2. Academic Validation
  3. Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531)

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.
Favaad Iqbal 1,  Ryan Ellwood,  Martin Mortensen,  Trevor G Smart,  James R Baker
Affiliations

Affiliation

  • 1 Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, United Kingdom.
PMID: 21664131 DOI: 10.1016/j.bmcl.2011.05.067
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.

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