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多巴胺的直接放射性氟化:用于使用正电子发射断层扫描成像人体心脏交感神经支配的18F标记的6-氟多巴胺。

Direct radiofluorination of dopamine: 18F-labeled 6-fluorodopamine for imaging cardiac sympathetic innervation in humans using positron emission tomography.

作者信息

Chirakal R, Coates G, Firnau G, Schrobilgen G J, Nahmias C

机构信息

Department of Nuclear Medicine, Chedoke-Mcmaster Hospitals, Hamilton, Ontario, Canada.

出版信息

Nucl Med Biol. 1996 Jan;23(1):41-5. doi: 10.1016/0969-8051(95)00213-8.

DOI:10.1016/0969-8051(95)00213-8
PMID:9004913
Abstract

Fluorine-18 labeled fluorodopamine (FDA) was synthesized by the direct fluorination with [18F]F2 [produced by the nuclear reaction 18O(p,n)18F] of dopamine in anhydrous hydrogen fluoride containing boron trifluoride at -65 degrees C. Reverse-phase high-performance liquid chromatography (HPLC) was used to separate [18F]6-FDA from the reaction mixture containing 18F-labeled 2- and 5-FDA. The radiochemical yield of [18F]6-FDA, with respect to [18F]F2, was 10 +/- 2% at the end of the 120-min synthesis from EOB1. The specific activity of [18F]6-FDA at the end of synthesis, 10 +/- 1.5 Ci/mmol, is sufficiently high that the amount of 6-FDA associated with the infusion of a dose of 5 mCi of [18F]6-FDA over 3 min into a 50-kg human (0.5-0.7 microgram/kg/min) is considerably lower than therapeutic doses (2-10 micrograms/kg/min) of dopamine.

摘要

氟-18标记的氟多巴胺(FDA)是通过在含有三氟化硼的无水氟化氢中,于-65℃下用[18F]F2(由核反应18O(p,n)18F产生)对多巴胺进行直接氟化反应合成的。采用反相高效液相色谱法(HPLC)从含有18F标记的2-氟多巴胺和5-氟多巴胺的反应混合物中分离出[18F]6-氟多巴胺。从EOB1开始进行120分钟的合成后,相对于[18F]F2,[18F]6-氟多巴胺的放射化学产率为10±2%。合成结束时,[18F]6-氟多巴胺的比活度为10±1.5 Ci/mmol,该比活度足够高,以至于在3分钟内将5 mCi的[18F]6-氟多巴胺注入一名50千克的人体(0.5 - 0.7微克/千克/分钟)时,所注入的6-氟多巴胺的量远低于多巴胺的治疗剂量(2 - 10微克/千克/分钟)。

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