Synthesis and evaluation of fluorine-18 21-fluoroprednisone as a potential ligand for neuro-PET studies Journal Article
| Authors: | Feliu, A. L.; Rottenberg, D. A. |
| Article Title: | Synthesis and evaluation of fluorine-18 21-fluoroprednisone as a potential ligand for neuro-PET studies |
| Abstract: | No-carrier-added fluorine-18-labeled fluoroprednisone ([18F]21-fluoroprednisone) was synthesized by tosylate displacement in 2%-8% radiochemical yield in 80 min end of cyclotron bombardment (EOB), and its metabolism and distribution were investigated. After intravenous administration to rats, [18F]21-fluoroprednisone was rapidly cleared from the blood and biotransformed into [18F]20-dihydro-21-fluoroprednisone. The suitability of [18F]21-fluorocorticoids for receptor imaging in humans with positron emitting tomography will depend on the synthesis of compounds with high binding affinity and low rate of carbonyl reduction at C-20. |
| Keywords: | unclassified drug; human cell; prednisone; methodology; animal; metabolism; animal experiment; drug synthesis; liver; drug distribution; isotope labeling; tissue distribution; rat; drug clearance; rats; drug monitoring; drug metabolism; drug blood level; high performance liquid chromatography; radioisotope; radioisotopes; synthesis; intravenous drug administration; normal human; pharmacokinetics; tomography, emission-computed; receptors, glucocorticoid; nervous system; drug solubility; drug identification; fluorine; body distribution; human; priority journal; support, u.s. gov't, p.h.s.; blood and hemopoietic system; drug analysis; 21 fluoro 20 dihydroprednisone f 18; 21 fluoroprednisone f 18 |
| Journal Title: | Journal of Nuclear Medicine |
| Volume: | 28 |
| Issue: | 6 |
| ISSN: | 0161-5505 |
| Publisher: | Society of Nuclear Medicine |
| Date Published: | 1987-06-01 |
| Start Page: | 998 |
| End Page: | 1005 |
| Language: | English |
| PUBMED: | 3495649 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Article -- Export Date: 5 February 2021 -- Source: Scopus |
