Neurotensin-like oligopeptides as potential antipsychotics: effect on dopamine system
Kost, N.V.; Meshavkin, V.K.; Batishcheva, E.I.; Sokolov, O.I.; Andreeva, L.A.; Miasoedov, N.F.
Eksperimental'naia i Klinicheskaia Farmakologiia 74(10): 3-6
2011
ISSN/ISBN: 0869-2092 PMID: 22238978 Document Number: 655865
According to published data, peptide neurotensin is considered as endogenous antipsychotic agent. A series of oligopeptides have been synthesized based on the proposed active center of neurotensin. These oligopeptides (called neurotensin-like peptides, NLPs) have been studied on behavioral models, in which the functional state of the dopamine system of animals was modified by apomorphine injections. The results of verticalization, stereotypy, and yawning tests revealed NLPs that behave as antagonists of dopamine receptors. Radioligand analysis showed that these peptides compete for specific binding to these receptors with sulpiride, which is a D2-type selective antagonist of dopamine receptors. The high degree of NLPs efficiency manifested in the behavioral tests and radioligand analysis suggests that the their antipsychotic action can be mediated by dopamine receptors.