{"title":"锝-99m对碘苯乙基二氨基二硫醇(DADT-IPE): SPECT潜在的脑灌注显像剂","authors":"K. Shiba , H. Mori , H. Matsuda , K. Hisada","doi":"10.1016/0883-2897(92)90115-F","DOIUrl":null,"url":null,"abstract":"<div><p>A new ligand, an <em>N</em>-<em>p</em>-iodophenethyl diaminodithiol (DADT-IPE), an anlog of <em>N</em>-isopropyl-<em>p</em>-iodoamphetamine (IMP), was synthesized and subsequently complexed with <sup>99m</sup>Tc, using stannous chloride as a reducing agent. Two complexes (a and b) were separated from <sup>99m</sup>Tc-DADT-IPE by high performance liquid chromatography (HPLC). Competitive inhibition studies showed that the IC<sub>50</sub> value of DADT-IPE (70 μM) was similar to that of IMP (49 μM). Biodistribution studies of one of the complexes [<sup>99m</sup>Tc-DADT-IPE(a)] in rats showed that 0.65% of the injected dose of the tracer remained in the brain at 5 min after intravenous injection, with 0.53% of the dose remaining in the brain at 60 min post-injection, whereas the corresponding values for the other complex [<sup>99m</sup>Tc-DADT-IPE(b)] were 0.34% dose in the brain at 5 min and 0.28% dose in the brain at 60 min post-injection. The half-life for clearance of <sup>99m</sup>Tc-DADT-IPE(a) from rat brain was found to be more than 5 h. These results suggested that <sup>99m</sup>Tc-DADT-IPE(a) has characteristics which are suitable for cerebral perfusion imaging.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 3","pages":"Pages 303-307, 309-310"},"PeriodicalIF":0.0000,"publicationDate":"1992-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90115-F","citationCount":"1","resultStr":"{\"title\":\"Technetium-99m p-iodophenethyldiaminodithiol (DADT-IPE): Potential brain perfusion imaging agent for SPECT\",\"authors\":\"K. Shiba , H. Mori , H. Matsuda , K. Hisada\",\"doi\":\"10.1016/0883-2897(92)90115-F\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>A new ligand, an <em>N</em>-<em>p</em>-iodophenethyl diaminodithiol (DADT-IPE), an anlog of <em>N</em>-isopropyl-<em>p</em>-iodoamphetamine (IMP), was synthesized and subsequently complexed with <sup>99m</sup>Tc, using stannous chloride as a reducing agent. Two complexes (a and b) were separated from <sup>99m</sup>Tc-DADT-IPE by high performance liquid chromatography (HPLC). Competitive inhibition studies showed that the IC<sub>50</sub> value of DADT-IPE (70 μM) was similar to that of IMP (49 μM). Biodistribution studies of one of the complexes [<sup>99m</sup>Tc-DADT-IPE(a)] in rats showed that 0.65% of the injected dose of the tracer remained in the brain at 5 min after intravenous injection, with 0.53% of the dose remaining in the brain at 60 min post-injection, whereas the corresponding values for the other complex [<sup>99m</sup>Tc-DADT-IPE(b)] were 0.34% dose in the brain at 5 min and 0.28% dose in the brain at 60 min post-injection. The half-life for clearance of <sup>99m</sup>Tc-DADT-IPE(a) from rat brain was found to be more than 5 h. These results suggested that <sup>99m</sup>Tc-DADT-IPE(a) has characteristics which are suitable for cerebral perfusion imaging.</p></div>\",\"PeriodicalId\":14328,\"journal\":{\"name\":\"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology\",\"volume\":\"19 3\",\"pages\":\"Pages 303-307, 309-310\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1992-04-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0883-2897(92)90115-F\",\"citationCount\":\"1\",\"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/088328979290115F\",\"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/088328979290115F","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Technetium-99m p-iodophenethyldiaminodithiol (DADT-IPE): Potential brain perfusion imaging agent for SPECT
A new ligand, an N-p-iodophenethyl diaminodithiol (DADT-IPE), an anlog of N-isopropyl-p-iodoamphetamine (IMP), was synthesized and subsequently complexed with 99mTc, using stannous chloride as a reducing agent. Two complexes (a and b) were separated from 99mTc-DADT-IPE by high performance liquid chromatography (HPLC). Competitive inhibition studies showed that the IC50 value of DADT-IPE (70 μM) was similar to that of IMP (49 μM). Biodistribution studies of one of the complexes [99mTc-DADT-IPE(a)] in rats showed that 0.65% of the injected dose of the tracer remained in the brain at 5 min after intravenous injection, with 0.53% of the dose remaining in the brain at 60 min post-injection, whereas the corresponding values for the other complex [99mTc-DADT-IPE(b)] were 0.34% dose in the brain at 5 min and 0.28% dose in the brain at 60 min post-injection. The half-life for clearance of 99mTc-DADT-IPE(a) from rat brain was found to be more than 5 h. These results suggested that 99mTc-DADT-IPE(a) has characteristics which are suitable for cerebral perfusion imaging.