Synthesis and radioparmacological 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)

被引：4

作者：

Wüst, F ^{[1
]}

Kniess, T ^{[1
]}

Kretzschmar, M ^{[1
]}

Bergmann, R ^{[1
]}

机构：

[1] Forschungszentrum Rossendorf EV, Inst Bioorgan & Radiopharmaceut Chem, D-01314 Dresden, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 05期

关键词：

positron emission tomography; glucocorticoid receptor; radiolabeling;

D O I：

10.1016/j.bmcl.2005.01.033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The radiosynthesis and the radiopharmacological evaluation of pyrazolo steroid 2'-(4-fluorophenyl)-21-[F-18]fluoro-20-oxo-1 11 beta, 17 alpha-dihydroxy-pregn-4-eno[3,2-c]pyrazole [F-18]-2 is described. The radiolabeling was accomplished in 3-4% decay-corrected radiochemical yield within 80 min at an specific radioactivity of 0.8-1.2 Ci/mu mol. Biodistribution studies in male Wistar rats showed an initial brain uptake of 0.25 +/- 0.03% ID/g after 5 min, which remained constant over 60 min. The radiopharmacological evaluation of compound [F-18]-2 was completed with autoradiography using rat brain sections and micro-PET imaging. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1303 / 1306

页数：4