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Among them, N\u2010(3\u2010iodobenzyl)\u20104,5\u2010dihydro\u20101H\u2010imidazol\u20102\u2010amine (Compound <jats:bold>9<\/jats:bold>) displayed the highest affinity for NET (IC<jats:sub>50<\/jats:sub>\u2009=\u20095.65\u2009\u00b1\u20090.97\u2009\u03bcM). The corresponding radiotracer <jats:bold>[<\/jats:bold><jats:sup><jats:bold>125<\/jats:bold><\/jats:sup><jats:bold>I]9<\/jats:bold> was further prepared by copper\u2010mediated radioiodination and evaluated both in vitro and in vivo. The cellular uptake results suggested that <jats:bold>[<\/jats:bold><jats:sup><jats:bold>125<\/jats:bold><\/jats:sup><jats:bold>I]9<\/jats:bold> was specifically taken up by the NET\u2010expressing SK\u2010N\u2010SH cell line. Biodistribution studies showed that <jats:bold>[<\/jats:bold><jats:sup><jats:bold>125<\/jats:bold><\/jats:sup><jats:bold>I]9<\/jats:bold> accumulated in the heart (5.54\u2009\u00b1\u20091.24 %ID\/g at 5\u2009min p.i. and 0.79\u2009\u00b1\u20090.08 %ID\/g at 2\u2009h p.i.) and adrenal gland (14.83\u2009\u00b1\u20093.47 %ID\/g at 5\u2009min p.i. and 3.87\u2009\u00b1\u20090.24 %ID\/g at 2\u2009h p.i.). The uptake in the heart and adrenal gland could be significantly inhibited by preinjection of desipramine (DMI). These results indicated that the benzylaminoimidazoline derivatives retained affinity for NET, which could provide structure\u2013activity relationship data for further studies.<\/jats:p>","DOI":"10.1111\/cbdd.14282","type":"journal-article","created":{"date-parts":[[2023,6,17]],"date-time":"2023-06-17T04:17:45Z","timestamp":1686975465000},"page":"738-748","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Synthesis and preliminary evaluation of benzylaminoimidazoline derivatives as novel norepinephrine transporter ligands"],"prefix":"10.1111","volume":"102","author":[{"given":"Hang","family":"Zhou","sequence":"first","affiliation":[{"name":"Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry Beijing Normal University  Beijing China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jingjing","family":"Yao","sequence":"additional","affiliation":[{"name":"Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry Beijing Normal University  Beijing China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zuoquan","family":"Zhao","sequence":"additional","affiliation":[{"name":"Department of Nuclear Medicine, Cardiovascular Institute and FuWai Hospital Chinese Academy of Medical Sciences  Beijing China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jie","family":"Lu","sequence":"additional","affiliation":[{"name":"Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry Beijing Normal University  Beijing China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2023,6,16]]},"reference":[{"key":"e_1_2_8_2_1","unstructured":"Ajay P. 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