Preparation of four fluorine- 18-labeled estrogens and their selective uptakes in target tissues of immature rats.
Preparation of four fluorine- 18-labeled estrogens and their selective uptakes in target tissues of immature rats.
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发表时间：
1984-11
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通讯作者：
D. Kiesewetter;M. Kilbourn;S. Landvatter;D. Heiman;J. Katzenellenbogen;M. Welch
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作者：
D. Kiesewetter;M. Kilbourn;S. Landvatter;D. Heiman;J. Katzenellenbogen;M. Welch
四种氟-18-标记雌激素--16 α-[18 F]氟-雌二醇-17 β（1）、16 β-[18 F]氟-雌二醇-17 β（2）、（2 R，3S）-1-[18 F]氟-2，3-双（4-羟苯基）戊烷（1-[18F]氟戊雌醇）（3）和（3R，4S）-1-[18F]氟-3，4-双（4-羟基苯基）己烷（1-[18 F]氟己雌酚）（4）--已通过简单置换反应利用反应性三氟甲烷磺酸盐（三氟甲磺酸盐）前体和F-18氟离子制备。所有四种氟代雌激素对雌激素受体都有很高的亲和力。在未成熟的雌性大鼠中，它们被靶组织如子宫以非常高的选择性摄取：1小时时的子宫与血液比率为：化合物1，39;化合物2，12;化合物3，13;和化合物4，19。化合物1在2小时时平均子宫-血液比超过80。通过共同施用的未标记雌二醇对靶组织摄取的抑制作用证明摄取过程涉及有限容量的雌激素特异性结合剂。
Four fluorine- 18-labeled estrogens--16 alpha-[18F]fluoro-estradiol-17 beta (1), 16 beta-[18F]fluoro-estradiol-17 beta (2), (2R, 3S)-1-[18F]fluoro-2,3-bis(4-hydroxyphenyl)-pentane (1-[18F]fluoropentestrol) (3), and (3R, 4S)-1-[18F]fluoro-3,4-bis(4-hydroxyphenyl)hexane (1-[18F]fluorohexestrol) (4)--have been prepared by simple displacement reactions utilizing reactive trifluoromethane sulfonate (triflate) precursors and F-18 fluoride ion. All four fluoroestrogens have high affinity for the estrogen receptor. In immature female rats, they are taken up by target tissues, such as the uterus, with very high selectivity: uterus-to-blood ratios at 1 hr are: Compound 1, 39; Compound 2, 12; Compound 3, 13; and Compound 4, 19. Average uterus-to-blood ratios exceed 80 for Compound 1 at 2 hr. That the uptake process involves an estrogen-specific binder of limited capacity is demonstrated by the suppressive effect of coadministered unlabeled estradiol on target tissue uptake.