Evaluation of selective inhibitors of 11β-HSD1 for the treatment of hypertension

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3650-3. doi: 10.1016/j.bmcl.2013.03.011. Epub 2013 Mar 22.

Abstract

In an effort to understand the origin of blood-pressure lowering effects observed in recent clinical trials with 11β-HSD1 inhibitors, we examined a set of 11β-HSD1 inhibitors in a series of relevant in vitro and in vivo assays. Select 11β-HSD1 inhibitors reduced blood pressure in our preclinical models but most or all of the blood pressure lowering may be mediated by a 11β-HSD1 independent pathway.

Publication types

  • Letter

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
  • Animals
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Hypertension / drug therapy*
  • Hypertension / enzymology*
  • Mice
  • Mice, Knockout
  • Rats
  • Rats, Inbred SHR
  • Triazoles / pharmacology*

Substances

  • Enzyme Inhibitors
  • Triazoles
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1