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 with the aim to realize a systematic investigation of the structure-activity relationships (SAR). All synthesized compounds have been tested against audiogenic seizures in DBA/2 mice and 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
CIRANNA, Lucia;
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 with the aim to realize a systematic investigation of the structure-activity relationships (SAR). All synthesized compounds have been tested against audiogenic seizures in DBA/2 mice and 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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