Tricyclic heteroaromatic systems. 3-substituted 1,2,3,5,6,7-hexahydro-2,5,6-trioxopyrazino[1,2,3-de]-quinoxalines as novel antagonists at the glycine-NMDA site
Varano, F.; Catarzi, D.; Colotta, V.; Cecchi, L.; Filacchioni, G.; Galli, A.; Costagli, C.
Farmaco 52(3): 179-182
1997
ISSN/ISBN: 0014-827X PMID: 9212452 Document Number: 469940
Two novel antagonists of the glycine-NMDA receptor have been synthesized and tested for their ability to displace [3H]glycine from its specific binding site in rat brain cortical membranes. The 3-substituted pyrazino[1,2,3-de]quinoxalin-2,5,6-triones 1a-b contain all the essential pharmacophoric descriptors of a glycine receptor antagonist. A model is proposed for the binding of these compounds that includes some of the interactions postulated for the potent glycine-NMDA receptor antagonist L-689,560.