{"title":"在采购中性和紧凑的二硫代氨基脲(DTS)衍生物的单体配合物:99mTc-KTS","authors":"Takeo Hosotani , Akira Yokoyama , Yasushi Arano , Kazuko Horiuchi , Hiroko Wasaki , Hideo Saji , Kanji Torizuka","doi":"10.1016/S0047-0740(86)80004-3","DOIUrl":null,"url":null,"abstract":"<div><p>As a basic structure of a bifunctional radiopharmaceutical (BR), dithiosemicarbazone (DTS) enables the formation of a small conjugated chelating ring with divalent metals (Cu<sup>2+</sup>, Zn<sup>2+</sup>, Ni<sup>2+</sup>), yielding stable and compact complexes.</p><p>In the development of a neutral and compact monomelic DTS complex of technetium (<sup>99m</sup>Tc), a DTS containing ligand, kethoxal-bis(thiosemicarbazone) (KTS) was selected. A well known monomelic Cu-KTS complex (or <sup>64</sup>Cu-KTS) is taken as a model compound, and <em>in vitro</em> (TLC, EP, HPLC) and <em>in vivo</em> (mice biodistribution) studies were compared. Using the stannous chloride method, under conditions to avoid the hydrolytic polynucleation of technetium, a good yield of <sup>99m</sup>Tc-KTS with characteristics resembling the non-charged, compact and stable Cu-KTS is obtained, in <em>in vitro</em> as well as <em>in vivo</em> studies. The importance of DTS as the constituent of a BR is discussed.</p></div>","PeriodicalId":75939,"journal":{"name":"International journal of nuclear medicine and biology","volume":"12 6","pages":"Pages 431-437"},"PeriodicalIF":0.0000,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0047-0740(86)80004-3","citationCount":"19","resultStr":"{\"title\":\"In the procurement of a neutral and compact monomeric complex of dithiosemicarbazone (DTS) derivative: 99mTc-KTS\",\"authors\":\"Takeo Hosotani , Akira Yokoyama , Yasushi Arano , Kazuko Horiuchi , Hiroko Wasaki , Hideo Saji , Kanji Torizuka\",\"doi\":\"10.1016/S0047-0740(86)80004-3\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>As a basic structure of a bifunctional radiopharmaceutical (BR), dithiosemicarbazone (DTS) enables the formation of a small conjugated chelating ring with divalent metals (Cu<sup>2+</sup>, Zn<sup>2+</sup>, Ni<sup>2+</sup>), yielding stable and compact complexes.</p><p>In the development of a neutral and compact monomelic DTS complex of technetium (<sup>99m</sup>Tc), a DTS containing ligand, kethoxal-bis(thiosemicarbazone) (KTS) was selected. A well known monomelic Cu-KTS complex (or <sup>64</sup>Cu-KTS) is taken as a model compound, and <em>in vitro</em> (TLC, EP, HPLC) and <em>in vivo</em> (mice biodistribution) studies were compared. Using the stannous chloride method, under conditions to avoid the hydrolytic polynucleation of technetium, a good yield of <sup>99m</sup>Tc-KTS with characteristics resembling the non-charged, compact and stable Cu-KTS is obtained, in <em>in vitro</em> as well as <em>in vivo</em> studies. The importance of DTS as the constituent of a BR is discussed.</p></div>\",\"PeriodicalId\":75939,\"journal\":{\"name\":\"International journal of nuclear medicine and biology\",\"volume\":\"12 6\",\"pages\":\"Pages 431-437\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1986-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/S0047-0740(86)80004-3\",\"citationCount\":\"19\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"International journal of nuclear medicine and biology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0047074086800043\",\"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 nuclear medicine and biology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0047074086800043","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
In the procurement of a neutral and compact monomeric complex of dithiosemicarbazone (DTS) derivative: 99mTc-KTS
As a basic structure of a bifunctional radiopharmaceutical (BR), dithiosemicarbazone (DTS) enables the formation of a small conjugated chelating ring with divalent metals (Cu2+, Zn2+, Ni2+), yielding stable and compact complexes.
In the development of a neutral and compact monomelic DTS complex of technetium (99mTc), a DTS containing ligand, kethoxal-bis(thiosemicarbazone) (KTS) was selected. A well known monomelic Cu-KTS complex (or 64Cu-KTS) is taken as a model compound, and in vitro (TLC, EP, HPLC) and in vivo (mice biodistribution) studies were compared. Using the stannous chloride method, under conditions to avoid the hydrolytic polynucleation of technetium, a good yield of 99mTc-KTS with characteristics resembling the non-charged, compact and stable Cu-KTS is obtained, in in vitro as well as in vivo studies. The importance of DTS as the constituent of a BR is discussed.