Indantadol (the free base of CHF-3381) is an orally active, non-selective NMDA antagonist and MAO inhibitor. Indantadol blocks the binding of [³H]-MK-801 to NMDA receptors in a non-competitive manner, with an IC 50 of 8.1 μM. Indantadol completely inhibits dopamine release caused by NMDA. Indantadol protects neurons, with an ED₅₀ of 35 μM. Indantadol has anticonvulsant and anti-high pain hypersensitivity activities.
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