[Neuroleptic-like activity of the tripeptide neurotensin analog GZR-123].
The neurotropic activity of GZR-123, a tripeptoid neurotensin analog was studied. It was found that the drug (0.8 mg/kg, i.p.) is capable of attenuating the apomorphine-induced climbing, stereotypy, and hyperactivity (locomotion) in mice, the apomorphine and L-DOPA induced stereotypy in rats, and the L-DOPA induced impairment of extraporatory escape in rats. The same dose neither induce myorelaxation, violated coordination of movements, and sedation, nor affected the emotional and anxiety levels. At a dose 1250 times the ED50 for apomorphine and L-DOPA dependent tests, GZR-123 did not cause acute toxicity and did not provoke catalepsy.
Guzevatykh
L S
LS
Laboratory of Psychopharmacology, Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya ul. 8, Moscow, 125315 Russia.
Ostrovskaia
R U
RU
Gudasheva
T A
TA
Zaĭtseva
N I
NI
Voronina
T A
TA
D000818:Animals; D014150:Antipsychotic Agents / Q000009:adverse effects / Q000494:pharmacology*; D001058:Apomorphine / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects*; D002375:Catalepsy / Q000139:chemically induced; D018491:Dopamine Agonists / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000494:pharmacology; D006220:Haloperidol; D007980:Levodopa / Q000494:pharmacology; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009496:Neurotensin / Q000737:chemistry* / Q000494:pharmacology; D011392:Proline / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013239:Stereotyped Behavior / Q000187:drug effects; D013469:Sulpiride / Q000494:pharmacology; D023382:Toxicity Tests, Acute; D014443:Tyrosine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*
D014150:Antipsychotic Agents; D018491:Dopamine Agonists; D018492:Dopamine Antagonists; C401484:GZR 123; D009496:Neurotensin; D014443:Tyrosine; D007980:Levodopa; D013469:Sulpiride; D011392:Proline; D006220:Haloperidol; D001058:Apomorphine