In vivo evaluation of 7 alpha-[11-(4-[125I]iodophenoxy)undecyl]-17 beta-estradiol: a potential vector for therapy of adrenal and estrogen receptor-positive cancers.
7 alpha-[11-(4-[125I]Iodophenoxy)undecyl]-17 beta-estradiol ([125I]IPUE2) was synthesized and its tissue distribution studied in immature female Fischer rats. Upon intravenous administration, [125I]IPUE2 was shown to accumulate in the adrenals and, to some extent, in the uterus and the ovaries. Coinjection with estrogen receptor (ER)-saturating quantities of unlabeled 17 beta-estradiol did not significantly reduce the uptake of [125I]IPUE2 in these tissues. The high adrenal uptake of [125I]IPUE2 is most likely associated with the lipophilic nature of the 7 alpha-substituted estradiol. The potential to use the 7 alpha-undecylestradiol as a vector to direct therapeutic groups to adrenal and ER-positive cancers is discussed.
DaSilva
J N
JN
MRC Group in the Radiation Sciences, Faculty of Medicine, University of Sherbrooke, Quebec, Canada.
van Lier
J E
JE
D000310:Adrenal Gland Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D000818:Animals; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use; D005260:Female; D006801:Humans; D007457:Iodine Radioisotopes; D051381:Rats; D011919:Rats, Inbred Strains; D011960:Receptors, Estrogen / Q000187:drug effects*; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; D011960:Receptors, Estrogen; C066479:7-(11-(4-iodophenoxy)undecyl)-17-estradiol; D004958:Estradiol