TSPO DIPEPTIDE LIGANDS HAVING NEUROPSYCHOTROPIC ACTIVITY Russian patent published in 2021 - IPC C07K5/78 C07K5/62 A61K38/05 A61P25/22 A61P25/24 

FIELD: medicine.

SUBSTANCE: group of inventions relates to new TSPO dipeptide ligands having the range of neuropsychotropic activity. Dipeptide of the general formula R₁-X-AК₁-Y-AК₂-R₂ is proposed, where X=L or D configuration, Y=L or D configuration, АК₁=Trp or Gly, АК₂=Leu, R₁=C₆H₅-(CH₂)₂-C(O), С₆Н₅-СН₂-С(O) or CH₃-(CH₂)₄C(O), R₂=OH, OCH₃, NH₂ or NHCH₃. A pharmaceutical composition of the specified dipeptide having neuropsychotropic activity, a method for the treatment of anxiety states, and a method for the treatment of depressive states by injecting effective amount of the specified dipeptide are also proposed. Anxiolytic activity of dipeptides was identified in doses of 0.1-1.0 mg/kg, and for C₆H₅-(CH₂)₂C(O)-L-Trp-L-Leu-NH₂ – in doses of 0.01-5.00 mg/kg. Antidepressant activity for C₆H₅-(CH₂)₂C(O)-L-Trp-L-Leu-NH₂ was identified in doses of 0.01-0.05 mg/kg.

EFFECT: obtaining TSPO dipeptide ligands with neuropsychotropic activity.

13 cl, 1 dwg, 14 tbl, 10 ex