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新型心肌灌注示踪剂 123I-CMICE-013 在健康大鼠体内的生物分布和放射性剂量学研究。

Biodistribution and radiodosimetry of a novel myocardial perfusion tracer 123I-CMICE-013 in healthy rats.

机构信息

Nordion Inc, 447 March Road, Ottawa, ON K2K 1X8, Canada.

出版信息

EJNMMI Res. 2014 Mar 13;4(1):16. doi: 10.1186/2191-219X-4-16.

DOI:10.1186/2191-219X-4-16
PMID:24620906
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3995622/
Abstract

BACKGROUND

123I-CMICE-013 is a novel radiotracer previously reported to have promising characteristics for single-photon emission computed tomography (SPECT) myocardial perfusion imaging. We evaluated the biokinetics and radiodosimetry of this rotenone-like 123I-labeled tracer in a microSPECT imaging-based study.

METHODS

37 to 111 MBq of 123I-CMICE-013 was synthesized and administered intravenously to 14 healthy rats. Images were acquired with a microSPECT/CT camera at various time intervals and reconstructed to allow activity quantification in the tissues of interest. Radiation dosage resulted from the injection of 123I-CMICE-013 was estimated base on the biodistribution data. Tissue uptake values from image analysis were verified by gamma-counting dissected organs ex vivo.

RESULTS

The heart/stomach and heart/intestine uptake ratios peaked shortly after the injection of 123I-CMICE-013, meanwhile the heart/liver ratio reached 2 as early as at 23 min post-injection. Little activity was observed in the lung and overnight clearance was significant in most of the measured tissues. The radiation dosimetry analysis based on the time-activity curves provided an estimate of the effective human dose of 6.99E-03 mSv/MBq using ICRP 60 and 7.15E-03 mSv/MBq using ICRP 103, which is comparable to the popular myocardium perfusion imaging (MPI) agents such as 99mTc-tetrofosmin and 99mTc-sestamibi, as well as other 123I-based radiotracers.

CONCLUSIONS

123I-CMICE-013 demonstrated desirable characteristics in its biokinetic and radiodosimetric profiles, supporting its potential application as a novel myocardial perfusion imaging agent.

摘要

背景

123I-CMICE-013 是一种新型放射性示踪剂，先前报道其具有单光子发射计算机断层扫描（SPECT）心肌灌注成像的有前景的特性。我们在基于微 SPECT 成像的研究中评估了这种类似鱼藤酮的 123I 标记示踪剂的生物动力学和放射剂量学。

方法

将 37 至 111 MBq 的 123I-CMICE-013 合成并静脉内给予 14 只健康大鼠。使用微 SPECT/CT 相机在不同时间间隔采集图像，并进行重建以允许对感兴趣的组织中的活性进行定量。根据生物分布数据，基于注射 123I-CMICE-013 估算辐射剂量。通过对离体解剖器官的伽马计数验证图像分析得出的组织摄取值。

结果

在注射 123I-CMICE-013 后不久，心脏/胃和心脏/肠的摄取比达到峰值，而心脏/肝的比值早在注射后 23 分钟就达到 2。在肺中观察到很少的活性，并且大多数测量的组织在过夜清除方面非常显著。基于时间-活性曲线的放射剂量学分析提供了使用 ICRP 60 的 6.99E-03 毫希沃特/MBq 和使用 ICRP 103 的 7.15E-03 毫希沃特/MBq 的有效人体剂量的估计值，这与流行的心肌灌注成像（MPI）剂如 99mTc-甲氧基异丁基异腈和 99mTc-甲氧基乙基异腈以及其他 123I 基放射性示踪剂相当。

结论

123I-CMICE-013 在其生物动力学和放射剂量学特征方面表现出理想的特性，支持其作为新型心肌灌注成像剂的潜在应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd2c/3995622/a5788fd5c029/2191-219X-4-16-9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd2c/3995622/90aa3987ddd4/2191-219X-4-16-1.jpg
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