E-17 alpha[125I]iodovinylestradiol: an estrogen-receptor-seeking radiopharmaceutical.
Through the use of radioiododestannylation, the specifically labeled E-17 alpha-[125I]iodovinylestradiol [(I-125)VE2] was synthesized rapidly and in high yield from the stable precursor E-17 alpha-tributylstannylvinylestradiol (SnVE2), and its biodistribution was determined in immature female rats. The agent accumulated in the uterus, achieving a peak uptake of 0.465% ID-kg/g at 2 hr. Uterus-to-blood ratios of 19 and 16 occurred at 1 and 2 hr, respectively, declining to 7 by 4 hr after injection. The uptake of (I-125)VE2 by the uterus at 2 hr was reduced 58--65% by pretreatment of the immature rats with estradiol (5 micrograms) or tamoxifen (100 micrograms), and compared with 16 alpha-[125I]iodoestradiol, (I-125)VE2 showed greater uterine uptake and similar uterus-to-blood ratios. The ease of preparation of the radioligand represents an advantage over the synthetic procedures for other estrogen-receptor-seeking agents.
D000818:Animals; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D007457:Iodine Radioisotopes; D051381:Rats; D011919:Rats, Inbred Strains; D011960:Receptors, Estrogen / Q000378:metabolism; D013629:Tamoxifen / Q000494:pharmacology; D014018:Tissue Distribution; D014599:Uterus / Q000378:metabolism
D007457:Iodine Radioisotopes; D011960:Receptors, Estrogen; D013629:Tamoxifen; D004958:Estradiol; C034555:17 alpha-iodovinylestradiol