Assessment of cerebral P-glycoprotein expression and function with PET by combined [11C]inhibitor and [11C]substrate scans in rats

Nuclear Medicine and Biology

Volumn 40, Issue 6, 2013, Pages 755-763

  Müllauer, Julia ^a   Karch, Rudolf ^b   Bankstahl, Jens P ^c   Bankstahl, Marion ^d   Stanek, Johann ^a   Wanek, Thomas ^a   Mairinger, Severin ^a,e   Müller, Markus ^b   Löscher, Wolfgang ^d   Langer, Oliver ^a,b   Kuntner, Claudia ^a  

^a AIT AUSTRIAN INSTITUTE OF TECHNOLOGY   (Austria)

^b MEDICAL UNIVERSITY OF VIENNA   (Austria)

^c HANNOVER MEDICAL SCHOOL   (Germany)

^d UNIVERSITY OF VETERINARY MEDICINE HANNOVER   (Germany)

^e UNIVERSITY OF VIENNA   (Austria)

Author keywords

(R) 11C verapamil; 11C elacridar; 11C tariquidar; Blood brain barrier; P glycoprotein; Positron emission tomography

Indexed keywords

ELACRIDAR C 11; MULTIDRUG RESISTANCE PROTEIN; TARIQUIDAR; TARIQUIDAR C 11; TRACER; UNCLASSIFIED DRUG; VERAPAMIL C 11;

ANIMAL EXPERIMENT; ARTICLE; BLOOD BRAIN BARRIER; BRAIN; COMPARTMENT MODEL; DRUG DISTRIBUTION; DRUG PROTEIN BINDING; DRUG TRANSPORT; FEMALE; ISOTOPE LABELING; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PROTEIN EXPRESSION; PROTEIN FUNCTION; RADIOACTIVITY; RAT;

EID: 84881029052     PISSN: 09698051     EISSN: 18729614     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2013.05.005     Document Type: Article

References (36)

1. Löscher W., Potschka H. Role of drug efflux transporters in the brain for drug disposition and treatment of brain diseases. Prog Neurobiol 2005, 76(1):22-76.
2. Giacomini K.M., Huang S.M., Tweedie D.J., Benet L.Z., Brouwer K.L., Chu X., et al. Membrane transporters in drug development. Nat Rev Drug Discov 2010, 9(3):215-236.
3. 11C-verapamil and PET. J Nucl Med 2009, 50(12):1954-1961.
4. Sasongko L., Link J.M., Muzi M., Mankoff D.A., Yang X., Collier A.C., et al. Imaging P-glycoprotein transport activity at the human blood-brain barrier with positron emission tomography. Clin Pharmacol Ther 2005, 77(6):503-514.
5. 11C]verapamil and PET. J Cereb Blood Flow Metab 2007, 27(2):424-433.
6. 11C-N-desmethyl-loperamide in monkeys. J Nucl Med 2009, 50(1):108-115.
7. 11C]verapamil PET. Eur J Nucl Med Mol Imaging 2010, 37(5):942-953.
8. 11C-N-desmethyl-loperamide. J Nucl Med 2010, 51(4):559-566.
9. 11C]verapamil and tariquidar at the human blood-brain barrier: a comparison with rat data. Clin Pharmacol Ther 2012, 91(2):227-233.
10. 11C]verapamil measured with PET. Neuroimage 2003, 20(3):1775-1782.
11. Bankstahl J.P., Bankstahl M., Kuntner C., Stanek J., Wanek T., Meier M., et al. A novel PET imaging protocol identifies seizure-induced regional overactivity of P-glycoprotein at the blood-brain barrier. J Neurosci 2011, 31(24):8803-8811.
12. 11C]WIN 35,428. Synapse 1993, 15(2):130-142.
13. Ginovart N., Wilson A.A., Meyer J.H., Hussey D., Houle S. Positron emission tomography quantification of [(11)C]-DASB binding to the human serotonin transporter: modeling strategies. J Cereb Blood Flow Metab 2001, 21(11):1342-1353.
14. Martin C., Berridge G., Mistry P., Higgins C., Charlton P., Callaghan R. The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein. Br J Pharmacol 1999, 128(2):403-411.
15. Hyafil F., Vergely C., Du Vignaud P., Grand-Perret T. In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res 1993, 53(19):4595-4602.
16. Kawamura K., Yamasaki T., Konno F., Yui J., Hatori A., Yanamoto K., et al. Evaluation of limiting brain penetration related to P-glycoprotein and breast cancer resistance protein using [(11)C]GF120918 by PET in mice. Mol Imaging Biol 2011, 13(1):152-160.
17. Kawamura K., Konno F., Yui J., Yamasaki T., Hatori A., Yanamoto K., et al. Synthesis and evaluation of [(11)C]XR9576 to assess the function of drug efflux transporters using PET. Ann Nucl Med 2010, 24(5):403-412.
18. 11C]-elacridar as a radiotracer to assess the distribution of P-glycoprotein at the blood-brain barrier. J Med Chem 2009, 52(19):6073-6082.
19. 11C]tariquidar, a positron emission tomography radiotracer based on a third-generation P-glycoprotein inhibitor. Bioorg Med Chem 2010, 18(15):5489-5497.
20. Kannan P., Telu S., Shukla S., Ambudkar S.V., Pike V.W., Halldin C., et al. The "specific" P-glycoprotein inhibitor tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2). ACS Chem Neurosci 2011, 2(2):82-89.
21. Wanek T., Kuntner C., Bankstahl J.P., Mairinger S., Bankstahl M., Stanek J., et al. A novel PET protocol for visualization of breast cancer resistance protein function at the blood-brain barrier. J Cereb Blood Flow Metab 2012, 32(11):2002-2011.
22. Bankstahl J.P., Bankstahl M., Römermann K., Wanek T., Stanek J., Windhorst A.D., et al. Tariquidar and elacridar are dose-dependently transported by p-glycoprotein and bcrp at the blood-brain barrier: a small-animal positron emission tomography and in vitro study. Drug Metab Dispos 2013, 41(4):754-762.
23. 11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in rats. Nucl Med Biol 2009, 36(6):643-649.
24. 11C]verapamil for detection of P-glycoprotein-expressing murine breast cancer. Eur J Nucl Med Mol Imaging 2012, 39(1):149-159.
25. Brunner M., Langer O., Sunder-Plassmann R., Dobrozemsky G., Müller U., Wadsak W., et al. Influence of functional haplotypes in the drug transporter gene ABCB1 on central nervous system drug distribution in humans. Clin Pharmacol Ther 2005, 78(2):182-190.
26. Gunn R.N., Gunn S.R., Cunningham V.J. Positron emission tomography compartmental models. J Cereb Blood Flow Metab 2001, 21(6):635-652.
27. 11C]verapamil. Epilepsia 2007, 48(9):1774-1784.
28. 11C-methyl]-(-)-cocaine PET studies in human subjects. J Cereb Blood Flow Metab 1990, 10(5):740-747.
29. 11C]methylpiperidin-4-yl propionate: alternatives for analysis of an irreversible positron emission tomography trace for measurement of acetylcholinesterase activity in human brain. J Cereb Blood Flow Metab 1999, 19(10):1150-1163.
30. Syvänen S., Blomquist G., Sprycha M., Urban Hoglund A., Roman M., Eriksson O., et al. Duration and degree of cyclosporin induced P-glycoprotein inhibition in the rat blood-brain barrier can be studied with PET. Neuroimage 2006, 32(3):1134-1141.
31. Kannan P., Brimacombe K.R., Kreisl W.C., Liow J.S., Zoghbi S.S., Telu S., et al. 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, 108(6):2593-2598.
32. 18F]MPPF uptake in rat brain and peripheral tissues: microPET and ex vivo studies. Eur J Nucl Med Mol Imaging 2008, 35(12):2256-2266.
33. van Vliet E.A., van Schaik R., Edelbroek P.M., Voskuyl R.A., Redeker S., Aronica E., et al. Region-specific overexpression of P-glycoprotein at the blood-brain barrier affects brain uptake of phenytoin in epileptic rats. J Pharmacol Exp Ther 2007, 322(1):141-147.
34. Kamiie J., Ohtsuki S., Iwase R., Ohmine K., Katsukura Y., Yanai K., et al. Quantitative atlas of membrane transporter proteins: development and application of a highly sensitive simultaneous LC/MS/MS method combined with novel in-silico peptide selection criteria. Pharm Res 2008, 25(6):1469-1483.
35. Pardridge W.M. Blood-brain barrier biology and methodology. J Neurovirol 1999, 5(6):556-569.
36. Kannan P., Pike V.W., Halldin C., Langer O., Gottesman M.M., Innis R.B., et al. Factors that limit PET imaging of P-glycoprotein density at the blood-brain barrier. Mol Pharm 2013, 10(6):2222-2229.