title: Biodistribution and breast tumor uptake of 16alpha-[18F]-fluoro-17beta-estradiol in rat.
abstract: To evaluate the usefulness of 16alpha-[18F]-fluoro-17beta-estradiol (FES) for the assessment of estrogen receptor (ER), we examined the tissue distribution and kinetics of FES in immature female Sprague-Dawley rats and then 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 highly 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 tissues were 0.12 +/- 0.05%ID/g or less and 0.05 +/- 0.03%ID/g or less, respectively. Coadministration of unlabeled beta-estradiol showed marked depression of uterine FES uptake. The FES uptake by rat breast tumors was 0.14 +/- 0.06%ID/g at 60 min and 0.12 +/- 0.09%ID/g at 120 min. The FES uptake by rat breast 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 ER mediated and FES is thus useful for detecting ER positive breast tumors.
authors.affiliation: Department of Clinical Radiology, Graduate School of Medical Sciences, Kyushu University, Fukuoka, Japan. msasaki@radiol.med.kyushu-u.ac.jp
authors.forename: M
authors.initials: M
authors.lastname: Sasaki
authors.forename: T
authors.initials: T
authors.lastname: Fukumura
authors.forename: Y
authors.initials: Y
authors.lastname: Kuwabara
authors.forename: T
authors.initials: T
authors.lastname: Yoshida
authors.forename: M
authors.initials: M
authors.lastname: Nakagawa
authors.forename: Y
authors.initials: Y
authors.lastname: Ichiya
authors.forename: K
authors.initials: K
authors.lastname: Masuda
mesh_terms: D015127:9,10-Dimethyl-1,2-benzanthracene / Q000633:toxicity; D000818:Animals; D002273:Carcinogens / Q000633:toxicity; D004958:Estradiol / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D005260:Female; D005462:Fluorine Radioisotopes / Q000493:pharmacokinetics*; D008325:Mammary Neoplasms, Experimental / Q000139:chemically induced / Q000000981:diagnostic imaging* / Q000378:metabolism*; D011877:Radionuclide Imaging; D051381:Rats; D017207:Rats, Sprague-Dawley; D011960:Receptors, Estrogen / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D002273:Carcinogens; D005462:Fluorine Radioisotopes; D011960:Receptors, Estrogen; D004958:Estradiol; D015127:9,10-Dimethyl-1,2-benzanthracene; C043436:16-fluoroestradiol