[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].

Abstract

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.

• Authors: V E Gmiro, S E Serdiuk
• Journal: Eksperimental'naia i klinicheskaia farmakologiia (Eksp Klin Farmakol) Vol. 63 Issue 2 Pg. 16-20 ( 2000) ISSN: 0869-2092 [Print] Russia (Federation)
• Vernacular Title: Sravnitel'noe issledovanie tsentral'nogo H-kholinoblokiruiushcheo o NMDA-blokiruiushchego deĭstviia MK-801, memantina, amantadina, pirilena i IEM-1754 v opytakh na intaktnykh krys.
• PMID: 10834088 (Publication Type: Comparative Study, English Abstract, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anticonvulsants
• Antiparkinson Agents
• Cholinergic Antagonists
• Excitatory Amino Acid Antagonists
• Ganglionic Blockers
• IEM 1754
• Quaternary Ammonium Compounds
• Receptors, N-Methyl-D-Aspartate
• pyrilen
• Dizocilpine Maleate
• Amantadine
• Pempidine
• Adamantane
• Memantine

Topics

• Adamantane (analogs & derivatives, pharmacology)
• Amantadine (pharmacology)
• Animals
• Anticonvulsants (pharmacology)
• Antiparkinson Agents (pharmacology)
• Cholinergic Antagonists (pharmacology)
• Dizocilpine Maleate (pharmacology)
• Dose-Response Relationship, Drug
• Excitatory Amino Acid Antagonists (pharmacology)
• Ganglionic Blockers (pharmacology)
• Male
• Memantine (pharmacology)
• Mice
• Pain Threshold (drug effects)
• Pempidine (pharmacology)
• Quaternary Ammonium Compounds (pharmacology)
• Rats
• Receptors, N-Methyl-D-Aspartate (antagonists & inhibitors, drug effects)