In vitro evaluation, biodistribution in rats of radiolabeled raloxifene

Appl Radiat Isot. 2010 Jan;68(1):33-6. doi: 10.1016/j.apradiso.2009.09.027. Epub 2009 Sep 19.

Abstract

Raloxifene is a selective estrogen receptor modulator that produces both estrogen agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue. In the present study, raloxifene was labeled with I-131 by iodogen method and investigated for its radiopharmaceutical potential. Radiolabeling yield is 91+/-0.7%, as determined by radio thin layer chromatography (RTLC). Results of in vitro study indicated (131)I-raloxifene has high stability (4h) in serum. Biodistribution study was carried out with Albino wistar female rats. The result has shown that the radioiodinated raloxifene has higher uptake in uterus than breast and ovarian.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Female
  • Iodine Radioisotopes / pharmacokinetics*
  • Raloxifene Hydrochloride / analogs & derivatives*
  • Raloxifene Hydrochloride / pharmacokinetics*
  • Rats
  • Rats, Wistar
  • Selective Estrogen Receptor Modulators / pharmacokinetics*
  • Tissue Distribution

Substances

  • Iodine Radioisotopes
  • Selective Estrogen Receptor Modulators
  • iodoraloxifene
  • Raloxifene Hydrochloride