Feliu A L, Rottenberg D A
J Nucl Med. 1987 Jun;28(6):998-1005.
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.
通过甲苯磺酸酯取代反应合成了无载体添加的氟-18标记氟泼尼龙（[18F]21-氟泼尼龙），在回旋加速器轰击结束后80分钟内放射化学产率为2%-8%，并对其代谢和分布进行了研究。给大鼠静脉注射后，[18F]21-氟泼尼龙迅速从血液中清除，并生物转化为[18F]20-二氢-21-氟泼尼龙。[18F]21-氟皮质激素用于人体正电子发射断层扫描受体成像的适用性将取决于具有高结合亲和力和低C-20羰基还原率的化合物的合成。
