Supplementary Materials

Supplementary Material for:

The prodrug DHED selectively delivers 17β-estradiol to the brain for treating estrogen-responsive disorders

Laszlo Prokai,* Vien Nguyen, Szabolcs Szarka, Puja Garg, Gauri Sabnis, Heather A. Bimonte-Nelson, Katie J. McLaughlin, Joshua S. Talboom, Cheryl D. Conrad, Paul J. Shughrue, Todd D. Gould, Angela Brodie, Istvan Merchenthaler, Peter Koulen, Katalin Prokai-Tatrai

*Corresponding author. E-mail: laszlo.prokai{at}

Published 22 July 2015, Sci. Transl. Med. 7, 297ra113 (2015)
DOI: 10.1126/scitranslmed.aab1290

This PDF file includes:

  • Methods
  • Fig. S1. DHED is converted to E2 in vitro in brain, but not uterine tissue of OVX Sprague-Dawley rats.
  • Fig. S2. Estrogen concentrations are increased in brain but not in circulation after DHED treatments.
  • Fig. S3. Bioluminescence imaging in repTOP ERE-Luc mice.
  • Fig. S4. Lack of uterotrophic effect after DHED treatment is independent of route of administration and treatment regimen.
  • Fig. S5. Additional expression data for estrogen-sensitive proteins from the uteri of OVX mice treated with E2 and DHED.
  • Table S1. Noncompartmental single-dose PK analysis of extracted E2 concentrations in brain over time.
  • Reference (51)

[Download PDF]