4-Acridinecarboxamide, N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-, hydrochloride (1:1)
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Transport inhibition of digoxin using several common P-gp expressing cell lines is not necessarily reporting only on inhibitor binding to P-gp. | PloS one 20130101 |
Oral availability and brain penetration of the B-RAFV600E inhibitor vemurafenib can be enhanced by the P-GLYCOprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar. | Molecular pharmaceutics 20121105 |
Active efflux of Dasatinib from the brain limits efficacy against murine glioblastoma: broad implications for the clinical use of molecularly targeted agents. | Molecular cancer therapeutics 20121001 |
Pharmacokinetic modeling to assess factors affecting the oral bioavailability of the lactone and carboxylate forms of the lipophilic camptothecin analogue AR-67 in rats. | Pharmaceutical research 20120701 |
Exploiting transport activity of p-glycoprotein at the blood-brain barrier for the development of peripheral cannabinoid type 1 receptor antagonists. | Molecular pharmaceutics 20120507 |
Stereoselective interaction of pantoprazole with ABCG2. I. Drug accumulation in rat milk. | Drug metabolism and disposition: the biological fate of chemicals 20120501 |
Understanding the interplay of drug transporters involved in the disposition of rosuvastatin in the isolated perfused rat liver using a physiologically-based pharmacokinetic model. | Xenobiotica; the fate of foreign compounds in biological systems 20120401 |
P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib. | The Journal of pharmacology and experimental therapeutics 20120401 |
Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration. | International journal of cancer 20120101 |
A comparative small-animal PET evaluation of [11C]tariquidar, [11C]elacridar and (R)-[11C]verapamil for detection of P-glycoprotein-expressing murine breast cancer. | European journal of nuclear medicine and molecular imaging 20120101 |
ABCG2- and ABCG4-mediated efflux of amyloid-β peptide 1-40 at the mouse blood-brain barrier. | Journal of Alzheimer's disease : JAD 20120101 |
Dual approach utilizing self microemulsifying technique and novel P-gp inhibitor for effective delivery of taxanes. | Journal of microencapsulation 20120101 |
The influence of modulation of P-glycoprotein and /or cytochrome P450 3A on the pharmacokinetics and pharmacodynamics of orally administered morphine in dogs. | Journal of veterinary pharmacology and therapeutics 20111001 |
Evaluation of the P-glycoprotein- and breast cancer resistance protein-mediated brain penetration of 11C-labeled topotecan using small-animal positron emission tomography. | Nuclear medicine and biology 20110701 |
The bioflavonoid kaempferol is an Abcg2 substrate and inhibits Abcg2-mediated quercetin efflux. | Drug metabolism and disposition: the biological fate of chemicals 20110301 |
Synthesis and in vivo evaluation of ¹⁸F-fluoroethyl GF120918 and XR9576 as positron emission tomography probes for assessing the function of drug efflux transporters. | Bioorganic & medicinal chemistry 20110115 |
Intestinal absorption of HMG-CoA reductase inhibitor pitavastatin mediated by organic anion transporting polypeptide and P-glycoprotein/multidrug resistance 1. | Drug metabolism and pharmacokinetics 20110101 |
Characterisation and manipulation of docetaxel resistant prostate cancer cell lines. | Molecular cancer 20110101 |
P-glycoprotein and breast cancer resistance protein affect disposition of tandutinib, a tyrosine kinase inhibitor. | Drug metabolism letters 20101201 |
The transport of gastrodin in Caco-2 cells and uptake in Bcap37 and Bcap37/MDR1 cells. | Yao xue xue bao = Acta pharmaceutica Sinica 20101201 |
Hepatobiliary disposition of 3alpha,6alpha,7alpha,12alpha-tetrahydroxy-cholanoyl taurine: a substrate for multiple canalicular transporters. | Drug metabolism and disposition: the biological fate of chemicals 20101001 |
Examination of the ability of the nasal administration route to confer a brain exposure advantage for three chemical inhibitors of P-glycoprotein. | Journal of pharmaceutical sciences 20100701 |
Distribution of gefitinib to the brain is limited by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2)-mediated active efflux. | The Journal of pharmacology and experimental therapeutics 20100701 |
Toxicokinetics of the food-toxin IQ in human placental perfusion is not affected by ABCG2 or xenobiotic metabolism. | Placenta 20100701 |
Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET. | European journal of nuclear medicine and molecular imaging 20100501 |
Absorption barriers in the rat intestinal mucosa: 2. Application of physiologically based mathematical models to quantify mechanisms of drug permeation and metabolism. | Journal of pharmaceutical sciences 20100201 |
Functional characterization of mouse organic anion transporting peptide 1a4 in the uptake and efflux of drugs across the blood-brain barrier. | Drug metabolism and disposition: the biological fate of chemicals 20100101 |
The P-glycoprotein inhibitor GF120918 modulates Ca2+-dependent processes and lipid metabolism in Toxoplasma gondii. | PloS one 20100101 |
Hepatitis C virus NS3 protease inhibitors: large, flexible molecules of peptide origin show satisfactory permeability across Caco-2 cells. | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20091208 |
Investigation of the micellar effect of pluronic P85 on P-glycoprotein inhibition: cell accumulation and equilibrium dialysis studies. | Journal of pharmaceutical sciences 20091101 |
Comparison of bidirectional lamivudine and zidovudine transport using MDCK, MDCK-MDR1, and Caco-2 cell monolayers. | Journal of pharmaceutical sciences 20091101 |
Decreased urinary secretion of belotecan in folic acid-induced acute renal failure rats due to down-regulation of Oat1 and Bcrp. | Xenobiotica; the fate of foreign compounds in biological systems 20091001 |
Multiple efflux pumps are involved in the transepithelial transport of colchicine: combined effect of p-glycoprotein and multidrug resistance-associated protein 2 leads to decreased intestinal absorption throughout the entire small intestine. | Drug metabolism and disposition: the biological fate of chemicals 20091001 |
P-glycoprotein and breast cancer resistance protein influence brain distribution of dasatinib. | The Journal of pharmacology and experimental therapeutics 20090901 |
Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs. | Pharmaceutical research 20090801 |
Identification of the efflux transporter of the fluoroquinolone antibiotic ciprofloxacin in murine macrophages: studies with ciprofloxacin-resistant cells. | Antimicrobial agents and chemotherapy 20090601 |
Brain accumulation of dasatinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by elacridar treatment. | Clinical cancer research : an official journal of the American Association for Cancer Research 20090401 |
In vivo evaluation of P-glycoprotein and breast cancer resistance protein modulation in the brain using [(11)C]gefitinib. | Nuclear medicine and biology 20090401 |
Substrate-dependent breast cancer resistance protein (Bcrp1/Abcg2)-mediated interactions: consideration of multiple binding sites in in vitro assay design. | Drug metabolism and disposition: the biological fate of chemicals 20090301 |
The effect of P-gp (Mdr1a/1b), BCRP (Bcrp1) and P-gp/BCRP inhibitors on the in vivo absorption, distribution, metabolism and excretion of imatinib. | Investigational new drugs 20090201 |
Cross-functioning between the extraneuronal monoamine transporter and multidrug resistance protein 1 in the uptake of adrenaline and export of 5-(glutathion-S-yl)adrenaline in rat cardiomyocytes. | Chemical research in toxicology 20090101 |
Knocking down breast cancer resistance protein (Bcrp) by adenoviral vector-mediated RNA interference (RNAi) in sandwich-cultured rat hepatocytes: a novel tool to assess the contribution of Bcrp to drug biliary excretion. | Molecular pharmaceutics 20090101 |
Molecular expression and functional evidence of a drug efflux pump (BCRP) in human corneal epithelial cells. | Current eye research 20090101 |
N-(4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]-phenyl)-9,10-dihydro-5-methoxy-9-oxo-4-acridine carboxamide (GF120918) as a chemical ATP-binding cassette transporter family G member 2 (Abcg2) knockout model to study nitrofurantoin transfer into milk. | Drug metabolism and disposition: the biological fate of chemicals 20081201 |
Apparent differences in mechanisms of harmol sulfate biliary excretion in mice and rats. | Drug metabolism and disposition: the biological fate of chemicals 20081101 |
A novel human multidrug resistance gene MDR1 variant G571A (G191R) modulates cancer drug resistance and efflux transport. | The Journal of pharmacology and experimental therapeutics 20081101 |
Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice. | Journal of cancer research and clinical oncology 20080501 |
Chemosensitivity determinants of irinotecan hydrochloride in hepatocellular carcinoma cell lines. | Basic & clinical pharmacology & toxicology 20080401 |
P-glycoprotein restricts the penetration of oseltamivir across the blood-brain barrier. | Drug metabolism and disposition: the biological fate of chemicals 20080201 |
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives. | Bioorganic & medicinal chemistry 20080101 |
P-glycoprotein-mediated active efflux of the anti-HIV1 nucleoside abacavir limits cellular accumulation and brain distribution. | Drug metabolism and disposition: the biological fate of chemicals 20071101 |
Placental transfer of quetiapine in relation to P-glycoprotein activity. | Journal of psychopharmacology (Oxford, England) 20070901 |
Modulation of the brain distribution of imatinib and its metabolites in mice by valspodar, zosuquidar and elacridar. | Pharmaceutical research 20070901 |
Influence of breast cancer resistance protein (Abcg2) and p-glycoprotein (Abcb1a) on the transport of imatinib mesylate (Gleevec) across the mouse blood-brain barrier. | Journal of neurochemistry 20070901 |
Abcg2/Bcrp1 mediates the polarized transport of antiretroviral nucleosides abacavir and zidovudine. | Drug metabolism and disposition: the biological fate of chemicals 20070701 |
Influence of biophase distribution and P-glycoprotein interaction on pharmacokinetic-pharmacodynamic modelling of the effects of morphine on the EEG. | British journal of pharmacology 20070701 |
Population pharmacokinetic modelling of non-linear brain distribution of morphine: influence of active saturable influx and P-glycoprotein mediated efflux. | British journal of pharmacology 20070701 |
A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. | Clinical cancer research : an official journal of the American Association for Cancer Research 20070601 |
The emerging pharmacotherapeutic significance of the breast cancer resistance protein (ABCG2). | British journal of pharmacology 20070501 |
Inhibitors of kinesin Eg5: antiproliferative activity of monastrol analogues against human glioblastoma cells. | Cancer chemotherapy and pharmacology 20070201 |
Danofloxacin-mesylate is a substrate for ATP-dependent efflux transporters. | British journal of pharmacology 20070201 |
Proteomic analysis to dissect mitoxantrone resistance-associated proteins in a squamous lung carcinoma. | Anticancer research 20070101 |
An in vitro and in silico study on the flavonoid-mediated modulation of the transport of 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) through Caco-2 monolayers. | Toxicology and applied pharmacology 20061201 |
Role of human placental efflux transporter P-glycoprotein in the transfer of buprenorphine, levo-alpha-acetylmethadol, and paclitaxel. | American journal of perinatology 20061001 |
The complexity of intestinal absorption and exsorption of digoxin in rats. | International journal of pharmaceutics 20060928 |
Differential in vivo sensitivity to inhibition of P-glycoprotein located in lymphocytes, testes, and the blood-brain barrier. | The Journal of pharmacology and experimental therapeutics 20060601 |
Comparison of drug efflux transport kinetics in various blood-brain barrier models. | Drug metabolism and disposition: the biological fate of chemicals 20060601 |
Saturable absorptive transport of the hydrophilic organic cation ranitidine in Caco-2 cells: role of pH-dependent organic cation uptake system and P-glycoprotein. | Pharmaceutical research 20060601 |
Intestinal absorptive transport of the hydrophilic cation ranitidine: a kinetic modeling approach to elucidate the role of uptake and efflux transporters and paracellular vs. transcellular transport in Caco-2 cells. | Pharmaceutical research 20060601 |
In vitro p-glycoprotein inhibition assays for assessment of clinical drug interaction potential of new drug candidates: a recommendation for probe substrates. | Drug metabolism and disposition: the biological fate of chemicals 20060501 |
Interactions between the dopamine agonist, bromocriptine and the efflux protein, P-glycoprotein at the blood-brain barrier in the mouse. | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20060201 |
Expression and functional activity of breast cancer resistance protein (BCRP, ABCG2) transporter in the human choriocarcinoma cell line BeWo. | Clinical and experimental pharmacology & physiology 20060101 |
Role of P-glycoprotein in the hepatic metabolism of tacrolimus. | Xenobiotica; the fate of foreign compounds in biological systems 20060101 |
The steady-state Michaelis-Menten analysis of P-glycoprotein mediated transport through a confluent cell monolayer cannot predict the correct Michaelis constant Km. | Pharmaceutical research 20051001 |
A combined cell based approach to identify P-glycoprotein substrates and inhibitors in a single assay. | International journal of pharmaceutics 20050914 |
Multiple mechanisms are involved in the biliary excretion of acetaminophen sulfate in the rat: role of Mrp2 and Bcrp1. | Drug metabolism and disposition: the biological fate of chemicals 20050801 |
Functional role of P-glycoprotein in the human blood-placental barrier. | Clinical pharmacology and therapeutics 20050801 |
The impact of pharmacologic and genetic knockout of P-glycoprotein on nelfinavir levels in the brain and other tissues in mice. | Journal of pharmaceutical sciences 20050601 |
Flavonoid structure-activity studies identify 6-prenylchrysin and tectochrysin as potent and specific inhibitors of breast cancer resistance protein ABCG2. | Cancer research 20050601 |
Expression, localization, and functional characteristics of breast cancer resistance protein in Caco-2 cells. | Drug metabolism and disposition: the biological fate of chemicals 20050501 |
The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients. | Cancer research 20050401 |
P-glycoprotein and mutlidrug resistance-associated proteins limit the brain uptake of saquinavir in mice. | The Journal of pharmacology and experimental therapeutics 20050301 |
Differential sensitivities of the human ATP-binding cassette transporters ABCG2 and P-glycoprotein to cyclosporin A. | Molecular pharmacology 20050301 |
Flavonoids chrysin and benzoflavone, potent breast cancer resistance protein inhibitors, have no significant effect on topotecan pharmacokinetics in rats or mdr1a/1b (-/-) mice. | Drug metabolism and disposition: the biological fate of chemicals 20050301 |
Investigation of efflux transport of dehydroepiandrosterone sulfate and mitoxantrone at the mouse blood-brain barrier: a minor role of breast cancer resistance protein. | The Journal of pharmacology and experimental therapeutics 20050101 |
Hepatobiliary disposition of the metabolically stable opioid peptide [D-Pen2, D-Pen5]-enkephalin (DPDPE): pharmacokinetic consequences of the interplay between multiple transport systems. | The Journal of pharmacology and experimental therapeutics 20041201 |
Substrates and inhibitors of efflux proteins interfere with the MTT assay in cells and may lead to underestimation of drug toxicity. | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20041001 |
Quantitative analysis of the P-glycoprotein inhibitor Elacridar (GF120918) in human and dog plasma using liquid chromatography with tandem mass spectrometric detection. | Journal of mass spectrometry : JMS 20041001 |
Preclinical pharmacokinetic properties of the P-glycoprotein inhibitor GF120918A (HCl salt of GF120918, 9,10-dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]phenyl]-4-acridine-carboxamide) in the mouse, rat, dog, and monkey. | The Journal of pharmacology and experimental therapeutics 20040801 |
Efficacy of novel P-glycoprotein inhibitors to increase the oral uptake of paclitaxel in mice. | Investigational new drugs 20040801 |
The systemic exposure of an N-methyl-D-aspartate receptor antagonist is limited in mice by the P-glycoprotein and breast cancer resistance protein efflux transporters. | Drug metabolism and disposition: the biological fate of chemicals 20040701 |
P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. | Pharmaceutical research 20040701 |
Improved penetration of docetaxel into the brain by co-administration of inhibitors of P-glycoprotein. | European journal of cancer (Oxford, England : 1990) 20040501 |
Cerebral uptake of mefloquine enantiomers with and without the P-gp inhibitor elacridar (GF1210918) in mice. | British journal of pharmacology 20040401 |
Flavonoid permeability across an in situ model of the blood-brain barrier. | Free radical biology & medicine 20040301 |
Reversal of breast cancer resistance protein-mediated drug resistance by tryprostatin A. | International journal of cancer 20031210 |
Enhanced exposure of phosphatidylserine in human gastric carcinoma cells overexpressing the half-size ABC transporter BCRP (ABCG2). | The Biochemical journal 20031201 |
Disposition of tacrolimus in isolated perfused rat liver: influence of troleandomycin, cyclosporine, and gg918. | Drug metabolism and disposition: the biological fate of chemicals 20031101 |
Increased penetration of paclitaxel into the brain by inhibition of P-Glycoprotein. | Clinical cancer research : an official journal of the American Association for Cancer Research 20030701 |
Effect of efflux inhibition on brain uptake of itraconazole in mice infected with Cryptococcus neoformans. | Drug metabolism and disposition: the biological fate of chemicals 20030301 |
Assessing safety and efficacy of directed P-glycoprotein inhibition to improve the pharmacokinetic properties of saquinavir coadministered with ritonavir. | The Journal of pharmacology and experimental therapeutics 20030201 |
A novel inhibitor of multidrug efflux pumps in Staphylococcus aureus. | The Journal of antimicrobial chemotherapy 20030101 |
Evaluation of the permeation characteristics of a model opioid peptide, H-Tyr-D-Ala-Gly-Phe-D-Leu-OH (DADLE), and its cyclic prodrugs across the blood-brain barrier using an in situ perfused rat brain model. | The Journal of pharmacology and experimental therapeutics 20021101 |
MDR1 modulators improve the chemotherapy response of human hepatoblastoma to doxorubicin in vitro. | Journal of pediatric surgery 20021101 |
Induction of breast cancer resistance protein by the camptothecin derivative DX-8951f is associated with minor reduction of antitumour activity. | British journal of cancer 20020909 |
Boosting bioavailability of topotecan: what do we gain? | Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20020701 |
Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. | Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20020701 |
Effects of a P-glycoprotein inhibitor on brain and plasma concentrations of anti-human immunodeficiency virus drugs administered in combination in rats. | Drug metabolism and disposition: the biological fate of chemicals 20020501 |
A mutation hot spot in the Bcrp1 (Abcg2) multidrug transporter in mouse cell lines selected for Doxorubicin resistance. | Cancer research 20020415 |
Delineating the contribution of secretory transporters in the efflux of etoposide using Madin-Darby canine kidney (MDCK) cells overexpressing P-glycoprotein (Pgp), multidrug resistance-associated protein (MRP1), and canalicular multispecific organic anion transporter (cMOAT). | Drug metabolism and disposition: the biological fate of chemicals 20020401 |
Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. | The Journal of pharmacology and experimental therapeutics 20020301 |
Anti-secretory properties of non-peptide somatostatin receptor agonists in isolated rat colon: luminal activity and possible interaction with P-glycoprotein. | British journal of pharmacology 20020301 |
Bioanalysis and preliminary pharmacokinetics of the acridonecarboxamide derivative GF120918 in plasma of mice and humans by ion-pairing reversed-phase high-performance liquid chromatography with fluorescence detection. | Journal of chromatography. B, Biomedical sciences and applications 20010805 |
Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918. | Clinical cancer research : an official journal of the American Association for Cancer Research 20010401 |
Screening of multidrug-resistance sensitive drugs by in situ brain perfusion in P-glycoprotein-deficient mice. | Pharmaceutical research 20010201 |
In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. | Cancer research 20010115 |
Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. | Bioorganic & medicinal chemistry letters 20010108 |
Co-administration of GF120918 significantly increases the systemic exposure to oral paclitaxel in cancer patients. | British journal of cancer 20010101 |
[Possible structural-functional organization of the system of local cerebral blood flow regulation]. | Fiziologicheskii zhurnal SSSR imeni I. M. Sechenova 19751001 |