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18F-Labeled BODIPY Dye: A Potential Prosthetic Group for Brain Hybrid PET/Optical Imaging Agents
ACS Chemical Neuroscience ( IF 4.1 ) Pub Date : 2018-12-28 00:00:00 , DOI: 10.1021/acschemneuro.8b00480 Hyunjung Kim 1 , Kyul Kim 2 , Sang-Hyun Son 2 , Joon Young Choi 3 , Kyung-Han Lee 1, 3 , Byung-Tae Kim 3 , Youngjoo Byun 2 , Yearn Seong Choe 1, 3
ACS Chemical Neuroscience ( IF 4.1 ) Pub Date : 2018-12-28 00:00:00 , DOI: 10.1021/acschemneuro.8b00480 Hyunjung Kim 1 , Kyul Kim 2 , Sang-Hyun Son 2 , Joon Young Choi 3 , Kyung-Han Lee 1, 3 , Byung-Tae Kim 3 , Youngjoo Byun 2 , Yearn Seong Choe 1, 3
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There are few hybrid positron emission tomography (PET)/fluorescence imaging agents available for brain imaging. For this purpose, BODIPY dye is very attractive because one of its fluorine atoms can be readily exchanged with 18F, and it can be modified to produce red-shifted fluorescence. In this study, therefore, we synthesized and investigated a 18F-labeled red-shifted BODIPY dye as a prosthetic group for brain hybrid PET/optical imaging agents and determined the optimal dose of this radioligand for hybrid imaging. The red-shifted BODIPY dye (1) was synthesized, and one of its fluorine atoms was exchanged with 18F using SnCl4 in high yield. Partition coefficients of 18F-labeled BODIPY dye ([18F]1) and 1 were measured using its radioactivity and fluorescence, respectively, which were shown to be suitable for brain penetration. Optimal dose for hybrid imaging was determined by analysis of PET/CT and optical images of Balb/C nude mice injected with [18F]1 and 1, respectively. Hybrid PET/optical images of mice injected with optimal dose of [18F]1 showed strong radioactivity and fluorescence signal in the brain at 2 min after injection, with rapid clearance by 30 min. Tissue distribution data confirmed the in vivo and ex vivo PET/optical imaging data, indicating desirable brain pharmacokinetics of the radioligand. Taken together, the results of this study suggest that [18F]1 can be widely used as a prosthetic group for brain hybrid PET/optical imaging agents.
中文翻译：
18 F标签的BODIPY染料：脑杂合PET /光学成像剂的潜在修复基团
很少有可用于大脑成像的混合正电子发射断层扫描（PET）/荧光成像剂。为此，BODIPY染料非常吸引人，因为其氟原子之一可以很容易地与18 F交换，并且可以对其进行修饰以产生红移荧光。因此，在这项研究中，我们合成并研究了18 F标记的红移BODIPY染料作为大脑杂合PET /光学显像剂的修复基团，并确定了用于混合显像的这种放射性配体的最佳剂量。合成了红移的BODIPY染料（1），并使用SnCl 4以高收率将其氟原子之一与18 F交换。分配系数为18F标记的BODIPY染料（[ 18 F] 1）和1分别使用其放射性和荧光进行了测量，结果表明它们适合于脑部渗透。混合成像的最佳剂量是通过PET / CT分析和分别注射了[ 18 F] 1和1的Balb / C裸鼠的光学图像确定的。最佳剂量[ 18 F] 1注射的小鼠的混合PET /光学图像注射后2分钟在大脑中显示出强大的放射性和荧光信号，并在30分钟后迅速清除。组织分布数据证实了体内和离体PET /光学成像数据，表明放射性配体的理想脑药代动力学。两者合计，这项研究的结果表明[ 18 F] 1可以广泛用作大脑混合PET /光学成像剂的义肢。
更新日期：2018-12-28
中文翻译：
18 F标签的BODIPY染料：脑杂合PET /光学成像剂的潜在修复基团
很少有可用于大脑成像的混合正电子发射断层扫描（PET）/荧光成像剂。为此，BODIPY染料非常吸引人，因为其氟原子之一可以很容易地与18 F交换，并且可以对其进行修饰以产生红移荧光。因此，在这项研究中，我们合成并研究了18 F标记的红移BODIPY染料作为大脑杂合PET /光学显像剂的修复基团，并确定了用于混合显像的这种放射性配体的最佳剂量。合成了红移的BODIPY染料（1），并使用SnCl 4以高收率将其氟原子之一与18 F交换。分配系数为18F标记的BODIPY染料（[ 18 F] 1）和1分别使用其放射性和荧光进行了测量，结果表明它们适合于脑部渗透。混合成像的最佳剂量是通过PET / CT分析和分别注射了[ 18 F] 1和1的Balb / C裸鼠的光学图像确定的。最佳剂量[ 18 F] 1注射的小鼠的混合PET /光学图像注射后2分钟在大脑中显示出强大的放射性和荧光信号，并在30分钟后迅速清除。组织分布数据证实了体内和离体PET /光学成像数据，表明放射性配体的理想脑药代动力学。两者合计，这项研究的结果表明[ 18 F] 1可以广泛用作大脑混合PET /光学成像剂的义肢。
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