Discovery of a Novel and Highly Potent Noncompetitive AMPA Receptor Antagonist

Gitto, R., Barreca, M.L., De Luca, L., De Sarro, G., Ferreri, G., Quartarone, S., Russo, E., Constanti, A. and Chimirri, A. (2003) Discovery of a Novel and Highly Potent Noncompetitive AMPA Receptor Antagonist. Journal of Medicinal Chemistry, 46 (1). pp. 197-200. 10.1021/jm0210008.

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DOI: 10.1021/jm0210008

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.

Item Type:Article
Departments, units and centres:Department of Pharmacology > Department of Pharmacology
ID Code:3289
Journal or Publication Title:Journal of Medicinal Chemistry
Deposited By:Library Staff
Deposited On:24 May 2012 17:42
Last Modified:24 May 2012 17:42

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