title: Comparison of Pharmacological Potency and Safety of Glutamate Blocker IEM-1913 and Memantine.
abstract: 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.
authors.affiliation: Research Institute of Experimental Medicine, Russian Academy of Medical Sciences, St. Petersburg, Russia. gmiro2119@gmail.com.
authors.forename: V E
authors.initials: VE
authors.lastname: Gmiro
authors.affiliation: Research Institute of Experimental Medicine, Russian Academy of Medical Sciences, St. Petersburg, Russia.
authors.forename: S E
authors.initials: SE
authors.lastname: Serdyuk
authors.affiliation: Verteks, St. Petersburg, Russia.
authors.forename: O S
authors.initials: OS
authors.lastname: Veselkina
mesh_terms: D000700:Analgesics / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology / Q000633:toxicity; D000928:Antidepressive Agents / Q000494:pharmacology / Q000633:toxicity; D000978:Antiparkinson Agents / Q000494:pharmacology / Q000633:toxicity; D001952:Bridged-Ring Compounds / Q000494:pharmacology* / Q000633:toxicity; D002375:Catalepsy / Q000139:chemically induced / Q000188:drug therapy; D004353:Drug Evaluation, Preclinical; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology* / Q000633:toxicity; D006220:Haloperidol / Q000633:toxicity; D006358:Hot Temperature / Q000009:adverse effects; D007928:Lethal Dose 50; D008559:Memantine / Q000494:pharmacology* / Q000633:toxicity; D051379:Mice; D010433:Pentylenetetrazole / Q000633:toxicity; D010807:Physical Endurance / Q000187:drug effects; D011700:Putrescine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors; D012018:Reflex / Q000187:drug effects; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy
chemical_list: D000700:Analgesics; D000927:Anticonvulsants; D000928:Antidepressive Agents; D000978:Antiparkinson Agents; D001952:Bridged-Ring Compounds; D018691:Excitatory Amino Acid Antagonists; C526128:IEM 1913; D018091:Receptors, AMPA; D016194:Receptors, N-Methyl-D-Aspartate; D006220:Haloperidol; D011700:Putrescine; D008559:Memantine; D010433:Pentylenetetrazole
keywords: AMPA; IEM-1913; NMDA; memantine; parkinsonism