Synthesis and radiopharmacological evaluation of 2′-(4-fluorophenyl)-21-[18F]fluoro-20-oxo-11β,17α-dihydroxy-pregn-4-eno[3,2-c]pyrazole as potential glucocorticoid receptor ligand for positron emission tomography (PET)
- 作者：W脙脙st ; Frank ; Kniess ; Torsten ; Kretzschmar ; Marion ; Bergmann ; Ralf
- 关键词：Positron emission tomography ; Glucocorticoid receptor ; Radiolabeling
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2005
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：March 1, 2005
- 卷：15
- 期：5
- 页码：1303-1306
- 文件大小：183 K
摘要
The radiosynthesis and the radiopharmacological evaluation of pyrazolo steroid 2芒芒芒-(4-fluorophenyl)-21-[18F]fluoro-20-oxo-11芒芒,17芒芒-dihydroxy-pregn-4-eno[3,2-c]pyrazole [18F]-2 is described. The radiolabeling was accomplished in 3芒芒芒4%decay-corrected radiochemical yield within 80min at an specific radioactivity of 0.8芒芒芒1.2Ci/芒芒mol. Biodistribution studies in male Wistar rats showed an initial brain uptake of 0.25芒芒0.03%ID/g after 5min, which remained constant over 60min. The radiopharmacological evaluation of compound [18F]-2 was completed with autoradiography using rat brain sections and micro-PET imaging.