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.
|Titolo:||AMPA receptor antagonists: synthesis and pharmacological evaluation|
|Data di pubblicazione:||2007|
|Citazione:||AMPA receptor antagonists: synthesis and pharmacological evaluation / GITTO R; DE LUCA L; PAGANO B; FERRO S; DE SARRO G; CITRARO R; CIRANNA L; COSTA L; CHIMIRRI A. - In: FARMACEVTSKI VESTNIK. - ISSN 0014-8229. - 58(2007), pp. 21-24.|
|Appare nelle tipologie:||4.1 Contributo in Atti di convegno|