[A comparative study of the central H-cholinergic-blocking and NMDA-blocking actions of MK-801, memantin, amantadine, pyrilen and IEM-1754 in experiments on intact rats].
Pyrilene acts as a central H-cholinoblocker upon intramuscular injection at a dose of 0.02-0.08 mg/kg, and as an NMDA-blocker, when the dose is increased to 0.2-0.8 mg/kg. Similarly, amantadine exhibits the properties of H-cholinoblocker and NMDA-blocker in the dose intervals 10-15 mg/kg and 120-180 mg/kg, respectively. The activity of MK-801 markedly exceeds that of memantine, although close doses of both NMDA-blockers inhibit the NMDA and corazole effects, as well as the central effects (analgesia and seizure) of nicotine, thus showing no significant selectivity with respect to NMDA. IEM-1754 tested on intact animals exhibited a selective action upon the NMDA receptors, preventing the NMDA-induced analgesia and lethality and the corazole-induced convulsions at doses 10-100 times lower as compared to those preventing nicotine-induced seizure and analgesia.
Gmiro
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Anichkov Department of Neuropharmacology, Russian Academy of Medical Sciences, St. Petersburg, Russia.
Serdiuk
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D000218:Adamantane / Q000031:analogs & derivatives* / Q000494:pharmacology; D000547:Amantadine / Q000494:pharmacology*; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology; D000978:Antiparkinson Agents / Q000494:pharmacology*; D018680:Cholinergic Antagonists / Q000494:pharmacology*; D016291:Dizocilpine Maleate / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology*; D005730:Ganglionic Blockers / Q000494:pharmacology*; D008297:Male; D008559:Memantine / Q000494:pharmacology*; D051379:Mice; D017288:Pain Threshold / Q000187:drug effects; D010393:Pempidine / Q000494:pharmacology*; D000644:Quaternary Ammonium Compounds / Q000494:pharmacology*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000187:drug effects
D000927:Anticonvulsants; D000978:Antiparkinson Agents; D018680:Cholinergic Antagonists; D018691:Excitatory Amino Acid Antagonists; D005730:Ganglionic Blockers; C092754:IEM 1754; D000644:Quaternary Ammonium Compounds; D016194:Receptors, N-Methyl-D-Aspartate; C012525:pyrilen; D016291:Dizocilpine Maleate; D000547:Amantadine; D010393:Pempidine; D000218:Adamantane; D008559:Memantine