Iodine-125 and fluorine-18 labeled aryl-1,4-dialkylpiperazines: Potential radiopharmaceuticals for in vivo study of the dopamine uptake system
dc.contributor.author | Van Dort, Marcian E. | en_US |
dc.contributor.author | Kilbourn, Michael R. | en_US |
dc.contributor.author | Chakraborty, Pulak K. | en_US |
dc.contributor.author | Richfield, Eric K. | en_US |
dc.contributor.author | Gildersleeve, David L. | en_US |
dc.contributor.author | Wieland, Donald M. | en_US |
dc.date.accessioned | 2006-04-10T15:15:09Z | |
dc.date.available | 2006-04-10T15:15:09Z | |
dc.date.issued | 1992-05 | en_US |
dc.identifier.citation | van Dort, Marcian E., Kilbourn, Michael R., Chakraborty, Pulak K., Richfield, Eric K., Gildersleeve, David L., Wieland, Donald M. (1992/05)."Iodine-125 and fluorine-18 labeled aryl-1,4-dialkylpiperazines: Potential radiopharmaceuticals for in vivo study of the dopamine uptake system." International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes 43(5): 671-680. <http://hdl.handle.net/2027.42/30090> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B6X3S-478BP45-21/2/a0ba473a07ac7e8e8512944a8116778c | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/30090 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=1325425&dopt=citation | en_US |
dc.description.abstract | A series of fluorine-18 and iodine-125 labeled aryl-1,4-dialkylpiperazine analogs, derivatives of GBR 12935, were synthesized as radiotracers for positron emission tomography or single photon emission computerized tomography imaging of the brain based on their affinity for the presynaptic dopamine reuptake system. High specific activity fluorine-18 tracers were prepared by nucleophilic aromatic substitution reactions; iodine-125 tracers were prepared by isotopic exchange reactions. In vitro competitive binding studies demonstrated that iodine substitution is tolerated in the 4-position of the phenyl ring of the phenalkylpiperazine group. In vivo regional brain biodistribution studies in mice indicated no selectivity of the radioiodinated ligands for the dopamine reuptake site, with striatum/cerebellum concentration ratios of 1. Similar negative results with the new fluorine-18 derivatives demonstrated that in vivo selectivity for the dopamine reuptake site appears to be critically dependent on the carbon chain length between the piperazine ring and the solitary aromatic ring. These studies suggest that development of new radiopharmaceuticals based on the GBR 12935 structure cannot be based solely on considerations of in vitro binding affinities. | en_US |
dc.format.extent | 1073808 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 | Iodine-125 and fluorine-18 labeled aryl-1,4-dialkylpiperazines: Potential radiopharmaceuticals for in vivo study of the dopamine uptake system | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Physics | en_US |
dc.subject.hlbsecondlevel | Nuclear Engineering and Radiological Sciences | en_US |
dc.subject.hlbtoplevel | Science | en_US |
dc.subject.hlbtoplevel | Engineering | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical School, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical School, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical School, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical School, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, Department of Internal Medicine, University of Michigan Medical School, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.contributor.affiliationother | Neurology Unit, University of Rochester, Monroe Community Hospital, 435 East Henrietta Road, Rochester, NY 14620, U.S.A. | en_US |
dc.identifier.pmid | 1325425 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/30090/1/0000461.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1016/0883-2889(92)90039-H | en_US |
dc.identifier.source | International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
Files in this item
Remediation of Harmful Language
The University of Michigan Library aims to describe library materials in a way that respects the people and communities who create, use, and are represented in our collections. Report harmful or offensive language in catalog records, finding aids, or elsewhere in our collections anonymously through our metadata feedback form. More information at Remediation of Harmful Language.
Accessibility
If you are unable to use this file in its current format, please select the Contact Us link and we can modify it to make it more accessible to you.