| pubmed-article:12620070 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C0170657 | lld:lifeskim |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C0023688 | lld:lifeskim |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C0303023 | lld:lifeskim |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C0040395 | lld:lifeskim |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C1708632 | lld:lifeskim |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C1708481 | lld:lifeskim |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C1880022 | lld:lifeskim |
| pubmed-article:12620070 | lifeskim:mentions | umls-concept:C1522485 | lld:lifeskim |
| pubmed-article:12620070 | pubmed:issue | 6 | lld:pubmed |
| pubmed-article:12620070 | pubmed:dateCreated | 2003-3-6 | lld:pubmed |
| pubmed-article:12620070 | pubmed:abstractText | 2beta-Carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane (ZIENT) (6) and 2beta-carbomethoxy-3beta-(4'-((E)-2-iodoethenyl)phenyl)nortropane (EIENT) (10) were prepared and evaluated in vitro and in vivo for serotonin transporter (SERT) selectivity and specificity. High specific activity [(123)I]ZIENT and [(123)I]EIENT were synthesized in 45% (n = 5) and 42% (n = 4) radiochemical yield (decay-corrected to end of bombardment (EOB)), respectively, by preparation of the precursor carbomethoxy-3beta-(4'-((Z)-2-trimethylstannylethenyl)phenyl)nortropane (7) and 2beta-carbomethoxy-3beta-(4'-((E)-2-tributylstannylethenyl)phenyl)nortropane (9), respectively, followed by treatment with no carrier-added sodium [(123)I]iodide and hydrogen peroxide in ethanolic HCl. Competition binding in cells stably expressing the transfected human SERT, dopamine transporter (DAT), and norepinephrine transporter (NET) using [(3)H]citalopram, [(3)H]WIN 35,428, and [(3)H]nisoxetine, respectively, demonstrated the following order of SERT affinity (K(i) in nM): ZIENT (0.05) > nor-CIT (0.12) >> EIENT (1.15) > fluvoxamine (1.46). The affinity of ZIENT and EIENT for DAT was 69 and 1.6-fold lower, respectively, than for SERT. In vivo biodistribution and blocking studies were performed in male rats and demonstrated that the brain uptake of [(123)I]ZIENT was selective and specific for SERT-rich regions (hypothalamus, striatum, pons, and prefrontal cortex). SPECT brain imaging studies in monkeys demonstrated high [(123)I]ZIENT uptake in the diencephalon, which resulted in diencephalon-to-cerebellum ratios of 2.12 at 190 min. [(123)I]ZIENT uptake in the diencephalon achieved transient equilibrium at 157 min. In a displacement experiment of [(123)I]ZIENT in a cynomolgus monkey, radioactivity was reduced by 39% in the diencephalon at 101 min following injection of citalopram. The high specific activity one-step radiolabeling preparation and high selectivity of [(123)I]ZIENT for SERT support its candidacy as a radioligand for mapping brain SERT sites. | lld:pubmed |
| pubmed-article:12620070 | pubmed:language | eng | lld:pubmed |
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| pubmed-article:12620070 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:12620070 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:12620070 | pubmed:month | Mar | lld:pubmed |
| pubmed-article:12620070 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:12620070 | pubmed:author | pubmed-author:NwaforP APA | lld:pubmed |
| pubmed-article:12620070 | pubmed:author | pubmed-author:NemeroffCharl... | lld:pubmed |
| pubmed-article:12620070 | pubmed:author | pubmed-author:ChenPingP | lld:pubmed |
| pubmed-article:12620070 | pubmed:author | pubmed-author:ShiBingB | lld:pubmed |
| pubmed-article:12620070 | pubmed:author | pubmed-author:VotawJohn RJR | lld:pubmed |
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| pubmed-article:12620070 | pubmed:author | pubmed-author:PlissonChrist... | lld:pubmed |
| pubmed-article:12620070 | pubmed:author | pubmed-author:GaltJamesJ | lld:pubmed |
| pubmed-article:12620070 | pubmed:author | pubmed-author:MalveauxGeneG | lld:pubmed |
| pubmed-article:12620070 | pubmed:author | pubmed-author:HowellLeonard... | lld:pubmed |
| pubmed-article:12620070 | pubmed:author | pubmed-author:McConathyJonJ | lld:pubmed |
| pubmed-article:12620070 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:12620070 | pubmed:day | 13 | lld:pubmed |
| pubmed-article:12620070 | pubmed:volume | 46 | lld:pubmed |
| pubmed-article:12620070 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:12620070 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:12620070 | pubmed:pagination | 925-35 | lld:pubmed |
| pubmed-article:12620070 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
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| pubmed-article:12620070 | pubmed:year | 2003 | lld:pubmed |
| pubmed-article:12620070 | pubmed:articleTitle | Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography. | lld:pubmed |
| pubmed-article:12620070 | pubmed:affiliation | Department of Radiology, Emory University, Atlanta, Georgia 30320, USA. mgoodma@emory.edu | lld:pubmed |
| pubmed-article:12620070 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:12620070 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| pubmed-article:12620070 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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