دورية أكاديمية
Synthesis of a 2-nitroimidazole derivative N-(4-[18F]fluorobenzyl)-2-(2-nitro-1H-imidazol-1-yl)-acetamide ([18 F]FBNA) as PET radiotracer for imaging tumor hypoxia
| العنوان: | Synthesis of a 2-nitroimidazole derivative N-(4-[18F]fluorobenzyl)-2-(2-nitro-1H-imidazol-1-yl)-acetamide ([18 F]FBNA) as PET radiotracer for imaging tumor hypoxia |
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| المؤلفون: | Arian Pérez Nario, Jenilee Woodfield, Sofia Nascimento dos Santos, Cody Bergman, Melinda Wuest, Yasniel Babí Araújo, André Luis Lapolli, Frederick G. West, Frank Wuest, Emerson Soares Bernardes |
| المصدر: | EJNMMI Radiopharmacy and Chemistry, Vol 7, Iss 1, Pp 1-16 (2022) |
| بيانات النشر: | SpringerOpen, 2022. |
| سنة النشر: | 2022 |
| المجموعة: | LCC:Medical physics. Medical radiology. Nuclear medicine LCC:Therapeutics. Pharmacology |
| مصطلحات موضوعية: | N-(4-[18F]fluorobenzyl)-2-(2-nitro-1H-imidazol-1-yl)acetamide ([18F]FBNA), Hypoxia, Positron emission tomography (PET), Medical physics. Medical radiology. Nuclear medicine, R895-920, Therapeutics. Pharmacology, RM1-950 |
| الوصف: | Abstract Background Tissue hypoxia is a pathological condition characterized by reducing oxygen supply. Hypoxia is a hallmark of tumor environment and is commonly observed in many solid tumors. Non-invasive imaging techniques like positron emission tomography (PET) are at the forefront of detecting and monitoring tissue hypoxia changes in vivo. Results We have developed a novel 18F-labeled radiotracer for hypoxia PET imaging based on cytotoxic agent benznidazole. Radiotracer N-(4-[18F]fluorobenzyl)-2-(2-nitro-1H-imidazol-1-yl)acetamide ([18F]FBNA) was synthesized through acylation chemistry with readily available 4-[18F]fluorobenzyl amine. Radiotracer [18F]FBNA was obtained in good radiochemical yields (47.4 ± 5.3%) and high radiochemical purity (> 95%). The total synthesis time was 100 min, including HPLC purification and the molar activity was greater than 40 GBq/µmol. Radiotracer [18F]FBNA was stable in saline and mouse serum for 6 h. [18F]FBNA partition coefficient (logP = 1.05) was found to be more lipophilic than [18F]EF-5 (logP = 0.75), [18F]FMISO (logP = 0.4) and [18F]FAZA (logP = − 0.4). In vitro studies showed that [18F]FBNA accumulates in gastric cancer cell lines AGS and MKN45 under hypoxic conditions. Conclusions Hence, [18F]FBNA represents a novel and easy-to-prepare PET radioligand for imaging hypoxia. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 2365-421X |
| Relation: | https://doaj.org/toc/2365-421X |
| DOI: | 10.1186/s41181-022-00165-0 |
| URL الوصول: | https://doaj.org/article/7847c548591345c4b59d72e89074972b |
| رقم الأكسشن: | edsdoj.7847c548591345c4b59d72e89074972b |
| قاعدة البيانات: | Directory of Open Access Journals |
Find this article in full text from Springer Verlag. 
Full Text Finder | تدمد: | 2365421X |
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| DOI: | 10.1186/s41181-022-00165-0 |