Symmetry-guided design and fluorous synthesis of a stable and rapidly excreted imaging tracer for (19)F MRI.
Symmetry-guided design and fluorous synthesis of a stable and rapidly excreted imaging tracer for (19)F MRI.
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DOI：
10.1002/anie.200901005
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发表时间：
2009
影响因子：
16.6
通讯作者：
Yu, Yihua Bruce
中科院分区：
文献类型：
--
作者：
Jiang, Zhong-Xing;Liu, Xin;Jeong, Eun-Kee;Yu, Yihua Bruce
1H和19 F是核磁共振成像（MRI）最敏感的核，1H信号适合收集有关身体的信息[1，2]，19 F信号适合收集有关体内药物的信息。[3，4]虽然19 F MRI [5]只比1H MRI年轻4年[6]，但它并没有在临床上使用。由于缺乏合适的显像剂，19 F MRI的进展一直停滞不前。目前的19 F显像剂是全氟化碳（PFC）乳剂[7-13]，并且具有严重的缺点，包括异质性、不稳定性、分裂的19 F信号、复杂的配制程序，以及最重要的是，试剂在器官内过度保留数月或更长时间。[8，14]我们开发了一种双球形碳氟化合物分子，表示为19 FIT以代表19 F成像示踪剂，其克服了基于PFC的成像剂的所有主要缺陷。19 FIT是利用模块化球对称原理设计的，是水溶性的，并从27个氟原子发射单个19 F信号。19 FIT在小鼠体内的滞留半衰期约为0.5天，没有发现器官滞留或体内降解的证据，表明模块对称性是设计具有多功能性分子的有效策略。有了合适的显像剂，如19 FIT，19 F MRI有可能在药物治疗中发挥重要作用，类似于1H MRI在疾病诊断中发挥的作用。
1H and 19F are the most sensitive nuclei for nuclear magnetic resonance imaging (MRI), with the 1H signal suited for collecting information about the body [1, 2] and the 19F signal suited for collecting information about drugs in the body.[3, 4] Although 19F MRI [5] is only four years younger than 1H MRI,[6] it is not in clinical use. The progress of 19F MRI has been stalled by the lack of suitable imaging agents. Current 19F imaging agents are perfluorocarbon (PFC) emulsions [7–13] and suffer severe shortcomings, including heterogeneity, instability, split 19Fsignals, complex formulation procedure and, most importantly, excessive retention of the agent within organs for months or longer.[8, 14] We developed a bispherical fluorocarbon molecule, denoted as 19FIT to stand for 19F imaging tracer, which overcame all the major deficiencies of PFC-based imaging agents. 19FIT, designed using the principle of modular spherical symmetry, is water soluble and emits a single 19F signal from 27 fluorine atoms. The in vivo residence half-life of 19FIT measured in mice is about 0.5 day, and no evidence of organ retention or in vivo degradation was found. Our result shows that modular symmetry is a useful strategy for designing molecules with multiple functionalities. With suitable imaging agents like 19FIT, 19F MRI has the potential to play an important role in drug therapy, analogous to the role played by 1H MRI in disease diagnosis.
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影响因子：
2.6
作者：
Jiang, Zhong-Xing;Yu, Y. Bruce
通讯作者：
Yu, Y. Bruce
DOI：
10.1002/jmri.1880040416
发表时间：
1994-07-01
期刊：
JMRI-JOURNAL OF MAGNETIC RESONANCE IMAGING
影响因子：
--
作者：
LEE, H;PRICE, RR;CACHERIS, WP
通讯作者：
CACHERIS, WP
影响因子：
46.9
作者：
Ahrens, ET;Flores, R;Morel, PA
通讯作者：
Morel, PA
影响因子：
3.9
作者：
Tomalia, D. A.;Reyna, L. A.;Svenson, S.
通讯作者：
Svenson, S.
影响因子：
6.7
作者：
MEYER, KL;CARVLIN, MJ;JOSEPH, PM
通讯作者：
JOSEPH, PM