18F-MFBG的自动化合成及其在健康比格犬中的心脏交感神经显像与体内分布的实验研究

Experimental study on the automated synthesis of 18F-MFBG and its cardiac sympathetic nerve imaging and in vivo distribution in healthy beagle dogs

  • 摘要:
    目的 探讨18F-间氟苄胍(MFBG)的自动化合成及其在健康比格犬心脏交感神经显像中的应用,以及其在体内的分布情况。
    方法 利用正电子药物合成模块建立18F-MFBG自动化合成方法。采用自身对照设计研究,使用健康比格犬3只,其中公犬2只、母犬1只,年龄13~15个月,体重约15 kg。18F-MFBG体内分布研究采用PET/CT全身动态显像,观察实验犬体内各主要脏器18F-MFBG分布随时间变化的特点,以及左室心肌与心血池、肝脏、肺、脾脏、肾脏的放射性计数比值随时间的变化,明确心脏最优显像时间。
    结果 连续5次成功自动化合成18F-MFBG,用时为(75±11) min,合成产率为(18.2±2.6)%。实验犬18F-MFBG心肌显影清晰,图像质量评分均为优秀(4分),各节段心肌显像剂分布均匀,心腔内放射性计数低,无心外放射性干扰。18F-MFBG注射后10 min左室心肌可清晰显像,并在2 h内始终保持高放射性摄取;60 min时左室心肌与肺的放射性计数比值的均数最大,为7.31,90 min时左室心肌与心血池的放射性计数比值的均数最大,为12.93。实验犬心脏显像最优时间为注射18F-MFBG后60~90 min。
    结论 实现了18F-MFBG的自动化合成。18F-MFBG在实验犬心脏交感神经显像中示图像清晰,心外无明显放射性干扰,是一种具有潜在应用前景的正电子心脏交感神经显像剂。

     

    Abstract:
    Objective To investigate the automated synthesis of 18F-meta-fluorobenzylguanidine (MFBG) and its application in cardiac sympathetic nerve imaging in healthy beagle dogs, and the in vivo distribution of this imaging agent.
    Methods The automated synthesis method was established using a positron-emitting drug synthesis module. A self-controlled design was adopted. Three healthy beagle dogs, 2 males and 1 female, aged 13−15 months and weighing approximately 15 kg, were used. In the 18F-MFBG in vivo distribution study, dynamic whole-body PET/CT imaging was performed on experimental dogs to observe the characteristics of the distribution of 18F-MFBG in major organs over time, as well as the changes in the radioactive count ratios of the left ventricular myocardium to the blood pool, liver, lungs, spleen, and kidneys over time, in order to determine the optimal cardiac imaging time.
    Results 18F-MFBG was successfully synthesized automatically in five consecutive runs, with the synthesis time of (75±11) min and the synthesis yield of (18.2±2.6) %. In the experimental dogs, 18F-MFBG provided clear myocardial imaging, with an image quality score of excellent (4 points). The imaging agent was distributed uniformly across myocardial segments, exhibiting low radioactive counts in the cardiac chambers and no extracardiac radioactive interference. The left ventricular myocardium was clearly visualized as early as 10 min post-injection and maintained high radioactive uptake for 2 h. At 60 min, the maximum mean value of the radioactive count ratio of the left ventricular myocardium to the lungs was 7.31. At 90 min, the maximum mean value of the radioactive count ratio of the left ventricular myocardium to the blood pool was 12.93. The optimal cardiac imaging time in experimental dogs was 60−90 min after injection.
    Conclusions The automated synthesis of 18F-MFBG was achieved. 18F-MFBG cardiac sympathetic nerve imaging in experimental dogs showed clear images, with no obvious extracardiac radioactive interference. Thus, it is a promising positron-emitting agent for cardiac sympathetic nerve imaging.

     

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