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

K. Shiba , H. Mori , H. Matsuda , K. Hisada
{"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 ,&nbsp;H. Mori ,&nbsp;H. Matsuda ,&nbsp;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 ,&nbsp;H. Mori ,&nbsp;H. Matsuda ,&nbsp;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}
引用次数: 1

摘要

合成了n -异丙基-对碘安非他明(IMP)类似物n -对碘苯乙二氨基二硫醇(DADT-IPE),并以氯化亚锡为还原剂与99mTc络合。用高效液相色谱法从99mTc-DADT-IPE中分离出两个配合物a和b。竞争抑制实验表明,DADT-IPE (70 μM)的IC50值与IMP (49 μM)相似。Biodistribution研究之一的复合物[99 mtc-dadt-ipe (a)]的老鼠显示0.65%的大脑中示踪剂的注入剂量仍在静脉注射后5分钟,剩下0.53%的剂量在60分钟post-injection大脑,而相应的值对于其他复杂[99 mtc-dadt-ipe (b)] 0.34%剂量在大脑中5分钟和0.28%剂量在60分钟post-injection大脑。99mTc-DADT-IPE(a)在大鼠脑内的清除半衰期大于5 h,表明99mTc-DADT-IPE(a)具有适合脑灌注成像的特性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
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.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
期刊最新文献
Evaluation of a DMSA kit for instant preparation of 99mTc(V)—DMSA for tumour and metastasis scintigraphy Pharmacokinetics of the SPECT benzodiazepine receptor radioligand [123I]iomazenil in human and non-human primates Quantification of in vivo binding of [3H]RX 821002 in rat brain: Evaluation as a radioligand for central α2-adrenoceptors A bifunctional HBED-derivative for labeling of antibodies with 67Ga, 111In and 59Fe. Comparative biodistribution with 111In-DPTA and 131I-labeled antibodies in mice bearing antibody internalizing and non-internalizing tumors Attachment of 99mTc to lipid vesicles containing the lipophilic chelate dipalmitoylphosphatidylethanolamine-DTTA
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1