Preparation and evaluation of 17 alpha-[125I]iodovinyl-11 beta-methoxyestradiol as a highly selective radioligand for tissues containing estrogen receptors: concise communication.
The moxestrol analog 17 alpha-[125I]iodovinyl-11 beta-methoxyestradiol was prepared in 95% radiochemical yield from the corresponding 17 alpha-(tributylstannyl) vinyl compound and no-carrier-added sodium [125I]iodide. The new radioligand was evaluated in immature female rats to determine the uptake in and selectivity for tissues containing estrogen receptors. At 1, 2, and 6 hr after injection, the agent demonstrates both high selectivity (uterus to blood ratio) and a high concentration in the target tissue. These values are considerably better than those previously reported for IVE2 or for the 16 alpha-radiohalogenated estradiols. The compound's biologic properties and its ease of preparation suggest that it would be a likely candidate for clinical use as an estrogen-receptor-seeking radiopharmaceutical.
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004353:Drug Evaluation, Preclinical; D004958:Estradiol / Q000031:analogs & derivatives / Q000378:metabolism; D005260:Female; D007457:Iodine Radioisotopes; D007553:Isotope Labeling; D007700:Kinetics; D011869:Radioligand Assay / Q000379:methods; D051381:Rats; D011919:Rats, Inbred Strains; D011960:Receptors, Estrogen / Q000032:analysis*; D014018:Tissue Distribution; D014599:Uterus / Q000378:metabolism
D007457:Iodine Radioisotopes; D011960:Receptors, Estrogen; D004958:Estradiol; C034555:17 alpha-iodovinylestradiol; C042716:17 alpha-iodovinyl-11 beta-methoxyestradiol