In vitro and ex vivo evaluation of cyclic aminoalkyl benzilates as potential emission tomography ligands for the muscarinic receptor
dc.contributor.author | Otto, Charlotte A. | en_US |
dc.contributor.author | Mulholland, G. Keith | en_US |
dc.contributor.author | Perry, S. E. | en_US |
dc.contributor.author | Combs, R. | en_US |
dc.contributor.author | Sherman, Phillip S. | en_US |
dc.contributor.author | Fisher, S. J. | en_US |
dc.date.accessioned | 2006-04-07T20:55:58Z | |
dc.date.available | 2006-04-07T20:55:58Z | |
dc.date.issued | 1989 | en_US |
dc.identifier.citation | Otto, C. A., Mulholland, G. K., Perry, S. E., Combs, R., Sherman, P. S., Fisher, S. J. (1989)."In vitro and ex vivo evaluation of cyclic aminoalkyl benzilates as potential emission tomography ligands for the muscarinic receptor." International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology 16(1): 51-55. <http://hdl.handle.net/2027.42/28116> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B7GH9-4D44P7N-9/2/cb55940f715c312f45841eb12a22984a | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/28116 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=2785511&dopt=citation | en_US |
dc.description.abstract | A series of muscarinic antagonists were screened as potential receptor imaging agents. (+)2[alpha]-tropanyl benzilate (TRB), N-methyl-4-piperidyl benzilate (NMPB) and several analogs amenable to labeling with positron emitting isotopes were evaluated for muscarinic binding to mouse brain tissue in vitro and ex vivo using [3H]quinuclidinyl benzilate as the probe. The in vitro assay directly compared the innate binding affinities of the compounds. The rank order of binding (IC50) was TRB (0.7 nm), QNB (0.8 nm), scopolamine (1.3 nm) and NMPB (1.6 nm). The ex vivo assay was used to gain information regarding the pharmacokinetics and brain penetration of the compounds in live animals. Ex vivo results demonstrated that TRB was rapidly taken up into the brain and was equipotent with QNB in occupying muscarinic binding sites at early time points, but TRB binding decreased twice as fast over time as QNB binding. The results suggest TRB would be a good candidate for radiolabeling and further study. | en_US |
dc.format.extent | 384617 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 | In vitro and ex vivo evaluation of cyclic aminoalkyl benzilates as potential emission tomography ligands for the muscarinic receptor | 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 | Department of Natural Sciences, University of Michigan-Dearborn, Dearborn, MI 48128, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.contributor.affiliationum | Department of Natural Sciences, University of Michigan-Dearborn, Dearborn, MI 48128, U.S.A. | en_US |
dc.contributor.affiliationum | Department of Natural Sciences, University of Michigan-Dearborn, Dearborn, MI 48128, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.contributor.affiliationum | Division of Nuclear Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109, U.S.A. | en_US |
dc.identifier.pmid | 2785511 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/28116/1/0000565.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1016/0883-2897(89)90215-8 | en_US |
dc.identifier.source | International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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