tariquidar






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1 11106230 Phase I trial of XR9576 in healthy volunteers demonstrates modulation of P-glycoprotein in CD56+ lymphocytes after oral and intravenous administration. Clin Cancer Res 2000 Nov 4
2 11212278 In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res 2001 Jan 15 2
3 12576431 Increased 99mTc-sestamibi accumulation in normal liver and drug-resistant tumors after the administration of the glycoprotein inhibitor, XR9576. Clin Cancer Res 2003 Feb 2
4 12712010 Overcoming multidrug resistance in cancer: an update on the clinical strategy of inhibiting p-glycoprotein. Cancer Control 2003 Mar-Apr 1
5 14534356 Pumping of drugs by P-glycoprotein: a two-step process? J Pharmacol Exp Ther 2003 Dec 3
6 14962729 Inhibition of P-glycoprotein function by XR9576 in a solid tumour model can restore anticancer drug efficacy. Eur J Cancer 2004 Mar 1
7 14973080 Pheophorbide a is a specific probe for ABCG2 function and inhibition. Cancer Res 2004 Feb 15 2
8 15457126 Ex vivo reversal of chemoresistance by tariquidar (XR9576). Anticancer Drugs 2004 Oct 3
9 15986399 Phase II study of tariquidar, a selective P-glycoprotein inhibitor, in patients with chemotherapy-resistant, advanced breast carcinoma. Cancer 2005 Aug 15 5
10 16043202 P-glycoprotein activity and biological response. Toxicol Appl Pharmacol 2005 Sep 1 1
11 16190932 A pilot study on brain-to-plasma partition of 10,11-dyhydro-10-hydroxy-5H-dibenzo(b,f)azepine-5-carboxamide and MDR1 brain expression in epilepsy patients not responding to oxcarbazepine. Epilepsia 2005 Oct 1
12 16650133 Inhibition of the multidrug transporter P-glycoprotein improves seizure control in phenytoin-treated chronic epileptic rats. Epilepsia 2006 Apr 1
13 16928449 The multidrug transporter hypothesis of drug resistance in epilepsy: Proof-of-principle in a rat model of temporal lobe epilepsy. Neurobiol Dis 2006 Oct 1
14 16952161 Quantification of serotonin 5-HT1A receptors in monkey brain with [11C](R)-(-)-RWAY. Synapse 2006 Dec 1 1
15 17027274 Determinants of drug brain uptake in a rat model of seizure-associated malformations of cortical development. Neurobiol Dis 2006 Dec 1
16 17326793 Development of a humanized in vitro blood-brain barrier model to screen for brain penetration of antiepileptic drugs. Epilepsia 2007 Mar 2
17 17392402 Region-specific overexpression of P-glycoprotein at the blood-brain barrier affects brain uptake of phenytoin in epileptic rats. J Pharmacol Exp Ther 2007 Jul 1
18 17399990 In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2). Bioorg Med Chem 2007 Jun 1 2
19 17428165 Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor. Expert Rev Anticancer Ther 2007 Apr 5
20 17437408 Upregulation of brain expression of P-glycoprotein in MRP2-deficient TR(-) rats resembles seizure-induced up-regulation of this drug efflux transporter in normal rats. Epilepsia 2007 Apr 2
21 17881135 Multidrug-resistance gene 1-type p-glycoprotein (MDR1 p-gp) inhibition by tariquidar impacts on neuroendocrine and behavioral processing of stress. Psychoneuroendocrinology 2007 Sep-Nov 2
22 17936633 Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives. Bioorg Med Chem 2008 Jan 1 1
23 17958337 Transport of a new erectogenic udenafil in Caco-2 cells. Arch Pharm Res 2007 Sep 1
24 18632828 Tariquidar-induced P-glycoprotein inhibition at the rat blood-brain barrier studied with (R)-11C-verapamil and PET. J Nucl Med 2008 Aug 2
25 18664392 Functional and energetic characterization of P-gp-mediated doxorubicin transport in rainbow trout (Oncorhynchus mykiss) hepatocytes. Comp Biochem Physiol C Toxicol Pharmacol 2009 Jan 4
26 18678495 Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2). Bioorg Med Chem 2008 Sep 1 2
27 18760905 Resistance to antiepileptic drugs and expression of P-glycoprotein in two rat models of status epilepticus. Epilepsy Res 2008 Nov 1
28 18824002 Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology 2008 Dec 1
29 19250834 Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators. Bioorg Med Chem 2009 Mar 15 1
30 19331851 Nanoparticle-mediated simultaneous and targeted delivery of paclitaxel and tariquidar overcomes tumor drug resistance. J Control Release 2009 May 21 1
31 19417029 A phase I study of the P-glycoprotein antagonist tariquidar in combination with vinorelbine. Clin Cancer Res 2009 May 15 6
32 19631619 Polarized P-glycoprotein expression by the immortalised human brain endothelial cell line, hCMEC/D3, restricts apical-to-basolateral permeability to rhodamine 123. Brain Res 2009 Oct 6 3
33 19654309 Moderate increase in Mdr1a/1b expression causes in vivo resistance to doxorubicin in a mouse model for hereditary breast cancer. Cancer Res 2009 Aug 15 1
34 19730994 The antiepileptic drug topiramate is a substrate for human P-glycoprotein but not multidrug resistance proteins. Pharm Res 2009 Nov 2
35 19796699 Uptake and binding of the serotonin 5-HT1A antagonist [18F]-MPPF in brain of rats: effects of the novel P-glycoprotein inhibitor tariquidar. Neuroimage 2010 Jan 15 6
36 19910428 A pilot study to assess the efficacy of tariquidar to inhibit P-glycoprotein at the human blood-brain barrier with (R)-11C-verapamil and PET. J Nucl Med 2009 Dec 4
37 20010957 Assessment of regional differences in tariquidar-induced P-glycoprotein modulation at the human blood-brain barrier. J Cereb Blood Flow Metab 2010 Mar 2
38 20016890 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. Eur J Nucl Med Mol Imaging 2010 May 1
39 20181488 Synthesis of carbon-11-labeled tariquidar derivatives as new PET agents for imaging of breast cancer resistance protein (ABCG2). Appl Radiat Isot 2010 Jun 3
40 20237038 P-glycoprotein function at the blood-brain barrier in humans can be quantified with the substrate radiotracer 11C-N-desmethyl-loperamide. J Nucl Med 2010 Apr 1
41 20460505 The skin cancer chemotherapeutic agent ingenol-3-angelate (PEP005) is a substrate for the epidermal multidrug transporter (ABCB1) and targets tumor vasculature. Cancer Res 2010 Jun 1 5
42 20610168 Synthesis and in vivo evaluation of the putative breast cancer resistance protein inhibitor [11C]methyl 4-((4-(2-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl)phenyl)amino-carbonyl)-2-(quinoline-2-carbonylamino)benzoate. Nucl Med Biol 2010 Jul 3
43 20621487 Synthesis and in vivo evaluation of [11C]tariquidar, a positron emission tomography radiotracer based on a third-generation P-glycoprotein inhibitor. Bioorg Med Chem 2010 Aug 1 2
44 20633036 Imaging of P-glycoprotein-mediated pharmacoresistance in the hippocampus: proof-of-concept in a chronic rat model of temporal lobe epilepsy. Epilepsia 2010 Sep 1
45 21081657 A pharmacodynamic study of docetaxel in combination with the P-glycoprotein antagonist tariquidar (XR9576) in patients with lung, ovarian, and cervical cancer. Clin Cancer Res 2011 Feb 1 1
46 21262843 Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET. Proc Natl Acad Sci U S A 2011 Feb 8 5
47 21514278 The B-cell lymphoma 2 (BCL2)-inhibitors, ABT-737 and ABT-263, are substrates for P-glycoprotein. Biochem Biophys Res Commun 2011 May 6 1
48 21600273 Increasing oxime efficacy by blood-brain barrier modulation. Toxicol Lett 2011 Sep 25 1
49 21677164 A novel positron emission tomography imaging protocol identifies seizure-induced regional overactivity of P-glycoprotein at the blood-brain barrier. J Neurosci 2011 Jun 15 3
50 21692796 In vitro transport profile of carbamazepine, oxcarbazepine, eslicarbazepine acetate, and their active metabolites by human P-glycoprotein. Epilepsia 2011 Oct 1