Efficient gallium-68 radiolabeling reaction of DOTA derivatives using a resonant-type microwave reactor
Efficient gallium-68 radiolabeling reaction of DOTA derivatives using a resonant-type microwave reactor
复制标题
使用谐振型微波反应器对 DOTA 衍生物进行高效镓 68 放射性标记反应
DOI：
10.1002/jlcr.3704
复制
发表时间：
2019
影响因子：
1.8
通讯作者：
Kimura Hiroyuki
中科院分区：
文献类型：
--
作者：
Yagi Yusuke;Shimizu Yoichi;Arimitsu Kenji;Nakamoto Yuji;Higuchi Takahiro;Togashi Kaori;Kimura Hiroyuki
镓-68（68 Ga，t1/2= 68 min）可以很容易地从68 Ge/68 Ga发生器中获得，并且几个这样的系统是商业上可获得的。使用68 Ga标记的放射性药物的正电子发射断层扫描（PET）成像的使用预计将在临床前和临床环境中增加。然而，a68 Ga阳离子与用于标记生物活性物质的双官能大环螯合物（例如1，4，7，10-四氮杂环十二烷-1，4，7，10-四乙酸（DOTA））之间的螯合需要相对长的反应时间和高温以实现高放射化学产率。在此之前，我们报道了一种新型的谐振型微波反应器，可用于放射性合成和该反应器在PET放射性合成18F中的有用性。在本研究中，这种谐振型微波反应器的有用性进行了评估的放射性标记的模型大环螯合物与68 Ga。结果，与使用常规加热方法相比，谐振型微波反应器的微波加热在2分钟的短时间内显著提高了68 Ga标记螯合反应的速率。此外，发现使用该反应器使得可以减少反应中所需的前体的量并提高标记化合物的摩尔活性。
Gallium‐68 (68Ga, t1/2= 68 min) can be easily obtained from a68Ge/68Ga generator, and several such systems are commercially available. The use of positron emission tomography (PET) imaging using68Ga‐labeled radiopharmaceuticals is expected to increase in both preclinical and clinical settings. However, the chelation between a68Ga cation and the bifunctional macrocyclic chelates that are used for labeling bioactive substances, such as 1,4,7,10‐tetraazacyclododecane‐1,4,7,10‐tetraacetic acid (DOTA), requires a relatively long reaction time and high temperature to achieve a high radiochemical yield. Previously, we reported on a novel resonant‐type microwave reactor that can be used for radiosynthesis and the usefulness of this reactor in the PET radiosynthesis of18F. In the present study, the usefulness of this resonant‐type microwave reactor was evaluated for the radiolabeling of model macrocyclic chelates with68Ga. As a result, microwave heating of resonant‐type microwave reactor notably improved the rate of the68Ga labeling chelate reaction in a short time period of 2 minutes, compared with the use of a conventional heating method. Additionally, it was found that the use of this reactor made it possible to decrease the amount of precursors required in the reaction and to improve the molar activity of the labeled compounds.