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

J Steroid Biochem Mol Biol. 1990 Sep;37(1):77-83. doi: 10.1016/0960-0760(90)90375-u.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenal Gland Neoplasms / drug therapy*
  • Adrenal Gland Neoplasms / metabolism
  • Animals
  • Estradiol / analogs & derivatives*
  • Estradiol / chemical synthesis
  • Estradiol / metabolism
  • Estradiol / pharmacokinetics
  • Estradiol / therapeutic use
  • Female
  • Humans
  • Iodine Radioisotopes
  • Rats
  • Rats, Inbred Strains
  • Receptors, Estrogen / drug effects*
  • Tissue Distribution

Substances

  • Iodine Radioisotopes
  • Receptors, Estrogen
  • 7-(11-(4-iodophenoxy)undecyl)-17-estradiol
  • Estradiol