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取代2-氨基吡咯的99mTc标记亚氨基二乙酸衍生物作为肝胆显像剂的评价。I.

Evaluation of 99mTc-labeled iminodiacetic acid derivatives of substituted 2-aminopyrroles as hepatobiliary imaging agents. I.

作者信息

DeJuliis C M, Graham B W, Mattson R J, Sowell J W

出版信息

J Pharm Sci. 1980 Jun;69(6):731-2. doi: 10.1002/jps.2600690634.

Abstract

N-(3-Cyano-4,5-dimethyl-2-pyrrylcarbamoylmethyl)iminodiacetic acid (IIa) and N-(3-cyano-4-methyl-5-benzyl-2-pyrrylcarbamoylmethyl)iminodiacetic acid (IIb) were synthesized, labeled with technetium 99m, and compared with 99mTc-labeled p-isopropylacetanilidoiminodiacetic acid (I) for hepatobiliary activity in rats. All three compounds showed similar clearance of radioactivity from the blood. Comparison of the amount of radioactivity in various organs 1 hr after injection showed no significant difference between I and IIb. Compound IIa showed significantly less radioactivity in the GI tract and a higher amount in the kidneys and bladder.

摘要

合成了N-(3-氰基-4,5-二甲基-2-吡咯甲酰氨基甲基)亚氨基二乙酸(IIa)和N-(3-氰基-4-甲基-5-苄基-2-吡咯甲酰氨基甲基)亚氨基二乙酸(IIb),用锝99m进行标记,并与99mTc标记的对异丙基乙酰苯胺基亚氨基二乙酸(I)在大鼠体内的肝胆活性进行比较。所有三种化合物从血液中清除放射性的情况相似。注射后1小时各器官放射性量的比较显示,I和IIb之间无显著差异。化合物IIa在胃肠道中的放射性显著较低,而在肾脏和膀胱中的放射性较高。

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