{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,9,9]],"date-time":"2025-09-09T20:53:51Z","timestamp":1757451231380,"version":"3.40.5"},"reference-count":34,"publisher":"Wiley","license":[{"start":{"date-parts":[[2014,12,25]],"date-time":"2014-12-25T00:00:00Z","timestamp":1419465600000},"content-version":"unspecified","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/3.0\/"}],"funder":[{"DOI":"10.13039\/501100003958","name":"Dutch Technology Foundation STW","doi-asserted-by":"crossref","award":["10127"],"award-info":[{"award-number":["10127"]}],"id":[{"id":"10.13039\/501100003958","id-type":"DOI","asserted-by":"crossref"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["International Journal of Molecular Imaging"],"published-print":{"date-parts":[[2014,12,25]]},"abstract":"<jats:p>For imaging of dopamine D<jats:sub>2\/3<\/jats:sub>receptors, agonist tracers are favoured over antagonists because they are more sensitive to detection of dopamine release and because they may selectively label the high-affinity receptor state. We have developed novel D<jats:sub>2\/3<\/jats:sub>receptor selective agonists that can be radiolabelled with [<jats:sup>123<\/jats:sup>I], which label is advantageous over most other labels, such as carbon-11, as it has a longer half-life. Particularly, we considered (R) N-[7-hydroxychroman-2-yl]-methyl 4-iodobenzyl amine (compound<jats:bold>1<\/jats:bold>) as an attractive candidate for development as it shows high binding affinity to D<jats:sub>2\/3<\/jats:sub>receptors in vitro, and here we report on the characterization of this first [<jats:sup>123<\/jats:sup>I]-labelled D<jats:sub>2\/3<\/jats:sub>receptor agonist radiopharmaceutical intended for SPECT imaging. The appropriate tin precursor for [<jats:sup>123<\/jats:sup>I]-<jats:bold>1<\/jats:bold>was developed and was successfully radiolabelled with iodine-123 giving a moderate yield (30\u201335%) and a good purity (&gt;95%) for [<jats:sup>123<\/jats:sup>I]-<jats:bold>1<\/jats:bold>. In biodistribution experiments in Wistar rats intravenous injection of [<jats:sup>123<\/jats:sup>I]-<jats:bold>1<\/jats:bold>resulted in a fast brain uptake, where the observed binding in the D<jats:sub>2\/3<\/jats:sub>receptor-rich striatum was slightly higher than that in the cerebellum 30\u2009min to 4\u2009h p.i. Storage phosphor imaging experiments, however, did not show specific D<jats:sub>2\/3<\/jats:sub>receptor binding. In conclusion, despite promising in vitro data for<jats:bold>1<\/jats:bold>, neither specific ex vivo binding nor high signal-to-noise ratios were found in rodents for [<jats:sup>123<\/jats:sup>I]-<jats:bold>1<\/jats:bold>.<\/jats:p>","DOI":"10.1155\/2014\/507012","type":"journal-article","created":{"date-parts":[[2014,12,25]],"date-time":"2014-12-25T21:02:14Z","timestamp":1419541334000},"page":"1-10","source":"Crossref","is-referenced-by-count":1,"title":["Ex Vivo Characterization of a Novel Iodine-123-Labelled Aminomethylchroman as a Potential Agonist Ligand for SPECT Imaging of Dopamine D<sub>2\/3<\/sub>Receptors"],"prefix":"10.1155","volume":"2014","author":[{"given":"Jan-Peter","family":"van Wieringen","sequence":"first","affiliation":[{"name":"Department of Nuclear Medicine, Academic Medical Center, University of Amsterdam, Meibergdreef 9, 1105 AZ Amsterdam, Netherlands"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kora","family":"de Bruin","sequence":"additional","affiliation":[{"name":"Department of Nuclear Medicine, Academic Medical Center, University of Amsterdam, Meibergdreef 9, 1105 AZ Amsterdam, Netherlands"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Henk M.","family":"Janssen","sequence":"additional","affiliation":[{"name":"SyMO-Chem BV, Den Dolech 2, 5612 AZ Eindhoven, Netherlands"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"P. 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