Nuclear Medicine and Biology
Volume 36, Issue 6 , Pages 643-649 , August 2009

Evaluation of [11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in rats

Received 27 October 2008 ,Revised 27 January 2009 ,Accepted 16 March 2009.

References 

  1. de Lange EC, Danhof M. Considerations in the use of cerebrospinal fluid pharmacokinetics to predict brain target concentrations in the clinical setting: implications of the barriers between blood and brain. Clin Pharmacokinet. 2002;41:691–703
  2. Gloor SM, Wachtel M, Bolliger MF, Ishihara H, Landmann R, Frei K. Molecular and cellular permeability control at the blood–brain barrier. Brain Res Brain Res Rev. 2001;36:258–264
  3. Pardridge WM. CNS drug design based on principles of blood–brain barrier transport. J Neurochem. 1998;70:1781–1792
  4. Taylor EM. The impact of efflux transporters in the brain on the development of drugs for CNS disorders. Clin Pharmacokinet. 2002;41:81–92
  5. Kuhnke D, Jedlitschky G, Grube M, et al. MDR1-P-Glycoprotein (ABCB1) mediates transport of Alzheimer's amyloid-beta peptides—implications for the mechanisms of Abeta clearance at the blood–brain barrier. Brain Pathol. 2007;17:347–353
  6. Marchi N, Hallene KL, Kight KM, et al. Significance of MDR1 and multiple drug resistance in refractory human epileptic brain. BMC Med. 2004;2:37
  7. Bigott HM, Mc Carthy DW, Wurst FR, Dahlheimer JL, Piwnica-Worms D, Welch MJ. Production, processing and uses of 94mTC. J Lab Compd Radiopharm. 2001;44:s119–s121
  8. Lewis JS, Dearling JL, Sosabowski JK, et al. Copper bis(diphosphine) complexes: radiopharmaceuticals for the detection of multi-drug resistance in tumours by PET. Eur J Nucl Med. 2000;27:638–646
  9. Sharma V, Beatty A, Wey SP, et al. Novel gallium(III) complexes transported by MDR1 P-glycoprotein: potential PET imaging agents for probing P-glycoprotein-mediated transport activity in vivo. Chem Biol. 2000;7:335–343
  10. Hendrikse NH, de Vries EG, Franssen EJ, Vaalburg W, van der Graaf WT. In vivo measurement of [11C]verapamil kinetics in human tissues. Eur J Clin Pharmacol. 2001;56:827–829
  11. Bartels AL, van Berckel BN, Lubberink M, Luurtsema G, Lammertsma AA, Leenders KL. Blood–brain barrier P-glycoprotein function is not impaired in early Parkinson's disease. Parkinsonism Relat Disord. 2008;14:505–508
  12. Lazarova N, Zoghbi SS, Hong J, et al. Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function. J Med Chem. 2008;19:6034–6043
  13. Zoghbi SS, Liow JS, Yasuno F, et al. [11C]Loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein efflux. J Nucl Med. 2008;49:649–656
  14. Mehta BM, Rosa E, Biedler JL, Larson SM. In vivo uptake of carbon-14-colchicine for identification of tumor multidrug resistance. J Nucl Med. 1994;35:1179–1184
  15. Bart J, Willemsen AT, Groen HJ, et al. Quantitative assessment of P-glycoprotein function in the rat blood–brain barrier by distribution volume of [11C]verapamil measured with PET. NeuroImage. 2003;20:1775–1782
  16. Kortekaas R, Leenders KL, van Oostrom JC, et al. Blood–brain barrier dysfunction in parkinsonian midbrain in vivo. Ann Neurol. 2005;57:176–179
  17. Sasongko L, Link JM, Muzi M, et al. Imaging P-glycoprotein transport activity at the human blood–brain barrier with positron emission tomography. Clin Pharmacol Ther. 2005;77:503–514
  18. Lubberink M, Luurtsema G, van Berckel BN, et al. Evaluation of tracer kinetic models for quantification of P-glycoprotein function using (R)-[11C]verapamil and PET. J Cereb Blood Flow Metab. 2006;27:424–433
  19. Bankstahl JP, Kuntner C, Abrahim A, et al. Tariquidar-induced P-glycoprotein inhibition at the rat blood–brain barrier studied with (R)-[11C]verapamil and PET. J Nucl Med. 2008;49:1328–1335
  20. Luurtsema G, Molthoff CF, Windhorst AD, et al. R- and S-[11C]Verapamil as PET tracers for measuring of P-glycoprotein function: in vitro and in vivo evaluation. Nucl Med Biol. 2003;30:747–751
  21. Abrahim A, Luurtsema G, Bauer M, et al. Peripheral metabolism of (R)-[11C]verapamil in epilepsy patients. Eur J Nucl Med Mol Imaging. 2007;
  22. Langer O, Bauer M, Hammers A, et al. Pharmacoresistance in epilepsy: a pilot PET study with the P-glycoprotein substrate (R)-[11C]verapamil. Epilepsia. 2007;48:1774–1784
  23. Toornvliet R, van Berckel BN, Luurtsema G, et al. Effect of age on functional P-glycoprotein in the blood–brain barrier measured by use of (R)-[11C]verapamil and positron emission tomography. Clin Pharmacol Ther. 2006;79:540–548
  24. Luurtsema G, Molthoff CF, Schuit RC, Windhorst AD, Lammertsma AA, Franssen EJ. Evaluation of (R)-[11C]verapamil as PET tracer of P-glycoprotein function in the blood–brain barrier: kinetics and metabolism in the rat. Nucl Med Biol. 2005;32:87–93
  25. Rice A, Michaelis ML, Georg G, Liu Y, Turunen B, Audus KL. Overcoming the blood–brain barrier to taxane delivery for neurodegenerative diseases and brain tumors. J Mol Neurosci. 2003;20:339–343
  26. van Zuylen L, Sparreboom A, van der GA, et al. Disposition of docetaxel in the presence of P-glycoprotein inhibition by intravenous administration of R101933. Eur J Cancer. 2002;38:1090–1099
  27. van Zuylen L, Sparreboom A, van der GA, et al. The orally administered P-glycoprotein inhibitor R101933 does not alter the plasma pharmacokinetics of docetaxel. Clin Cancer Res. 2000;6:1365–1371
  28. Bardelmeijer HA, Ouwehand M, Beijnen JH, Schellens JH, van Tellingen O. Efficacy of novel P-glycoprotein inhibitors to increase the oral uptake of paclitaxel in mice. Invest New Drugs. 2004;22:219–229
  29. Wang RB, Kuo CL, Lien LL, Lien EJ. Structure–activity relationship: analyses of P-glycoprotein substrates and inhibitors. J Clin Pharm Ther. 2003;28:203–228
  30. Thomas H, Coley HM. Overcoming multidrug resistance in cancer: an update on the clinical strategy of inhibiting P-glycoprotein. Cancer Control. 2003;10:159–165
  31. Luurtsema G, Windhorst AD, Mooijer PJ, Herscheid JDM, Lammertsma AA, Franssen EJF. Fully automated high yield synthesis of (R)- and (S)-[11C]verapamil for measuring the P-glycoprotein function with positron emission tomography. J Labelled Compds Radiopharm. 2002;45:1199–1207
  32. Windhorst AD, Linden ter T, Nooij de A, et al. A complete, multipurpose, low cost, fully automated and GMP compliant radiosynthesis system. J Labelled Compnds & Radiopharm. 2001;44:S1052–S1055
  33. Lundkvist C, Halldin C, Swahn CG, et al. [O-Methyl-11C]beta-CIT-FP, a potential radioligand for quantitation of the dopamine transporter: preparation, autoradiography, metabolite studies, and positron emission tomography examinations. Nucl Med Biol. 1995;22:905–913
  34. Bergstrom M, Bonasera TA, Lu L, et al. In vitro and in vivo primate evaluation of carbon-11-etomidate and carbon-11-metomidate as potential tracers for PET imaging of the adrenal cortex and its tumors. J Nucl Med. 1998;39:982–989
  35. Wang JQ, Pollok KE, Cai S, Stantz KM, Hutchins GD, Zheng QH. PET imaging and optical imaging with d-luciferin [11C]methyl ester and d-luciferin [11C]methyl ether of luciferase gene expression in tumor xenografts of living mice. Bioorganic & Medicinal Chemistry Letters. 2006;16:331–337
  36. Mandema JW, Gubbens-Stibbe JM, Danhof M. Stability and pharmacokinetics of flumazenil in the rat. Psychopharmacology (Berl). 1991;103:384–387
  37. Shao X, Lisi JM, Butch ER, Kilbourn MR, Snyder SE. N-Methylpiperidinemethyl, N-methylpyrrolidyl and N-methylpyrrolidinemethyl esters as PET radiotracers for acetylcholinesterase activity. Nuc Med Biol. 2003;30:293–302
  38. Hsiao P, Bui T, Ho RJ, Unadkat JD. In vitro to in vivo prediction of P-glycoprotein based drug interactions at the human and rodent blood–brain barrier. Drug Metab Dispos. 2007;36:481–484
  39. Summerfield SG, Read K, Begley DJ, et al. Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction. J Pharmacol Exp Ther. 2007;322:205–213
  40. Ishiwata K, Kawamura K, Yanai K, Hendrikse NH. In vivo evaluation of P-glycoprotein modulation of 8 PET radioligands used clinically. J Nucl Med. 2007;48:81–87

☆ The presented work was made possible by a financial contribution from the European Community's Seventh Framework Programme, project EURIPIDES, HEALTH-F5-2007-201380.

PII: S0969-8051(09)00082-1

doi: 10.1016/j.nucmedbio.2009.03.004

Nuclear Medicine and Biology
Volume 36, Issue 6 , Pages 643-649 , August 2009

Article Tools

* Image Usage & Resolution