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396 results

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Page 1
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.
Ward KW, Azzarano LM. Ward KW, et al. J Pharmacol Exp Ther. 2004 Aug;310(2):703-9. doi: 10.1124/jpet.104.068288. Epub 2004 Mar 31. J Pharmacol Exp Ther. 2004. PMID: 15056727
However, to date, a detailed description of the preclinical pharmacokinetic properties of GF120918A has not been published. This investigation was performed to evaluate in vitro and in vivo pharmacokinetic properties of GF120918A in the mouse, rat, dog, and monkey a …
However, to date, a detailed description of the preclinical pharmacokinetic properties of GF120918A has not been published. This inve …
P-glycoprotein (P-gp)-mediated efflux limits intestinal absorption of the Hsp90 inhibitor SNX-2112 in rats.
Liu H, Sun H, Wu Z, Zhang X, Wu B. Liu H, et al. Xenobiotica. 2014 Aug;44(8):763-8. doi: 10.3109/00498254.2014.891781. Epub 2014 Feb 20. Xenobiotica. 2014. PMID: 24555822
By contrast, the compound was well absorbed in the colon with a [Formula: see text] value of 1.19. The P-gp inhibitors cyclosporine and elacridar (i.e. GF120918A) markedly enhanced SNX-2112 absorption in all four intestinal segments (i.e. duodenum, jejunum, ileum an …
By contrast, the compound was well absorbed in the colon with a [Formula: see text] value of 1.19. The P-gp inhibitors cyclosporine and e …
In-vitro respiratory drug absorption models possess nominal functional P-glycoprotein activity.
Madlova M, Bosquillon C, Asker D, Dolezal P, Forbes B. Madlova M, et al. J Pharm Pharmacol. 2009 Mar;61(3):293-301. doi: 10.1211/jpp/61.03.0003. J Pharm Pharmacol. 2009. PMID: 19222901
The purpose of this study was to use the highly specific P-gp inhibitor GF120918A to investigate the activity of the P-gp transporter in the airways to determine whether P-gp could influence inhaled drug disposition. METHODS: P-gp activity was measured as a change in digox …
The purpose of this study was to use the highly specific P-gp inhibitor GF120918A to investigate the activity of the P-gp transporter …
O-[11C]methyl derivative of 6,7-dimethoxy-2-(4-methoxy-biphenyl-4-yl-methyl)-1,2,3,4-tetrahydro-isoquinoline.
Chopra A. Chopra A. 2012 Nov 5 [updated 2013 Jan 31]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2012 Nov 5 [updated 2013 Jan 31]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 23390669 Free Books & Documents. Review.
As an alternative to the use of labeled substrates for the detection and quantification of P-gp in the brain, it was proposed that radiolabeled inhibitors of P-gp, such as [(11)C]laniquidar, [(11)C]elacridar, and [(11)C]traiquidar, would probably yield superior results bec …
As an alternative to the use of labeled substrates for the detection and quantification of P-gp in the brain, it was proposed that radiolabe …
Co-administration of MDR1 and BCRP or EGFR/PI3K inhibitors overcomes lenvatinib resistance in hepatocellular carcinoma.
Sun D, Liu J, Wang Y, Dong J. Sun D, et al. Front Oncol. 2022 Sep 8;12:944537. doi: 10.3389/fonc.2022.944537. eCollection 2022. Front Oncol. 2022. PMID: 36158676 Free PMC article.
Following LR induction, multidrug resistance protein 1 (MDR1) and breast cancer resistance protein (BCRP) transporters were markedly upregulated, and the epidermal growth factor receptor (EGFR), MEK/ERK, and PI3K/AKT pathways were activated. In vitro, the co-administration of …
Following LR induction, multidrug resistance protein 1 (MDR1) and breast cancer resistance protein (BCRP) transporters were markedly upregul …
The Tetrahydroisoquinoline Scaffold in ABC Transporter Inhibitors that Act as Multidrug Resistance (MDR) Reversers.
Teodori E, Braconi L, Manetti D, Romanelli MN, Dei S. Teodori E, et al. Curr Top Med Chem. 2022;22(31):2535-2569. doi: 10.2174/1568026623666221025111528. Curr Top Med Chem. 2022. PMID: 36284399 Review.
However, more recently discovered MDR reversing agents, such as the two tetrahydroisoquinoline derivatives tariquidar and elacridar, are characterized by high affinity towards the ABC proteins and by reduced negative properties. ...
However, more recently discovered MDR reversing agents, such as the two tetrahydroisoquinoline derivatives tariquidar and elacridar, …
Current drug therapy for multiple myeloma.
Huang YW, Hamilton A, Arnuk OJ, Chaftari P, Chemaly R. Huang YW, et al. Drugs. 1999 Apr;57(4):485-506. doi: 10.2165/00003495-199957040-00004. Drugs. 1999. PMID: 10235689 Review.
The clinical application of chemosensitising agents that can inhibit P-glycoprotein (P-gp) expression and function, and particularly the development of more potent P-gp modulators such as valspodar (PSC 833) and elacridar (GF120918) has made it possible to reverse multidru …
The clinical application of chemosensitising agents that can inhibit P-glycoprotein (P-gp) expression and function, and particularly the dev …
Kinetic Models for Measuring P-glycoprotein Function at the Blood-Brain Barrier with Positron Emission Tomography.
Lubberink M. Lubberink M. Curr Pharm Des. 2016;22(38):5786-5792. doi: 10.2174/1381612822666160804093852. Curr Pharm Des. 2016. PMID: 27494063 Review.
Then, the methods that have been used to quantify PET data of the P-gp tracers [11C]verapamil, [11C]N-desmetyl-loperamide (dLop), [11C]laniquidar, [11C]phenytoin, [11C]tariquidar and [11C]elacridar are reviewed. In summary, the extraction of P-gp substrate PET tracers, whi …
Then, the methods that have been used to quantify PET data of the P-gp tracers [11C]verapamil, [11C]N-desmetyl-loperamide (dLop), [11C]laniq …
396 results