title: Central effects of SL 82.0715, an antagonist of polyamine site of the NMDA receptor complex.
abstract: Central effects of SL 82.0715, an antagonist of polyamine site of the NMDA receptor complex, was studied in male Albino-Swiss mice. SL 82.0715, in doses which given alone were inactive in electroshock-induced seizures, potentiated the anticonvulsant effects of CGP 37849. In normal mice, SL 82.0715 decreased the spontaneous locomotor activity, did not affect the locomotor hyperactivity induced by MK-801 and attenuated CGP 37849-induced locomotor hyperactivity. The D-amphetamine locomotor hyperactivity was also antagonized by SL 82.0715. SL 82.0715 did not significantly change the locomotor activity in monoamine-depleted mice (treated with reserpine + alpha-methyl-p-tyrosine). When administered together with clonidine, SL 82.0715 increased the locomotor activity in monoamine-depleted mice but this effect did not reach the level of statistical significance. SL 82.0715 did not change the locomotor activity induced by joint administration of clonidine and MK-801 or clonidine and CGP 37849, in monoamine-depleted mice. The locomotor hyperactivity evoked by L-DOPA (given jointly with benserazide) was not changed by SL 82.0715. SL 82.0715 had no effect on fluphenazine- and haloperidol-induced catalepsy in mice. CGP 37849 attenuated catalepsy induced by haloperidol; that effect was not changed by SL 82.075. The studied compound did not affect the immobility time and had no effect on the action of MK-801 or CGP 37849 in the forced swimming test. The obtained results indicate that SL 82.0715 has a different pharmacological profile than other NMDA antagonists (at least MK-801 and CGP 37849). SL 82.0715 does not increase behavioral actions of MK-801 and CGP 37849, potentiating anticonvulsant effect of CGP 37849 only.
authors.affiliation: Institute of Pharmacology, Polish Academy of Sciences, Kraków.
authors.forename: A
authors.initials: A
authors.lastname: Dereń-Wesołek
authors.forename: J
authors.initials: J
authors.lastname: Maj
mesh_terms: D015763:2-Amino-5-phosphonovalerate / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology; D014150:Antipsychotic Agents; D015306:Biogenic Monoamines / Q000502:physiology; D015317:Biogenic Polyamines / Q000737:chemistry / Q000378:metabolism*; D002375:Catalepsy / Q000139:chemically induced; D003000:Clonidine / Q000494:pharmacology; D003913:Dextroamphetamine / Q000494:pharmacology; D016291:Dizocilpine Maleate / Q000494:pharmacology; D004597:Electroshock; D007980:Levodopa / Q000494:pharmacology; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010880:Piperidines / Q000494:pharmacology*; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects / Q000378:metabolism*; D012640:Seizures / Q000517:prevention & control; D013550:Swimming
chemical_list: D000927:Anticonvulsants; D014150:Antipsychotic Agents; D015306:Biogenic Monoamines; D015317:Biogenic Polyamines; D010880:Piperidines; D016194:Receptors, N-Methyl-D-Aspartate; C064539:2-amino-4-methyl-5-phosphono-3-pentenoic acid; D007980:Levodopa; D016291:Dizocilpine Maleate; D015763:2-Amino-5-phosphonovalerate; D003000:Clonidine; D003913:Dextroamphetamine; C058083:eliprodil