Binding characteristics of 9-fluoropropyl-(+)-dihydrotetrabenzazine (AV-133) to the vesicular monoamine transporter type 2 in rats

Nuclear Medicine and Biology

Volumn 37, Issue 4, 2010, Pages 413-419

  Tsao, Hsin Hsin ^a   Lin, Kun Ju ^a   Juang, Jyuhn Huarng ^b   Skovronsky, Daniel M ^c,d   Yen, Tzu Chen ^a   Wey, Shiaw Pyng ^a   Kung, Mei Ping ^a,d  

^a CHANG GUNG UNIVERSITY   (Taiwan)

^b CHANG GUNG MEMORIAL HOSPITAL   (Taiwan)

^c AVID RADIOPHARMACEUTICALS   (United States)

^d UNIVERSITY OF PENNSYLVANIA   (United States)

Author keywords

Autoradiography; Exocrine cells; Homogenate binding; Islet cells; Positron emission tomography

Indexed keywords

9 FLUOROPROPYL DIHYDROTETRABENZAZINE F 18; INSULIN ANTIBODY; TRACER; UNCLASSIFIED DRUG; VESICULAR MONOAMINE TRANSPORTER 2;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BINDING AFFINITY; BINDING SITE; BRAIN; CELL ISOLATION; CELL LABELING; CONTROLLED STUDY; CORPUS STRIATUM; DRUG PROTEIN BINDING; DRUG STRUCTURE; EX VIVO STUDY; EXOCRINE CELL; FROZEN SECTION; HYPOTHALAMUS; IMMUNOHISTOCHEMISTRY; IN VITRO STUDY; MALE; MOLECULAR IMAGING; NONHUMAN; PANCREAS; PANCREAS ISLET BETA CELL; POSITRON EMISSION TOMOGRAPHY; PROTEIN LOCALIZATION; RAT; SPRAGUE DAWLEY RAT; STRUCTURE ACTIVITY RELATION; TISSUE HOMOGENATE;

ANIMALS; AUTORADIOGRAPHY; BRAIN; FLUORINE RADIOISOTOPES; IMMUNOHISTOCHEMISTRY; MALE; MOLECULAR IMAGING; PANCREAS; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; TETRABENAZINE; VESICULAR MONOAMINE TRANSPORT PROTEINS;

EID: 77952551571     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2010.01.002     Document Type: Article

References (24)

1. Souza F., Freeby M., Hultman K., Simpson N., Herron A., Witkowsky P., et al. Current progress in non-invasive imaging of beta cell mass of the endocrine pancreas. Curr Med Chem 2006, 13:2761-2773.
2. Harris P.E., Ferrara C., Barba P., Polito T., Freeby M., Maffei A. VMAT2 gene expression and function as it applies to imaging beta-cell mass. J Mol Med 2008, 86:5-16.
3. Maffei A., Liu Z., Witkowski P., Moschella F., Del Pozzo G., Liu E., et al. Identification of tissue-restricted transcripts in human islets. Endocrinology 2004, 145:4513-4521.
4. Anlauf M., Eissele R., Schafer M.K., Eiden L.E., Arnold R., Pauser U., et al. Expression of the two isoforms of the vesicular monoamine transporter (VMAT1 and VMAT2) in the endocrine pancreas and pancreatic endocrine tumors. J Histochem Cytochem 2003, 51:1027-1040.
5. Souza F., Simpson N., Raffo A., Saxena C., Maffei A., Hardy M., et al. Longitudinal noninvasive PET-based beta cell mass estimates in a spontaneous diabetes rat model. J Clin Invest 2006, 116:1506-1513.
6. 11C-Dihydrotetrabenazine PET of the pancreas in subjects with long-standing type 1 diabetes and in healthy controls. J Nucl Med 2009, 50:382-389.
7. Kilbourn M., Lee L., Borght T.V., Jewett D., Frey K. Binding of [alpha]-dihydrotetrabenazine to the vesicular monoamine transporter is stereospecific. Eur J Pharmacol 1995, 278:249-252.
8. 3H]dihydrotetrabenazine to the vesicular monoamine transporter of rat brain: bolus vs. equilibrium studies. Eur J Pharmacol 1997, 331:161-168.
9. Kilbourn M.R. In vivo radiotracers for vesicular neurotransmitter transporters. Nucl Med Biol 1997, 24:615-619.
10. Bohnen N.I., Albin R.L., Koeppe R.A., Wernette K.A., Kilbourn M.R., Minoshima S., et al. Positron emission tomography of monoaminergic vesicular binding in aging and Parkinson disease. J Cereb Blood Flow Metab 2006, 26:1198-1212.
11. 18F-FDG PET measures in differentiating dementias. J Nucl Med 2005, 46:936-944.
12. Simpson N.R., Souza F., Witkowski P., Maffei A., Raffo A., Herron A., et al. Visualizing pancreatic beta-cell mass with [(11)C]DTBZ. Nucl Med Biol 2006, 33:855-864.
13. Goswami R., Ponde D.E., Kung M.P., Hou C., Kilbourn M.R., Kung H.F. Fluoroalkyl derivatives of dihydrotetrabenazine as positron emission tomography imaging agents targeting vesicular monoamine transporters. Nucl Med Biol 2006, 33:685-694.
14. Kung M.P., Hou C., Goswami R., Ponde D.E., Kilbourn M.R., Kung H.F. Characterization of optically resolved 9-fluoropropyl-dihydrotetrabenazine as a potential PET Imaging agent targeting vesicular monoamine transporters. Nucl Med Biol 2007, 34:239-246.
15. Kilbourn M.R., Hockley B., Lee L., Hou C., Goswami R., Ponde D.E., et al. Pharmacokinetics of [(18)F]fluoroalkyl derivatives of dihydrotetrabenazine in rat and monkey brain. Nucl Med Biol 2007, 34:233-237.
16. 18F-FP-(+)-DTBZ: a potential PET ligand for studying diabetes mellitus. J Nucl Med 2008, 49:1171-1176.
17. Montana E., Bonner-Weir S., Weir G.C. Beta cell mass and growth after syngeneic islet cell transplantation in normal and streptozocin diabetic C57BL/6 mice. J Clin Invest 1993, 91:780-787.
18. el-Naggar M.M., Elayat A.A., Ardawi M.S., Tahir M. Isolated pancreatic islets of the rat: an immunohistochemical and morphometric study. Anat Rec 1993, 237:489-497.
19. Tahir M., Elayat A.A., Jalalah S., el-Naggar M.M. Isolated pancreatic islets of the rat: an ultrastructural study. Acta Anat (Basel) 1992, 145:93-100.
20. Kruger N. Bradford method for protein quantitation. The Protein Protocols Handbook 2002, 15-21. Humana Press, Totowa (NJ). 2nd ed. J.M. Walker (Ed.).
21. Frey R.K., Kilbourn M., Manchanda R., Pontecorvo M., Skovronsky D. Imaging VMAT2 in Parkinson disease with F-18-AV-133. J Nucl Med 2008, 49:5.
22. Clark C., Pontecorvo M., Saha K., Jennings D., Adler L., Zweig R., et al. Test-retest reproducibility of F-18-AV-133 PET imaging of dopaminergic neuron integrity. J Nucl Med 2009, 50:1249.
23. 11C-dihydrotetrabenazine PET: a perspective. J Nucl Med 2009, 50:335-337.
24. Kung H.F., Lieberman B.P., Zhuang Z.P., Oya S., Kung M.P., Choi S.R., et al. In vivo imaging of vesicular monoamine transporter 2 in pancreas using an (18)F epoxide derivative of tetrabenazine. Nucl Med Biol 2008, 35:825-837.