Nuclear Medicine and Biology
Volume 33, Issue 6 , Pages 685-694 , August 2006

Fluoroalkyl derivatives of dihydrotetrabenazine as positron emission tomography imaging agents targeting vesicular monoamine transporters

  • Rajesh Goswami

      Affiliations

    • Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
    • ,
  • Datta E. Ponde

      Affiliations

    • Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
    • ,
  • Mei-Ping Kung

      Affiliations

    • Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
    • ,
  • Catherine Hou

      Affiliations

    • Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
    • ,
  • Mike R. Kilbourn

      Affiliations

    • Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA
    • ,
  • Hank F. Kung

      Affiliations

    • Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
    • Department Pharmacology, University of Pennsylvania, Philadelphia, PA 19104, USA
    • Corresponding Author InformationCorresponding author. Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA. Tel.: +1 215 662 3096; fax: +1 215 349 5035.

Received 13 April 2006 ,Revised 16 May 2006 ,Accepted 25 May 2006.

References 

  1. Albin R, Koeppe R. Rapid loss of striatal VMAT2 binding associated with onset of Lewy body dementia. Mov Disord. 2006;21:287–288
  2. Tatsch K. Can SPET imaging of dopamine uptake sites replace PET imaging in Parkinson's disease? For. Eur J Nucl Med Mol Imaging. 2002;29:711–714
  3. Brooks DJ. Monitoring neuroprotection and restorative therapies in Parkinson's disease with PET. J Neural Transm Suppl. 2000;60:125–137
  4. Brooks DJ. The early diagnosis of Parkinson's disease. Ann Neurol. 1998;44:S10–S18
  5. Frey KA. Can SPET imaging of dopamine uptake sites replace PET imaging in Parkinson's disease? Against. Eur J Nucl Med Mol Imaging. 2002;29:715–717
  6. Lee CS, Samii A, Sossi V, Ruth TJ, Schulzer M, Holden JE, et al. In vivo positron emission tomographic evidence for compensatory changes in presynaptic dopaminergic nerve terminals in Parkinson's disease. Ann Neurol. 2000;47:493–503
  7. Meegalla SK, Plössl K, Kung M-P, Stevenson DA, Mu M, Kushner S, et al. Specificity of diastereomers of [99mTc]TRODAT-1 as dopamine transporter imaging agents. J Med Chem. 1998;41:428–436
  8. Mozley PD, Schneider JS, Acton PD, Plössl K, Stern MB, Siderowf A, et al. Binding of [99mTc]TRODAT-1 to dopamine transporters in patients with Parkinson's disease and in healthy volunteers. J Nucl Med. 2000;41:584–589
  9. Ravina B, Eidelberg D, Ahlskog JE, Albin RL, Brooks DJ, Carbon M, et al. The role of radiotracer imaging in Parkinson disease. Neurology. 2005;64:208–215
  10. Albin RL, Koeppe RA, Bohnen NI, Nichols TE, Meyer P, Wernette K, et al. Increased ventral striatal monoaminergic innervation in Tourette syndrome. Neurology. 2003;61:310–315
  11. Kilbourn MR, Frey KA, Vander Borght T, Sherman PS. Effects of dopaminergic drug treatments on in vivo radioligand binding to brain vesicular monoamine transporters. Nucl Med Biol. 1996;23:467–471
  12. Frey KA, Koeppe RA, Kilbourn MR. Imaging the vesicular monoamine transporter. Adv Neurol. 2001;86:237–247
  13. Bohnen NI, Albin RL, Koeppe RA, Wernette KA, Kilbourn MR, Minoshima S, et al. Positron emission tomography of monoaminergic vesicular binding in aging and Parkinson disease. J Cereb Blood Flow Metab. 2006;[in press]
  14. Lee CS, Schulzer M, de la Fuente-Fernandez R, Mak E, Kuramoto L, Sossi V, et al. Lack of regional selectivity during the progression of Parkinson disease: implications for pathogenesis. Arch Neurol. 2004;61:1920–1925
  15. Kilbourn MR, Lee LC, Heeg MJ, Jewett DM. Absolute configuration of (+)-alpha-dihydrotetrabenazine, an active metabolite of tetrabenazine. Chirality. 1997;9:59–62
  16. Frey KA, Koeppe RA, Kilbourn MR, Vander Borght TM, Albin RL, Gilman S, et al. Presynaptic monoaminergic vesicles in Parkinson's disease and normal aging. Ann Neurol. 1996;40:873–884
  17. Canney DJ, Guo Y-Z, Kung M-P, Kung HF. Synthesis and preliminary evaluation of an iodovinyl-tetrabenazine analog as a marker for the vesicular monoamine transporter. J Lab Compds Radiopharm. 1993;18:355–368
  18. DaSilva JN, Kilbourn MR, Domino EF. In vivo imaging of monoaminergic nerve terminals in normal and MPTP-lesioned primate brain using positron emission tomography (PET) and [11C]tetrabenazine. Synapse. 1993;14:128–131
  19. Kilbourn M, Sherman P. In vivo binding of (+)-[alpha]-[3H]dihydrotetrabenazine to the vesicular monoamine transporter of rat brain: bolus vs. equilibrium studies. Eur J Pharmacol. 1997;331:161–168
  20. Kilbourn M, Lee L, Borght TV, Jewett D, Frey K. Binding of [alpha]-dihydrotetrabenazine to the vesicular monoamine transporter is stereospecific. Eur J Pharmacol. 1995;278:249–252
  21. Scherman D, Raisman R, Ploska A, Agid Y. [3H]Dihydrotetrabenazine, a new in vitro monoaminergic probe for human brain. J Neurochem. 1988;50:1131–1136
  22. Munson PJ, Rodbard D. LIGAND: a versatile computerized approach for characterization of ligand-binding systems. Anal Biochem. 1980;107:220–239

PII: S0969-8051(06)00097-7

doi: 10.1016/j.nucmedbio.2006.05.006

Nuclear Medicine and Biology
Volume 33, Issue 6 , Pages 685-694 , August 2006

Article Tools

* Image Usage & Resolution