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一种新型脑灌注显像剂^(99m)TcN-CPDTC的制备及生物分布 被引量:8

Preparation and Biodistribution of the ~ (99m)TcN-CPDTC Complex as a New Potential Brain Perfusion Imaging Agent
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摘要 The complex 99m TcN CPDTC(CPDTC: N cyclopropyl dithiocarbamate trihydrate) is synthesized through ligand exchange reaction. The two step procedure involves the initial reaction of 99m TcO - 4 with succinic dihydrazide(SDH) as a donor of nitrido ligand(N 3- ) in the presence of stannous chloride dihydrate as reducing agent and propylenediamine tetraacetic acid(PDTA) as complex agent, followed by the addition of sodium N cyclopropyl dithiocarbamate trihydrate. The radiochemical purity(RCP) of the product is over 90% as measured by thin layer chromatography(TLC). It is stable over 6 h at room temperature. Its partition coefficient indicates it is a good lipophilic complex. The biodistribution results in mice indicate that 99m TcN CPDTC is significantly retained into the brain. The brain uptake(%, ID/g) is 4.64, 3 54 and 2.59 and the brain/blood ratio is 1.08, 1.27 and 1.28 at 5, 30 and 60 min post injection respectively. These results suggest potential usefulness of the complex as a brain perfusion imaging agent. The complex 99m TcN CPDTC(CPDTC: N cyclopropyl dithiocarbamate trihydrate) is synthesized through ligand exchange reaction. The two step procedure involves the initial reaction of 99m TcO - 4 with succinic dihydrazide(SDH) as a donor of nitrido ligand(N 3- ) in the presence of stannous chloride dihydrate as reducing agent and propylenediamine tetraacetic acid(PDTA) as complex agent, followed by the addition of sodium N cyclopropyl dithiocarbamate trihydrate. The radiochemical purity(RCP) of the product is over 90% as measured by thin layer chromatography(TLC). It is stable over 6 h at room temperature. Its partition coefficient indicates it is a good lipophilic complex. The biodistribution results in mice indicate that 99m TcN CPDTC is significantly retained into the brain. The brain uptake(%, ID/g) is 4.64, 3 54 and 2.59 and the brain/blood ratio is 1.08, 1.27 and 1.28 at 5, 30 and 60 min post injection respectively. These results suggest potential usefulness of the complex as a brain perfusion imaging agent.
出处 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 2001年第7期1095-1097,共3页 Chemical Journal of Chinese Universities
基金 北京市科委重点基金 (批准号 :95 330 430 0 )
关键词 锝-99m 锝氮配合物 放射性药物 生物分布 脑灌注显像剂 放射性标记物 Technetium 99m Technetium nitrido complex Radiopharmaceutical Biodistribution
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  • 1张俊波 王学斌 等.-[J].北京师范大学学报:自然科学版,1996,32(4):529-533.
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  • 4张俊波,北京师范大学学报,1996年,32卷,4期,529页
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