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American Chemical Society, Journal of Medicinal Chemistry, 1(46), p. 197-200, 2002

DOI: 10.1021/jm0210008

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Discovery of a Novel and Highly Potent Noncompetitive AMPA Receptor Antagonist

Journal article published in 2003 by Rosaria Gitto, Maria Letizia Barreca ORCID, Laura De Luca ORCID, Giovambattista De Sarro, Guido Ferreri, Silvana Quartarone, Emilio Russo, Andrew Constanti, Alba Chimirri
This paper is available in a repository.
This paper is available in a repository.

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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.