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采用同位素方法进行[18F] -氟马西尼的放射性合成。

Radiosynthesis of [18F]-flumazenil Using an Isotopic Approach.

作者信息

Thakur Riptee, Kumar Aishwarya, Joshi Raman Kumar, Kumar Pardeep

机构信息

Department of Neuroimaging and Interventional Radiology, National Institute of Mental Health and Neurosciences, Bengaluru, Karnataka, India.

出版信息

Indian J Nucl Med. 2024 Jul-Aug;39(4):286-291. doi: 10.4103/ijnm.ijnm_82_24. Epub 2024 Nov 18.

DOI:10.4103/ijnm.ijnm_82_24
PMID:39790826
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11708791/
Abstract

BACKGROUND

Fluorine-18 (F) flumazenil (FMZ) has been synthesized using various precursors, and its role has been explored in imaging Gamma-aminobutyric acid-A receptors.

AIM AND OBJECTIVE

The main objective was to synthesize (F) FMZ using isotopic substitution.

MATERIALS AND METHODS

Around 18 ± 2 GBq was added to the module, dried, and radiolabeling was standardized with 3.0 mg of the FMZ precursor at various temperatures (110°C -160°C) for 10-30 min. The product was finally eluted with 20% ethanol (in phosphate buffer). The final product was characterized by high-performance liquid chromatography (HPLC). The stability was evaluated in water, saline, and phosphate-buffered saline for 4 h.

RESULTS

The radiolabelling efficiency of cartridge-based purification was 16 ± 4% ( = 10) with a radiochemical purity of 96.5 ± 1.8%, whereas in HPLC-based purification, the yield was 10 ± 4% ( = 5) with a radiochemical purity of 97.3 ± 1.4%. The specific activity was 120 ± 20 GBq/μmol.

CONCLUSIONS

(F) FMZ was successfully synthesized using an isotopic approach and could be used as an alternative cheaper option for the synthesis.

摘要

背景

已使用多种前体合成了氟-18（F）氟马西尼（FMZ），并已探索其在γ-氨基丁酸-A受体成像中的作用。

目的

主要目的是通过同位素取代合成（F）FMZ。

材料与方法

向模块中加入约18±2GBq，干燥后，在不同温度（110°C - 160°C）下用3.0mg FMZ前体进行10 - 30分钟的放射性标记标准化。最终产物用20%乙醇（磷酸盐缓冲液中）洗脱。最终产物通过高效液相色谱（HPLC）进行表征。在水、盐水和磷酸盐缓冲盐水中评估其4小时的稳定性。

结果

基于柱盒的纯化放射性标记效率为16±4%（n = 10），放射化学纯度为96.5±1.8%，而基于HPLC的纯化产率为10±4%（n = 5），放射化学纯度为97.3±1.4%。比活度为120±20GBq/μmol。

结论

采用同位素方法成功合成了（F）FMZ，可作为一种更便宜的合成替代选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/c3479021d0f4/IJNM-39-286-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/870a791a4184/IJNM-39-286-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/d75ada15d2db/IJNM-39-286-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/20d4caf9b734/IJNM-39-286-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/b756aaef4c51/IJNM-39-286-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/c3479021d0f4/IJNM-39-286-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/870a791a4184/IJNM-39-286-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/d75ada15d2db/IJNM-39-286-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/20d4caf9b734/IJNM-39-286-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/b756aaef4c51/IJNM-39-286-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0df/11708791/c3479021d0f4/IJNM-39-286-g005.jpg

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本文引用的文献

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