[PMID]: | 10834088 |
[Au] Autor: | Gmiro VE; Serdiuk SE |
[Ad] Endereço: | Anichkov Department of Neuropharmacology, Russian Academy of Medical Sciences, St. Petersburg, Russia. |
[Ti] Título: | [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]. |
[Ti] Título: | Sravnitel'noe issledovanie tsentral'nogo H-kholinoblokiruiushcheo o NMDA-blokiruiushchego deistviia MK-801, memantina, amantadina, pirilena i IEM-1754 v opytakh na intaktnykh krys.. |
[So] Source: | Eksp Klin Farmakol;63(2):16-20, 2000 Mar-Apr. |
[Is] ISSN: | 0869-2092 |
[Cp] País de publicação: | Russia (Federation) |
[La] Idioma: | rus |
[Ab] Resumo: | 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. |
[Mh] Termos MeSH primário: |
Adamantano/análogos & derivados Amantadina/farmacologia Antiparkinsonianos/farmacologia Antagonistas Colinérgicos/farmacologia Maleato de Dizocilpina/farmacologia Antagonistas de Aminoácidos Excitatórios/farmacologia Bloqueadores Ganglionares/farmacologia Memantina/farmacologia Pempidina/farmacologia Compostos de Amônio Quaternário/farmacologia Receptores de N-Metil-D-Aspartato/antagonistas & inibidores
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[Mh] Termos MeSH secundário: |
Adamantano/farmacologia Animais Anticonvulsivantes/farmacologia Relação Dose-Resposta a Droga Masculino Camundongos Limiar da Dor/efeitos dos fármacos Ratos Receptores de N-Metil-D-Aspartato/efeitos dos fármacos
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[Pt] Tipo de publicação: | COMPARATIVE STUDY; ENGLISH ABSTRACT; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T |
[Nm] Nome de substância:
| 0 (Anticonvulsants); 0 (Antiparkinson Agents); 0 (Cholinergic Antagonists); 0 (Excitatory Amino Acid Antagonists); 0 (Ganglionic Blockers); 0 (IEM 1754); 0 (Quaternary Ammonium Compounds); 0 (Receptors, N-Methyl-D-Aspartate); 6152-93-8 (pyrilen); 6LR8C1B66Q (Dizocilpine Maleate); BF4C9Z1J53 (Amantadine); N5I18JI9D6 (Pempidine); PJY633525U (Adamantane); W8O17SJF3T (Memantine) |
[Em] Mês de entrada: | 0007 |
[Cu] Atualização por classe: | 131121 |
[Lr] Data última revisão:
| 131121 |
[Sb] Subgrupo de revista: | IM |
[Da] Data de entrada para processamento: | 000602 |
[St] Status: | MEDLINE |
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