[Glutamate receptor antagonists attenuate experimental catalepsy in rats].
A long-term akinesia induced by haloperidol used as an experimental model of catalepsy helped to reveal that a dicationic derivatives adamantane (IEM-1754) and phenylcyclohexyl (IEM-1925) exerted different degrees of inhibition of the haloperidol effect: the IEM-1754 proved to be not inferior to the most effective NMDA antagonist MK-801. A relatively low potency of the IEM-1925 may be due to its obvious equal effects both on the NMDA and the AMPA receptor channels. A good correlation between the anticataleptic effects of the glutamate antagonists and the NMDA receptor blocking activity, were found. The AMPA receptor blockade might negatively affect the anticataleptic potency of the drugs under study.
Rukoiatkina
N I
NI
I. M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Acad. Sci., St. Petersburg, Russia.
Gorbunova
L V
LV
Gmiro
V E
VE
Lukomskaia
N Ia
NIa
D000218:Adamantane / Q000009:adverse effects / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D014150:Antipsychotic Agents; D001259:Ataxia / Q000139:chemically induced; D002375:Catalepsy / Q000139:chemically induced / Q000517:prevention & control*; D003959:Diamines / Q000009:adverse effects / Q000494:pharmacology; D016291:Dizocilpine Maleate / Q000009:adverse effects / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D018691:Excitatory Amino Acid Antagonists / Q000009:adverse effects / Q000494:pharmacology*; D006220:Haloperidol; D000644:Quaternary Ammonium Compounds / Q000009:adverse effects / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013239:Stereotyped Behavior / Q000187:drug effects
D014150:Antipsychotic Agents; D003959:Diamines; D018691:Excitatory Amino Acid Antagonists; C092754:IEM 1754; C406748:IEM 1925; D000644:Quaternary Ammonium Compounds; D016291:Dizocilpine Maleate; D006220:Haloperidol; D000218:Adamantane