{"title":"同位素法放射性合成[18F]-氟马西尼。","authors":"Riptee Thakur, Aishwarya Kumar, Raman Kumar Joshi, Pardeep Kumar","doi":"10.4103/ijnm.ijnm_82_24","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Fluorine-18 (<sup>18</sup>F) flumazenil (FMZ) has been synthesized using various precursors, and its role has been explored in imaging Gamma-aminobutyric acid-A receptors.</p><p><strong>Aim and objective: </strong>The main objective was to synthesize (<sup>18</sup>F) FMZ using isotopic substitution.</p><p><strong>Materials and methods: </strong>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.</p><p><strong>Results: </strong>The radiolabelling efficiency of cartridge-based purification was 16 ± 4% (<i>n</i> = 10) with a radiochemical purity of 96.5 ± 1.8%, whereas in HPLC-based purification, the yield was 10 ± 4% (<i>n</i> = 5) with a radiochemical purity of 97.3 ± 1.4%. The specific activity was 120 ± 20 GBq/μmol.</p><p><strong>Conclusions: </strong>(<sup>18</sup>F) FMZ was successfully synthesized using an isotopic approach and could be used as an alternative cheaper option for the synthesis.</p>","PeriodicalId":45830,"journal":{"name":"Indian Journal of Nuclear Medicine","volume":"39 4","pages":"286-291"},"PeriodicalIF":0.4000,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11708791/pdf/","citationCount":"0","resultStr":"{\"title\":\"Radiosynthesis of [18F]-flumazenil Using an Isotopic Approach.\",\"authors\":\"Riptee Thakur, Aishwarya Kumar, Raman Kumar Joshi, Pardeep Kumar\",\"doi\":\"10.4103/ijnm.ijnm_82_24\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>Fluorine-18 (<sup>18</sup>F) flumazenil (FMZ) has been synthesized using various precursors, and its role has been explored in imaging Gamma-aminobutyric acid-A receptors.</p><p><strong>Aim and objective: </strong>The main objective was to synthesize (<sup>18</sup>F) FMZ using isotopic substitution.</p><p><strong>Materials and methods: </strong>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.</p><p><strong>Results: </strong>The radiolabelling efficiency of cartridge-based purification was 16 ± 4% (<i>n</i> = 10) with a radiochemical purity of 96.5 ± 1.8%, whereas in HPLC-based purification, the yield was 10 ± 4% (<i>n</i> = 5) with a radiochemical purity of 97.3 ± 1.4%. The specific activity was 120 ± 20 GBq/μmol.</p><p><strong>Conclusions: </strong>(<sup>18</sup>F) FMZ was successfully synthesized using an isotopic approach and could be used as an alternative cheaper option for the synthesis.</p>\",\"PeriodicalId\":45830,\"journal\":{\"name\":\"Indian Journal of Nuclear Medicine\",\"volume\":\"39 4\",\"pages\":\"286-291\"},\"PeriodicalIF\":0.4000,\"publicationDate\":\"2024-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11708791/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Indian Journal of Nuclear Medicine\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.4103/ijnm.ijnm_82_24\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/11/18 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q4\",\"JCRName\":\"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Indian Journal of Nuclear Medicine","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4103/ijnm.ijnm_82_24","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/11/18 0:00:00","PubModel":"Epub","JCR":"Q4","JCRName":"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING","Score":null,"Total":0}
Radiosynthesis of [18F]-flumazenil Using an Isotopic Approach.
Background: Fluorine-18 (18F) 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 (18F) 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% (n = 10) with a radiochemical purity of 96.5 ± 1.8%, whereas in HPLC-based purification, the yield was 10 ± 4% (n = 5) with a radiochemical purity of 97.3 ± 1.4%. The specific activity was 120 ± 20 GBq/μmol.
Conclusions: (18F) FMZ was successfully synthesized using an isotopic approach and could be used as an alternative cheaper option for the synthesis.
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