新型硒-75标记的放射性药物：多巴胺的硒鎓类似物。

New selenium-75 labeled radiopharmaceuticals: selenonium analogues of dopamine.

作者信息

Sadek S A, Basmadjian G P, Hsu P M, Rieger J A

出版信息

J Med Chem. 1983 Jul;26(7):947-50. doi: 10.1021/jm00361a003.

Abstract

Selenium-75 labeled selenonium analogues of dopamine, [2-(3,4-dimethoxyphenyl)ethyl]dimethylselenonium iodide (4) and its dihydroxy analogue (7), were prepared by reducing [75Se]selenious acid with sodium borohydride at pH 6.0 and reacting the NaSeH produced with 1-(3,4-dimethoxyphenyl)-2-(p-toluenesulfonyloxy)ethane. Tissue distribution studies in rats given the 75Se-labeled selenonium agents intravenously demonstrated high initial heart uptake (2.38% dose/g at 5 min). Prolonged adrenal retention (t1/2 = 10 h) and high adrenal to blood ratio of compound 4 (21/1 at 4 h after injection) were observed. The high uptake and adrenal to blood ratio suggest the potential use of compound 4 as a radiopharmaceutical for the adrenal gland.

摘要

用硼氢化钠在pH 6.0条件下还原亚硒酸[75Se]，并使生成的NaSeH与1-(3,4-二甲氧基苯基)-2-(对甲苯磺酰氧基)乙烷反应，制备了多巴胺的硒-75标记的硒鎓类似物，即[2-(3,4-二甲氧基苯基)乙基]二甲基碘化硒鎓(4)及其二羟基类似物(7)。对静脉注射75Se标记的硒鎓试剂的大鼠进行的组织分布研究表明，心脏在注射初期摄取量较高(5分钟时为2.38%剂量/克)。观察到化合物4在肾上腺中长时间滞留(t1/2 = 10小时)，且肾上腺与血液的比值较高(注射后4小时为21/1)。高摄取量和肾上腺与血液的比值表明化合物4有潜力用作肾上腺的放射性药物。