A single intrauterine injection of the serine protease inhibitor 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride reversibly inhibits embryo implantation in mice

Contraception. 2007 Sep;76(3):250-5. doi: 10.1016/j.contraception.2007.05.084. Epub 2007 Jul 5.

Abstract

Background: The study was conducted to investigate the inhibitory effect of 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride (AEBSF) on embryo implantation in mice with a view to identifying whether it might be a suitable agent for postcoital contraception.

Study design: The anti-implantation efficacy of AEBSF was determined by counting the number of visible implanted embryos on Day 8 of pregnancy following a single intrauterine injection of AEBSF at doses of 30, 300 and 3000 microg per mouse uterine horn on Day 3 of pregnancy. The reversibility of the inhibitory effect of AEBSF on implantation was further evaluated by observing the outcome of a subsequent pregnancy without AEBSF treatment.

Results: A dose-dependent inhibitory effect of AEBSF on embryo implantation in vivo was observed. Morphological analysis revealed no significant cytotoxicity of AEBSF on the mouse uterine epithelia. Furthermore, the anti-implantation effect of AEBSF was reversible.

Conclusion: Intrauterine administration of AEBSF at an appropriate dose might provide a basis for the development of novel contraception.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Embryo Implantation / drug effects*
  • Epithelium / drug effects
  • Female
  • Fertility / drug effects
  • Injections
  • Mice
  • Mice, Inbred ICR
  • Serine Endopeptidases / metabolism
  • Serine Proteinase Inhibitors / pharmacology*
  • Sulfones / pharmacology*
  • Uterus / drug effects
  • Uterus / metabolism

Substances

  • Serine Proteinase Inhibitors
  • Sulfones
  • 4-(2-aminoethyl)benzenesulfonylfluoride
  • Prss29 protein, mouse
  • Serine Endopeptidases