cp-465-022 has been researched along with piriqualone* in 1 studies
1 other study(ies) available for cp-465-022 and piriqualone
Article | Year |
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Atropisomeric quinazolin-4-one derivatives are potent noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists.
Piriqualone (1) was found to be an antagonist of AMPA receptors. Structure activity optimization was conducted on each of the three rings in 1 to afford a series of potent and selective antagonists. The sterically crowded environment surrounding the N-3 aryl group provided sufficient thermal stability for atropisomers to be isolated. Separation of these atropisomers resulted in the identification of (+)-38 (CP-465,022), a compound that binds to the AMPA receptor with high affinity (IC50 = 36 nM) and displays potent anticonvulsant activity. Topics: Animals; Anticonvulsants; Binding, Competitive; Brain; Calcium; Disease Models, Animal; Inhibitory Concentration 50; Isomerism; Neuromuscular Blocking Agents; Protein Binding; Pyridines; Quinazolines; Quinazolinones; Rats; Receptors, AMPA; Seizures; Solubility; Structure-Activity Relationship; Synaptic Transmission | 2001 |