To evaluate the usefulness of 16 alpha-[F-18]-fluoro-17 beta-estradiol (FES
) for the assessment of estrogen receptor (ER), we examined the tissue dist
ribution and kinetics of FES in immature female Sprague-Dawley rats and the
n examined FES uptake in rat breast tumors induced by 7,12-dimethylbenz(a)
anthracene (DMBA). The FES uptake by the uterus, an ER-rich tissue, was hig
hly selective and it was 3.34 +/- 0.79%ID/g at 60 minutes and 1.57 +/- 0.57
%ID/g at 120 minutes after injection. The FES uptakes in ER-negative tissue
s were 0.12 +/- 0.05%ID/g or less and 0.05 +/- 0.03%ID/g or less, respectiv
ely. Coadministration of unlabeled beta-estradiol showed marked depression
of uterine FES uptake. The FES uptake by rat breast tumors was 0.14 +/- 0.0
6%ID/g at 60 min and 0.12 +/- 0.09%ID/g at 120 min. The FES uptake by rat b
reast tumors correlated with the ER concentration (r = 0.45, p < 0.05). In
conclusion, these results suggest that the FES uptake by tissue is mainly E
R mediated and FES is thus useful for detecting ER positive breast tumors.