Literature DB >> 12502375

Discovery of a novel and highly potent noncompetitive AMPA receptor antagonist.

Rosaria Gitto1, Maria Letizia Barreca, Laura De Luca, Giovambattista De Sarro, Guido Ferreri, Silvana Quartarone, Emilio Russo, Andrew Constanti, Alba Chimirri.   

Abstract

N-Acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives were designed and synthesized as potential noncompetitive AMPA receptor antagonists on the basis of molecular modeling studies. Sound-induced seizure testing showed that this class of compounds possessed anticonvulsant properties. In particular, 10c was more potent than talampanel (2), a noncompetitive AMPA receptor antagonist currently being investigated in phase III trials as an antiepileptic agent. Furthermore, electrophysiological studies indicated that 10c was a highly effective noncompetitive-type modulator of the AMPA receptor.

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Year:  2003        PMID： 12502375     DOI： 10.1021/jm0210008

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  5 in total

Review 1.  Glutamate receptor ion channels: structure, regulation, and function.

Authors:  Stephen F Traynelis; Lonnie P Wollmuth; Chris J McBain; Frank S Menniti; Katie M Vance; Kevin K Ogden; Kasper B Hansen; Hongjie Yuan; Scott J Myers; Ray Dingledine
Journal:  Pharmacol Rev       Date:  2010-09       Impact factor: 25.468

2.  Synthesis and contractile activity of substituted 1,2,3,4-tetrahydroisoquinolines.

Authors:  Iliyan Ivanov; Stoyanka Nikolova; Dimo Aladjov; Iliyana Stefanova; Plamen Zagorchev
Journal:  Molecules       Date:  2011-08-16       Impact factor: 4.411

3.  Synthesis of σ Receptor Ligands with a Spirocyclic System Connected with a Tetrahydroisoquinoline Moiety via Different Linkers.

Authors:  Melanie Bergkemper; Dirk Schepmann; Bernhard Wünsch
Journal:  ChemMedChem       Date:  2021-02-02       Impact factor: 3.466

4.  Synthesis and fluorescent properties of boroisoquinolines, a new family of fluorophores.

Authors:  Dénes Sóvári; Attila Kormos; Orsolya Demeter; András Dancsó; György Miklós Keserű; Mátyás Milen; Péter Ábrányi-Balogh
Journal:  RSC Adv       Date:  2018-11-15       Impact factor: 3.361

Review 5.  1-Methyl-1,2,3,4-tetrahydroisoquinoline, an endogenous amine with unexpected mechanism of action: new vistas of therapeutic application.

Authors:  Lucyna Antkiewicz-Michaluk; Agnieszka Wąsik; Jerzy Michaluk
Journal:  Neurotox Res       Date:  2013-05-30       Impact factor: 3.911
  5 in total

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