TRICYCLIC HETEROAROMATIC SYSTEMS - 3-SUBSTITUTED XAHYDRO-2,5,6-TRIOXOPYRAZINO[1,2,3-DE]QUINOXALINES AS NOVEL ANTAGONISTS AT THE GLYCINE-NMDA SITE

Authors
VARANO F CATARZI D COLOTTA V CECCHI V CECCHI L FILACCHIONI G GALLI A COSTAGLI C
Citation
F. Varano et al., TRICYCLIC HETEROAROMATIC SYSTEMS - 3-SUBSTITUTED XAHYDRO-2,5,6-TRIOXOPYRAZINO[1,2,3-DE]QUINOXALINES AS NOVEL ANTAGONISTS AT THE GLYCINE-NMDA SITE, Il Farmaco, 52(3), 1997, pp. 179-182
Citations number
14
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
Il Farmaco → ACNP
ISSN journal
0014827X
Volume
52
Issue
3
Year of publication
1997
Pages
179 - 182
Database
ISI
SICI code
0014-827X(1997)52:3<179:THS-3X>2.0.ZU;2-Q
Abstract
Two novel antagonists of the glycine-NMDA receptor have been synthesiz ed and tested for their ability to displace [H-3]glycine from its spec ific binding site in rat brain cortical membranes. The 3-substituted p yrazino[1,2,3-de]quinoxalin-2,5,6-trion 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 t he interactions postulated for the potent glycine-NMDA receptor antago nist L-689,560.