Study of 3,4-Methylenedioxyphenyl Formylmorpholine Binding to AMPA Receptor

OBJECTIVE To investigate the binding of 3,4-methylenedioxyphenyl formylmorpholine(compound 1) to AMPA receptor. METHODS The potency of compound 1 binding to AMPA receptor was evaluated by radioligand binding assay. Meanwhile, the binding mode of compound 1 to AMPA receptor was evaluated by molecular docking.RESULTS Compound 1 showed high affinity of AMPA receptor with the IC₅₀ value of 1.74×10^-9 mol·L^-1. Meanwhile, the results from molecular docking indicated that compound 1 could bind to AMPA receptor by high affinity with the ΔE value of -5.46 kcal·mol^-1. Hydrogen bond, hydrophobic force and electrostatic interaction played key roles in binding. Moreover, the O atoms of compound 1 could form hydrogen bond with Ser108 and Ser242 of AMPA receptor, which was recommended as the key binding site. CONCLUSION The results demonstrate that compound 1 could bind to AMPA receptor with high affinity,.