1.
Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531).
Bioorg Med Chem Lett
; 21(14): 4252-4, 2011 Jul 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21664131
RESUMO
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.