cp-465-022 and piriqualone

cp-465-022 has been researched along with piriqualone* in 1 studies

Other Studies

1 other study(ies) available for cp-465-022 and piriqualone

Article	Year
Atropisomeric quinazolin-4-one derivatives are potent noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists. Bioorganic & medicinal chemistry letters, 2001, Jan-22, Volume: 11, Issue:2 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

Article

Year

Atropisomeric quinazolin-4-one derivatives are potent noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists.

Bioorganic & medicinal chemistry letters, 2001, Jan-22, Volume: 11, Issue:2

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