A large series of N-substituted-1,2,3,4-tetrahydroisoquinolines, bearing the most salient features described by our 3D pharmacophore model for this class of AMPAR antagonists, have been synthesized. When tested against audiogenic seizures in DBA/2 mice, some derivatives showed anticonvulsant properties. The most active compound was also tested in vitro using the patch clamp technique on hippocampal slices.
AMPA receptor antagonists: Synthesis and pharmacological evaluation
GITTO, Rosaria
Primo
;DE LUCA, Laura;FERRO, Stefania;COSTA, LARA TANIAPenultimo
;CHIMIRRI, AlbaUltimo
2007-01-01
Abstract
A large series of N-substituted-1,2,3,4-tetrahydroisoquinolines, bearing the most salient features described by our 3D pharmacophore model for this class of AMPAR antagonists, have been synthesized. When tested against audiogenic seizures in DBA/2 mice, some derivatives showed anticonvulsant properties. The most active compound was also tested in vitro using the patch clamp technique on hippocampal slices.File in questo prodotto:
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