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Updated: Oct 1, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
[Neuroleptic-like activity of the tripeptide neurotensin analog GZR-123]
L S Guzevatykh1, R U Ostrovskaia, T A Gudasheva
1Laboratory of Psychopharmacology, Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya ul. 8, Moscow, 125315 Russia.
Abstract:
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.
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