NMDA receptor channels: Labeling of MK-801 with iodine-125 and fluorine-18
dc.contributor.author | Wieland, Donald M. | en_US |
dc.contributor.author | Kilbourn, Michael R. | en_US |
dc.contributor.author | Yang, David J. | en_US |
dc.contributor.author | Laborde, E. | en_US |
dc.contributor.author | Gildersleeve, David L. | en_US |
dc.contributor.author | Van Dort, Marcian E. | en_US |
dc.contributor.author | Pirat, Jean-Luc | en_US |
dc.contributor.author | Ciliax, Brian J. | en_US |
dc.contributor.author | Young, Anne B. | en_US |
dc.date.accessioned | 2006-04-07T20:33:55Z | |
dc.date.available | 2006-04-07T20:33:55Z | |
dc.date.issued | 1988 | en_US |
dc.identifier.citation | Wieland, D. M., Kilbourn, M. R., Yang, D. J., Laborde, E., Gildersleeve, D. L., van Dort, M. E., Pirat, J-L., Ciliax, B. J., Young, A. B. (1988)."NMDA receptor channels: Labeling of MK-801 with iodine-125 and fluorine-18." International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes 39(12): 1219-1225. <http://hdl.handle.net/2027.42/27605> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B6X3S-46Y3JK4-VP/2/66118fcaf9013f2e97106b20a90205f0 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/27605 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=2851002&dopt=citation | en_US |
dc.description.abstract | Methods for labeling the glutamate channel blocking agent MK-801 with iodine-125 (125I) and fluorine-18 (18F) are described. Radioiodine was incorporated in the 1- or 3-positions of the aromatic ring of (+/-)MK-801 by solid-state halogen exchange techniques. Attachment of the [18F]fluoromethyl group to the bridgehead methyl position was achieved by reaction of [18F]fluoride with the triflamide alcohol 8 or the novel cyclic sulfamate 9 recently reported by Merck chemists. Radiochemical yields of (+/-)13-[18F]- fluoromethyl-MK-801 were >72%, EOB; radiochemical purity >99%. In competitive binding studies using rat brain homogenates, (+/-)3-bromo-MK-801 showed greater affinity than (+/-)MK-801 for the glutamate-linked channel. The experimental log P (2.1 +/- 0.1) of MK-801 is optimal for transit of the blood-brain barrier. These preliminary findings support further testing of 3-[123I]iodo-MK-801 and (+/-)13-[18F]fluoromethyl-MK-801 as possible agents for in vivo mapping of the glutamate receptor complex. | en_US |
dc.format.extent | 810719 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 | NMDA receptor channels: Labeling of MK-801 with iodine-125 and fluorine-18 | 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.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 | Department of Neurology, University of Michigan Medical School, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.contributor.affiliationum | Department of Neurology, University of Michigan Medical School, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.identifier.pmid | 2851002 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/27605/1/0000649.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1016/0883-2889(88)90103-7 | 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 |
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