C. Foulon , L. Garreau , S. Chalon , G. Desplanches , Y. Frangin , J.-C. Besnard , J.L. Baulieu , D. Guilloteau
{"title":"新型多巴胺摄取载体配体卤代GBR类似物的合成及体外结合性能研究","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":"{\"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}","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}
Synthesis and in vitro binding properties of halogenated analogues of GBR as new dopamine uptake carrier ligands
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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