Characterization of [11C]tetrabenazine as an in vivo radioligand for the vesicular monoamine transporter
dc.contributor.author | DaSilva, Jean N. | en_US |
dc.contributor.author | Carey, James E. | en_US |
dc.contributor.author | Sherman, Philip S. | en_US |
dc.contributor.author | Pisani, Teresa J. | en_US |
dc.contributor.author | Kilbourn, Michael R. | en_US |
dc.date.accessioned | 2006-04-10T18:22:00Z | |
dc.date.available | 2006-04-10T18:22:00Z | |
dc.date.issued | 1994-02 | en_US |
dc.identifier.citation | Dasilva, Jean N., Carey, James E., Sherman, Philip S., Pisani, Teresa J., Kilbourn, Michael R. (1994/02)."Characterization of [11C]tetrabenazine as an in vivo radioligand for the vesicular monoamine transporter." Nuclear Medicine and Biology 21(2): 151-156. <http://hdl.handle.net/2027.42/31800> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B6T9Y-4BXGNF7-1M/2/f0614a8b30aaf327ad98792a17c1820c | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/31800 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=9234277&dopt=citation | en_US |
dc.description.abstract | [11C]Tetrabenazine ([11C]TBZ) is a new in vivo radioligand for positron emission tomographic (PET) imaging of vesicular monoamine transporters. The in vivo distribution, metabolism and pharmacological specificity of [11C]TBZ has been determined in rodents. Regional mouse brain retention of [11C]TBZ is highest in brain regions with greatest monoaminergic innervation (striatum, hypothalamus) and can be reduced with ligands for the monoamine vesicular transporter (TBZ, ketanserin) but not haloperidol, a dopamine D2 receptor antagonist. Chromatographic analysis of rat blood demonstrated rapid metabolism of [11C]TBZ to radiolabeled metabolites ([alpha]- and /gb-[11C]dihydrotetrabenazine) resulting from reduction of the 2-keto group. These metabolites, as well as a third potential metabolite, 9-O-desmethylTBZ, have been synthesized in unlabeled form and all three were shown to be capable of greatly reducing in vivo accumulation of [11C]TBZ in mouse striatum and hypothalamus. Whole body biodistribution of radioactivity after [11C]TBZ injection was determined in rats, and the data used to calculate the expected human dosimetry from this radiotracer. These studies demonstrated that [11C]TBZ can be safely administered for in vivo PET imaging and semi-quantitative determination of vesicular monoamine transporters in living human brain, but quantitative pharmacokinetic modeling of radioactivity distribution will be complicated by the presence of pharmacologically active metabolites. | en_US |
dc.format.extent | 723985 bytes | |
dc.format.extent | 3118 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | Elsevier | en_US |
dc.title | Characterization of [11C]tetrabenazine as an in vivo radioligand for the vesicular monoamine transporter | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Radiology | en_US |
dc.subject.hlbsecondlevel | Physics | en_US |
dc.subject.hlbsecondlevel | Biological Chemistry | en_US |
dc.subject.hlbtoplevel | Science | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109-0552, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109-0552, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109-0552, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109-0552, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109-0552, U.S.A. | en_US |
dc.identifier.pmid | 9234277 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/31800/1/0000746.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1016/0969-8051(94)90003-5 | en_US |
dc.identifier.source | Nuclear Medicine and Biology | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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