碘标记阿片受体单光子发射计算机断层显像剂的制备  

Preparation of Radioiodinated 7α-O-IA-DPN as an Single Photon Emission Computed Tomographic Imaging Agent for Mapping Opioid Receptors

作　　者：王荣福[1] 何晓坤[1] 张春丽[1] 霍力[1] 

机构地区：[1]北京大学第一医院核医学科,北京100034

出　　处：《核化学与放射化学》2004年第2期71-76,共6页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金资助项目(39870241)

摘　　要：研制了一种适合单光子发射计算机断层(SPECT)显像用的阿片受体配基碘烷特培洛菲(7α O IA DPN),合成了阿片受体显像剂125I 7α O IA DPN,并检测了标记物的体外稳定性,进行了体内外结合实验研究。研制结果为:碘标记的7α O IA DPN放化纯度大于95%,标记率为81%～90%,比活度高达83.25PBq/mol,室温下放置24h,放化纯度仍大于90%。体外结合实验结果显示,其Kd=0.23nmol/L,Bmax为38pmol/g。研究结果表明,碘标记的7α O IA DPN有望成为SPECT的阿片受体显像剂。The radioiodinated 7α-O-iodoallyl diprenorphine (7α-O-IA-DPN) as a new opioid receptor imaging agent for SPECT study is developed. The design and radiochemical synthesis of 7α-O-IA-DPN labeled with iodine-125 are performed. In vitro and in vivo opioid receptor binding assays, and in vitro stability are studied, respectively. The radiochemical purity of radioiodinated 7α-O-IA-DPN is more than 95%, and still greater than 90% kept for 24 h at room temperature. Radiochemical yields is 81%～90%, and specific radioactivity is 83.25 PBq/mol. The binding assay in vitro shows a very high affinity(K_d=0.23 nmol/L) with B_(max) of 38 pmol/g. The proposed compound of 7α-O-IA-DPN appears to be a potential opioid receptor imaging agent for SPECT study.

关 键 词：碘标记 阿片受体 单光子发射计算机断层显像 显像剂 制备 核医学 

分 类 号：R817[医药卫生—影像医学与核医学]