[Dilept: a tripeptoid neurotensin analog combining neuroleptic activity with positive mnemotropic action].
The effect of N-caproyl-L-prolyl-L-tyrosine methyl ester (GZR-123, Dilept), a new antipsychotic drug with a dipeptide structure, on cognitive functions was studied using the passive avoidance conditioned reflex (PACR) test. It was found that the drug improved both the acquisition and retrieval of PACR under the conditions of undertraining and prevented the amnesic effect of transcorneal electroshock. The neurotransmitter analysis of these effects using the corresponding blockers showed the ability of dilept to facilitate the central glutamatergic (NMDA type) and cholinergic (of both muscarine and nicotine types) neurotransmission. No evidence of the involvement of the GABAergic system was observed. The experimental data on the combination of antipsychotic effect with memory improving activity suggests that dilept may be effective in cases of negative symptoms of schizophrenia and psychotic manifestations in Alzheimer disease.
Ostrovskaia
R U
RU
Retiunskaia
M V
MV
Guzevatykh
L S
LS
Gudasheva
T A
TA
Voronina
T A
TA
Seredin
S B
SB
D000544:Alzheimer Disease / Q000188:drug therapy; D000818:Animals; D014150:Antipsychotic Agents / Q000008:administration & dosage*; D001362:Avoidance Learning / Q000187:drug effects; D001522:Behavior, Animal / Q000187:drug effects*; D008297:Male; D009496:Neurotensin / Q000008:administration & dosage / Q000031:analogs & derivatives*; D011392:Proline / Q000008:administration & dosage* / Q000031:analogs & derivatives*; D051381:Rats; D012559:Schizophrenia / Q000188:drug therapy; D015398:Signal Transduction / Q000187:drug effects*; D014443:Tyrosine / Q000008:administration & dosage* / Q000031:analogs & derivatives*
D014150:Antipsychotic Agents; C401484:GZR 123; D009496:Neurotensin; D014443:Tyrosine; D011392:Proline