| Abstract
| - N-Acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives were designed andsynthesized as potential noncompetitive AMPA receptor antagonists on the basis of molecularmodeling studies. Sound-induced seizure testing showed that this class of compounds possessedanticonvulsant properties. In particular, 10c was more potent than talampanel (2), anoncompetitive AMPA receptor antagonist currently being investigated in phase III trials asan antiepileptic agent. Furthermore, electrophysiological studies indicated that 10c was a highlyeffective noncompetitive-type modulator of the AMPA receptor.
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