摘要
目的：建立99Tcm标记HYNIC-Octreotide的最佳方法，评价该显像剂用于临床的可能性。方法： 以SnCl2为还原剂，按间接法标记99Tcm-HYNIC-Octreotide。观察标记物的体内、体外稳定性。对6只实验用大耳白兔、3名健康志愿者及3名后来经病理证实的脑膜瘤患者初步进行了生长抑素受体显像。结果： 99Tcm-HYNIC-Octreotide的标记率为97.8%±0.55%。99Tcm-HYNIC-Octreotide的体内、体外稳定性：①静置稳定性：静置4h标记率仍达90%以上。②半胱氨酸置换试验：游离99Tcm随半胱氨酸的增加而缓慢上升，当半胱氨酸达200mmol/L时，99Tcm-HYNIC-Octreotide分子中约23%的99Tcm的被置换出。③血清结合试验：24h 99Tcm-HYNIC-Octreotide与蛋白结合率为17.04%±0.01%。99Tcm-HYNIC-Octreotide显像结果：①正常兔及正常人99Tcm-HYNIC-Octreotide体内分布特点：膀胱和肾脏最浓，其次是肝脏，鼻黏膜轻度浓聚，颅脑、双肺、肠道内未见明显核素浓聚。②3名脑膜瘤患者放射性核素明显浓聚，注射显像剂4h后肿瘤放射性计数与本底放射性计数的比值（T/NT）为5.36。结论：99Tcm标记HYNIC-Octreotide方法可行，标记率和放化纯高，稳定性好。初步临床显像证明99Tcm-HYNIC-Octreotide是一种具有潜力的诊断脑膜瘤的生长抑素受体显像剂。
Abstract
Objective: To develop a method to label HYNIC-Octreotide with 99Tcm indirectly and evaluate its potential as a clinical imaging agent. Methods: SnCl2 as a reducing agent was adopted to label HYNIC-Octreotide with 99Tcm indirectly, to observe the stability of the labeled drugs; 6 rabbits, 3 healthy volunteers and 3 patients with meningioma were examined by this somatostatin receptor agent. Results: The label rate of 99Tcm-HYNIC-Octreotide was 97.8%±0.55%. The stability of the labeled drugs: ①The stability after 4 hours were above 90%. ②The replace test of cysteine: with the increase of cysteine, free 99Tcm was found to raise slowly, about 23% free 99Tcm was break away from 99Tcm-HYNIC-Octreotide when the concentration of cysteine was up to 200mmol/L. ③Plasma binding: the rate of 99Tcm-HYNIC-Octreotide combined with plasma is 17.04%±0.01% for 24 hours. ①Character of distribution with the radionuclide drug in rabbits and volunteers: Intense uptake was found in bladder and kidney, moderate uptake in liver, mild uptake in mucous membrane of nose, no obvious uptake in brain, lung and intestinal tract. ②Intense uptake was found in 3 patients with meningioma, the average value of T/NT was 5.36 after 4 hours. Conclusions: This method to label HYNIC-Octreotide with 99Tcm is promising; it has a high label rate and stability. 99Tcm-HYNIC-Octreotide has a potential as an agent imaging to meningioma.
关键词
脑膜瘤 /
放射性核素显像
Key words
Meningioma /
Radionuclide imaging
王胜军;汪 静;邓敬兰;曾 瑾;王喜青;王云雅;梁晓燕.
99Tcｍ-HYNIC-Octreotide的标记及其在脑膜瘤诊断中的初步应用[J]. 中国临床医学影像杂志. 2008, 19(8): 551-554
WANG Sheng-jun;WANG Jing;DENG Jing-lan;ZENG Jin;WANG Xi-qing;WANG Yun-ya;LIANG Xiao-yan.
Preliminary clinical application of HYNIC-Octreotide labeled with 99Tcm in the diagnosis of meningioma[J]. Journal of China Clinic Medical Imaging. 2008, 19(8): 551-554
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