C. Foulon , L. Garreau , S. Chalon , G. Desplanches , Y. Frangin , J.-C. Besnard , J.L. Baulieu , D. Guilloteau
{"title":"Synthesis and in vitro binding properties of halogenated analogues of GBR as new dopamine uptake carrier ligands","authors":"C. Foulon , L. Garreau , S. Chalon , G. Desplanches , Y. Frangin , J.-C. Besnard , J.L. Baulieu , D. Guilloteau","doi":"10.1016/0883-2897(92)90155-R","DOIUrl":null,"url":null,"abstract":"<div><p>We present the original synthesis of two halogenated analogues of the diphenyl piperazine GBR, bromo-GBR and iodo-GBR, as new dopamine uptake carrier ligands. The derivatives were purified by HPLC and chemically characterized. Bromo-GBR and iodo-GBR are potent inhibitors of [<sup>3</sup>H]GBR 12935 binding to rat striatal membrane, with <em>K<sub>i</sub></em> values of 116 and 113 nM, respectively. We prepared iodo-GBR labeled with iodide-125 from the brominated derivative and concluded that [<sup>123</sup>I]iodo-GBR could be a potential tool to explore the <em>in vivo</em> dopamine uptake carrier.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 5","pages":"Pages 597-600"},"PeriodicalIF":0.0000,"publicationDate":"1992-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90155-R","citationCount":"6","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/088328979290155R","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 6
Abstract
We present the original synthesis of two halogenated analogues of the diphenyl piperazine GBR, bromo-GBR and iodo-GBR, as new dopamine uptake carrier ligands. The derivatives were purified by HPLC and chemically characterized. Bromo-GBR and iodo-GBR are potent inhibitors of [3H]GBR 12935 binding to rat striatal membrane, with Ki values of 116 and 113 nM, respectively. We prepared iodo-GBR labeled with iodide-125 from the brominated derivative and concluded that [123I]iodo-GBR could be a potential tool to explore the in vivo dopamine uptake carrier.
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