Abstracto

IEM-1913: a novel glutamate antagonist that is effective and safe compared to memantine

Gmiro VE, Serdyuk SE, Veselkina OS

The adamantane-containing glutamate antagonist IEM-1913, 1-amino-4-(1-adamantanamino)butane dihydrochloride, has antiparkinsonian activity similar to memantine, but surpasses memantine in anticonvulsant, antidepressant and analgesic activity, and also unlike memantine is less toxic and safer for application. IEM-1913 causes reliable pharmacological effects in a wide dose range of 0.03-1 mg/kg, while memantine is effective only in a narrow dose range, 15-20 mg/kg. The high pharmacological activity and relatively weak toxicity of IEM-1913 are due to the fact that the biscationic glutamate antagonist IEM-1913, unlike the selective monocationic NMDA antagonist memantine, causes combined blockade of both NMDA and AMPA receptors in the brain.