of the OATP Transporter Family and a Benzbromarone-SensitiveEfflux Transporter in the Hepatocellular Disposition of Vincristine.Pharmaceutical research · 2017Article
- Oatp1 enhances bioluminescence by acting as a plasma membrane transporter for D-luciferin.Molecular imaging and biology · 2014Article
- P-glycoprotein- and organic anion-transporting polypeptide-mediated transport of periplocin may lead to drug-herb/drug-drug interactions.Drug design, development and therapy · 2014Article
- Genetics or environment in drug transport: the case of organic anion transporting polypeptides and adverse drug reactions.Expert opinion on drug metabolism & toxicology · 2012Review
- Ibuprofen is a non-competitive inhibitor of the peptide transporter hPEPT1 (SLC15A1): possible interactions between hPEPT1 substrates and ibuprofen.British journal of pharmacology · 2010Article
- Interaction between topically and systemically coadministered P-glycoprotein substrates/inhibitors: effect on vitreal kinetics.Drug metabolism and disposition: the biological fate of chemicals · 2010Article
- Transactivation of genes encoding for phase II enzymes and phase III transporters by phytochemical antioxidants.Molecules (Basel, Switzerland) · 2010Review
- Hepatic disposition of ximelagatran and its metabolites in pig; prediction of the impact of membrane transporters through a simple disposition model.Pharmaceutical research · 2010Article
- Concentration-dependent effect of naringin on intestinal absorption of beta(1)-adrenoceptor antagonist talinolol mediated by p-glycoprotein and organic anion transporting polypeptide (Oatp).Pharmaceutical research · 2009Article
- Competitive inhibition of organic anion transporting polypeptide 1c1-mediated thyroxine transport by the fenamate class of nonsteroidal antiinflammatory drugs.Endocrinology · 2009Article
- Effect of albumin on the biliary clearance of compounds in sandwich-cultured rat hepatocytes.Drug metabolism and disposition: the biological fate of chemicals · 2008Article
- Pharmacokinetics and response to pravastatin in paediatric patients with familial hypercholesterolaemia and in paediatric cardiac transplant recipients in relation to polymorphisms of the SLCO1B1 and ABCB1 genes.British journal of clinical pharmacology · 2006Article
- Brain uptake of nonsteroidal anti-inflammatory drugs: ibuprofen, flurbiprofen, and indomethacin.Pharmaceutical research · 2006Article
- The drug transporter-metabolism alliance: uncovering and defining the interplay.Molecular pharmaceuticsReview
Corrections and comments
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Authors and funding
8 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe purpose of the present study is to examine the selectivity of various inhibitors towards the rat organic anion transporting polypeptides 1 (Oatp1: gene symbol Slc21a1) and 2 (Oatp2: Slc21a5).
methodsThe inhibitory effects of 20 compounds on the Oatpl-mediated transport of estradiol 17beta-D-glucuronide and on the Oatp2-mediated transport of digoxin were examined in cDNA-transfected LLC-PK1cells.
resultsAmong the compounds examined in this study, nonsteroidal anti-inflammatory drugs, deoxycorticosterone. and quinidine preferentially inhibited Oatpl. whereas digoxin, quinine, and rifampicin preferentially inhibited Oatp2 at low concentrations. On the other hand, propionic acid, re-ketoglutarate and p-aminohippurate showed no inhibitory effects on either transporter up to a concentration of 1,000 microM. The Ki values of ibuprofen and quinidine were estimated to be 19 and 13 times lower for Oatpl compared with Oatp2, whereas the values for rifampicin, quinine, and digoxin were 13, 20, and 100< times lower for Oatp2 compared with Oatpl.
conclusionsAt low concentrations, some of the tested inhibitors exert selective inhibition of either Oatpl- or Oatp2-mediated substrate transport. These selective inhibitors may be used at appropriate concentrations to estimate the maximum contribution of Oatp1 or Oatp2 to the total substrate uptake into rat hepatocytes.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.