{"title":"1,8-二胺-3,6-二硫辛烷(DDO)配体锝-99m配合物的合成、放射化学和生物学评价","authors":"Th Maina, E Chiotellis","doi":"10.1016/0883-2897(92)90162-R","DOIUrl":null,"url":null,"abstract":"<div><p>The synthesis, radiochemical analysis and biological characteristics of some 1,8-diamine-3,6-dithiaoctane derivatives labelled with Tc-99m are reported. Analysis by HPLC shows that most of the <sup>99m</sup>Tc-chelates are multicomponent. Furthermore, almost all <sup>99m</sup>Tc-complexes isolated by HPLC are lipophilic and stable <em>in vitro</em>. The biodistributions of the most lipophilic of these complexes were evaluated in mice. The <em>N</em>-morpholinylethyl and <em>N,N'</em>′-bisalicylyl derivatives of 1,8-diamine-3,6-dithiaoctane yielded <sup>99m</sup>Tc-complexes which exhibit considerable uptake and retention in organs of interest, such as the heart and the brain.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 4","pages":"Pages 481-489"},"PeriodicalIF":0.0000,"publicationDate":"1992-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90162-R","citationCount":"2","resultStr":"{\"title\":\"Synthesis, radiochemistry and biological evaluation of technetium-99m complexes with 1,8-diamine-3,6-dithiaoctane (DDO) ligands\",\"authors\":\"Th Maina, E Chiotellis\",\"doi\":\"10.1016/0883-2897(92)90162-R\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The synthesis, radiochemical analysis and biological characteristics of some 1,8-diamine-3,6-dithiaoctane derivatives labelled with Tc-99m are reported. Analysis by HPLC shows that most of the <sup>99m</sup>Tc-chelates are multicomponent. Furthermore, almost all <sup>99m</sup>Tc-complexes isolated by HPLC are lipophilic and stable <em>in vitro</em>. The biodistributions of the most lipophilic of these complexes were evaluated in mice. The <em>N</em>-morpholinylethyl and <em>N,N'</em>′-bisalicylyl derivatives of 1,8-diamine-3,6-dithiaoctane yielded <sup>99m</sup>Tc-complexes which exhibit considerable uptake and retention in organs of interest, such as the heart and the brain.</p></div>\",\"PeriodicalId\":14328,\"journal\":{\"name\":\"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology\",\"volume\":\"19 4\",\"pages\":\"Pages 481-489\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1992-05-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0883-2897(92)90162-R\",\"citationCount\":\"2\",\"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/088328979290162R\",\"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/088328979290162R","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis, radiochemistry and biological evaluation of technetium-99m complexes with 1,8-diamine-3,6-dithiaoctane (DDO) ligands
The synthesis, radiochemical analysis and biological characteristics of some 1,8-diamine-3,6-dithiaoctane derivatives labelled with Tc-99m are reported. Analysis by HPLC shows that most of the 99mTc-chelates are multicomponent. Furthermore, almost all 99mTc-complexes isolated by HPLC are lipophilic and stable in vitro. The biodistributions of the most lipophilic of these complexes were evaluated in mice. The N-morpholinylethyl and N,N'′-bisalicylyl derivatives of 1,8-diamine-3,6-dithiaoctane yielded 99mTc-complexes which exhibit considerable uptake and retention in organs of interest, such as the heart and the brain.
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