摘要目的：采用放射性核素99mTc直接标记Octreotide；评价甲状腺突眼患者临床受体影像。方法：标记是通过对半胱氨酸桥还原后提供的巯基与99mTc螯合后完成的。新华I号纸层析测定标记率，通过Sep pak C18柱层析、半胱氨酸置换实验、血清蛋白结合实验及体外稳定性实验对99mTc-OCT的放射化学性质进行评价，对甲状腺突眼患者进行SPECT与同机CT融合显像。结果：99mTc-OCT标记率为（95.8±0.55）%，标记物具有良好的放射化学性质，活动期甲状腺突眼患者融合图像清晰，病灶放射性浓聚明显。结论：99mTc直接法标记OCT方法简便，标记率高（>95％），体内外稳定性好；99mTc-Octreotide是一种极具前景的生长抑素受体显像剂。
Abstract：Objective: Octreotide was labeled with 99mTc, to analyse radiochemical characters of 99mTc-Octreotide and investigate the clinical receptor imaging in patient with Graves’ ophthalmopathy(GO). Methods: Labeling was accomplished by reduction of the cysteine bridge, which provided sulfhydryl groups for chelation with 99mTc. The labeling rate was determined with Xinhua I chromatography. The radiochemical property of 99mTc-OCT were evaluated by Sep pak Cl8 chromatography, the cysteine challenge experiment, the serum incubation test and the stability experiment in vitro and the clinical procedures of receptor fusion imaging were carried out in patient with GO. Results: The labeling rate of 99mTc-OCT was (95.8±0.55)％, the99mTc-OCT compound has excellent radiochemical characters. SRS showed markedly increased orbital uptake of 99mTc-OCT in patient with active GO. Conclusion: 99mTc-OCT can be readily prepared, the labeling yields are quite high(>95％), and stability in vivo(vitro); 99mTc-OCT is a promising radiopharmaceutical for somatostatin receptor scintigraphic imaging.
赵 荣;汪 静;邓敬兰;王 江. 99mTc直接法标记Octreotide及其在甲状腺突眼患者的临床初步应用研究[J]. , 2007, 18(8): 533-536.
ZHAO Rong;WANG Jing;DENG Jing-lan;WANG Jiang. Direct labeling of Octreotide with 99mTc and clinical study in patients with Graves’ ophthalmopathy. , 2007, 18(8): 533-536.
2007, Vol. 18 
