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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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.
|Departments, units and centres:||Department of Pharmacology > Department of Pharmacology|
|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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