新型炎症显像剂的初步研究

A PRELIMINARY STUDY OF NEW IMAGING AGENTS ON INFLAMMATION LESIONS

对柠檬酸 (Cit)、酒石酸 (Tar)、DL 苹果酸 (DL Mal)、L 苹果酸 (L Mal)和D 葡萄糖二酸 (D Gca)等 5种含有羟基和羧基的小分子化合物的99mTc标记条件以及亲炎症的生物性能进行了初步研究 .根据它们的最佳标记条件 ,分别对其进行标记 .标记率均大于 90 % .这 5种配合物和99mTcO- 4(P)在松节油致炎小鼠中的生物分布结果表明 :炎症模型脓肿与肌肉的质量活度分数之比值 (am(A) /am(M) )分别达 4 .0 2± 0 .2 1(Cit,3h) ,3.2 0± 0 .17(Tar,1h) ,4 .0 4± 0 .2 1(DL Mal,6h) ,3.50± 0 .2 3(L Mal,1h) ,4 .30± 0 .77(D Gca ,3h)和 3.2 3± 0 .4 1(P ,1h) .对99mTc D Gca在松节油致炎家兔中的生物分布进行了静态显像 ,结果较好 .据此可认为99mTc标记的 5种配合物和99mTcO- 4均有亲炎症组织的生物性质 ,其中 ,99mTc Cit国外已用于临床 ,而99mTc D Gca很可能是一种潜在的炎症显像剂 ,值得进一步研究 .

Labelling conditions with 99m Tc and biobehavior of five small molecular compounds that have hydroxyl and carboxyl groups in structure are preliminarily studied. The labelling yields of citric acid (Cit), tartaric acid (Tar), DL malic acid ( DL Mal), L malic acid ( L Mal) and D glucaric acid ( D Gca) are all more than 90 % according to the best conditions. The biodistributions of them and 99m TcO - 4 (P) are studied in mice with turpentine induced abscesses at 1,3 and 6h after 99m Tc labelled compounds i.v.injection. The results demonstrate that the maximum a m (A)/a m (M) ratios are 4.02±0.21(Cit,3 h), 3.20± 0.17 (Tar,1 h), 4.04±0.21( DL Mal,6 h), 3.50±0.23( L Mal,1 h), 4.30±0.77( D Gca, 3 h ) and 3.23±0.41(P,1 h)respectively. Therefore, they all have the biobehavior accumulating in inflammation lesions. Of them, 99m Tc Cit is used in clinic abroad, 99m Tc D Gca is probably a potential imaging agent on inflammation lesions and further study is needed.