Adamantane-containing glutamate blocker IEM-1913 (1-amino-4-(1-adamantane-amino)-butane dihydrochloride) equals to memantine in antiparkinsonian potency, but surpasses it in anticonvulsive, antidepressant, and analgesic activities. Moreover, its use is less toxic and safer. IEM-1913 produces significant pharmacological effects at a wide concentration diapason (0.03-1.00 mg/kg), while memantine is effective within a narrow range only (15-20 mg/kg). High pharmacological efficacy and low toxicity of IEM-1913 can be explained by the fact that in contrast to monocationic selective NMDA antagonist memantine, the dicationic glutamate blocker IEM-1913 produces a combined block of cerebral NMDA and AMPA receptors.
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Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 160, No. 7, pp. 80-83, July, 2015
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Gmiro, V.E., Serdyuk, S.E. & Veselkina, O.S. Comparison of Pharmacological Potency and Safety of Glutamate Blocker IEM-1913 and Memantine. Bull Exp Biol Med 160, 68–71 (2015). https://doi.org/10.1007/s10517-015-3100-9
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DOI: https://doi.org/10.1007/s10517-015-3100-9