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1. 中国科学院上海应用物理研究所放射性药物研究中心
2. 中国科学院上海应用物理研究所放射性药物研究中心,上海,201800
纸质出版日期:2006-05-01
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[1]李谷才,尹端沚,程登峰,王明伟,郑明强,汪勇先.3-(4-[~(18)F]氟苄基)-8-羟基-1,2,3,4-四氢苯并吡喃[3,4-c]吡啶-5-酮的放射化学合成[J].核技术,2006(05):368-371.
LI Gucai YIN Duanzhi CHENG Dengfeng WANG Mingwei ZHENG Mingqiang WANG Yongxian. Synthesis of 3-(4-[18F] fluorobenzyl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one[J]. Nuclear techniques, 2006, (5): 368-371.
[1]李谷才,尹端沚,程登峰,王明伟,郑明强,汪勇先.3-(4-[~(18)F]氟苄基)-8-羟基-1,2,3,4-四氢苯并吡喃[3,4-c]吡啶-5-酮的放射化学合成[J].核技术,2006(05):368-371. DOI:
LI Gucai YIN Duanzhi CHENG Dengfeng WANG Mingwei ZHENG Mingqiang WANG Yongxian. Synthesis of 3-(4-[18F] fluorobenzyl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one[J]. Nuclear techniques, 2006, (5): 368-371. DOI:
多巴胺D4受体是一种G蛋白偶联受体
在精神分裂症病因发展中起着重要作用。通过核医学显像仪器
利用PET显像剂可以确定受体在活体内的分布、含量变化等。本文用三氟甲基磺酸-4-三甲基铵苯甲醛作标记前体
采用“一锅法”制备了一种潜在的多巴胺D4受体PET显像剂3-(4-[18F]氟苄基)-8-羟基-1
2
3
4-四氢苯并吡喃[3
4-c]吡啶-5-酮(18F-FHTP)。其总的合成时间为105min
放射化学产率为19.7%
比活度大于120GBq/μmol。
Dopamine D4 receptor is a G-protein coupled receptor and it is hypothesized to relate with the patho- physiology and pharmacotherapy of schizophrenia while its level in brain regions is much lower. With the help of nu- clear medicine imaging technology and suitable imaging agents
the receptors’ distribution and the level variation can be determined in living bodies. In this article we describe the synthesis of a putative dopamine D4 receptor radioli- gand
3-(4-[18F]fluorobenzyl)-8-hydroxy-1
2
3
4-tetrahydrochromeno[3
4-c] pyridin–5-one (18F-FHTP) from 4-trimethylammoniumbenzaldehyde triflate through a two-steps one-pot procedure with a total radiochemical yield of 19.7% (decay-corrected). The radiochemical synthesis of 18F-FHTP took about 105 min and its specific activity was greater than 120GBq / μmol.
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