Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531)

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4252-4. doi: 10.1016/j.bmcl.2011.05.067. Epub 2011 May 25.

Abstract

A selection of highly potent analogues based on the gabazine structure is described. Their syntheses are carried out in just four steps, and their potencies for antagonism at the GABA(A) receptor were measured. All antagonists showed significantly higher potencies compared to the parent competitive antagonist, gabazine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • GABA-A Receptor Antagonists / chemical synthesis*
  • GABA-A Receptor Antagonists / chemistry
  • GABA-A Receptor Antagonists / pharmacology
  • Pyridazines / chemical synthesis
  • Pyridazines / chemistry*
  • Pyridazines / pharmacology
  • Receptors, GABA-A / chemistry*
  • Receptors, GABA-A / metabolism

Substances

  • GABA-A Receptor Antagonists
  • Pyridazines
  • Receptors, GABA-A
  • gabazine