Synthesis and pharmacokinetics of 131I labeled benzoyl derivatives of estrone and estradiol.
3-(2-[131I]iodobenzoyl)estradiol-17 beta (1), 3-(2-[131I]iodobenzoyl)estrone (2) and 17 beta-(2-[131I]iodobenzoyl)-estradiol (3) have been prepared by bromine-iodine exchange followed by preparative HPLC in radiochemical yields greater than 70% (isolated). The specific activities were greater than 200 Ci/mmol. Tissue distribution studies in DMBA-induced tumor bearing rats showed a rapid clearance via the kidneys and poor accumulation in the target tissues. The relative binding affinities to the estrogen receptor were estimated as 3.5% 1, 1.7% 2 and 0.05% 3 of the affinity of estradiol (100%).
D015127:9,10-Dimethyl-1,2-benzanthracene; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism*; D004970:Estrone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism*; D005260:Female; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D007700:Kinetics; D008325:Mammary Neoplasms, Experimental / Q000139:chemically induced / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; D004970:Estrone; D004958:Estradiol; D015127:9,10-Dimethyl-1,2-benzanthracene; C046149:3-(2-iodobenzoyl)estradiol; C046150:3-(2-iodobenzoyl)estrone