PREPARATION OF 4 FLUORINE-18-LABELED ESTROGENS AND THEIR SELECTIVE UPTAKES IN TARGET TISSUES OF IMMATURE RATS

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  • 1 January 1984
    • journal article
    • research article
    • Vol. 25  (11) , 1212-1221
Abstract
Four fluorine-18-labeled estrogens were prepared: 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). They were prepared by simple displacement reactions utilizing reactive trifluoromethane sulfonate (triflate) precursors and 18F-. All 4 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 h are: 1, 39; 2, 12; 3, 13; and 4, 19. Average uterus-to-blood ratios exceed 80 for 1 at 2 h. 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. [This research has application to antiestrogen therapy of human breast cancer.].

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