NMDAR antagonist 5 (Compound A17) is a multi-target antagonist against NMDAR and monoamine transporters ( SERT 、 DAT and NET ). NMDAR antagonist 5 shows good NMDAR antagonistic potency ( IC 50 = 0.3 μM) and monoamine transporter activities (SERT IC 50 = 1.1 μM、DAT IC 50 = 0.7 μM、NET IC 50 = 2.7 μM). NMDAR antagonist 5 is highly safe and has low toxicity (hepatotoxicity and nephrotoxicity (IC 50 > 100 μM); cardiotoxicity (IC 50 = 24.5 μM)). NMDAR antagonist 5 has antidepressant effects and can be used in the study of depression.
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