title: Synthesis and radiopharmacological evaluation of 2'-(4-fluorophenyl)-21-[18F]fluoro-20-oxo-11beta,17alpha-dihydroxy-pregn-4-eno[3,2-c]pyrazole as potential glucocorticoid receptor ligand for positron emission tomography (PET).
abstract: The radiosynthesis and the radiopharmacological evaluation of pyrazolo steroid 2'-(4-fluorophenyl)-21-[18F]fluoro-20-oxo-11beta,17alpha-dihydroxy-pregn-4-eno[3,2-c]pyrazole [18F]-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/micromol. 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 [18F]-2 was completed with autoradiography using rat brain sections and micro-PET imaging.
authors.affiliation: Institut für Bioanorganische und Radiopharmazeutische Chemie, Forschungszentrum Rossendorf e.V., PO Box 51 01 19, D-01314 Dresden, Germany. f.wuest@fz-rossendorf.de
authors.forename: Frank
authors.initials: F
authors.lastname: Wüst
authors.forename: Torsten
authors.initials: T
authors.lastname: Kniess
authors.forename: Marion
authors.initials: M
authors.lastname: Kretzschmar
authors.forename: Ralf
authors.initials: R
authors.lastname: Bergmann
mesh_terms: D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000000981:diagnostic imaging / Q000187:drug effects / Q000378:metabolism*; D004355:Drug Stability; D005462:Fluorine Radioisotopes; D007553:Isotope Labeling; D008024:Ligands; D008297:Male; D008968:Molecular Conformation; D049268:Positron-Emission Tomography / Q000379:methods*; D011278:Pregnanes / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D011965:Receptors, Glucocorticoid / Q000032:analysis / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
chemical_list: C501617:2'-(4-fluorophenyl)-21-fluoro-20-oxo-11beta,17alpha-dihydroxy-pregn-4-eno(3,2-c)pyrazole; D005462:Fluorine Radioisotopes; D008024:Ligands; D011278:Pregnanes; D011720:Pyrazoles; D011965:Receptors, Glucocorticoid