Vv Zakusov Research Institute Of Pharmacology Of Rams

Moscow, Russia

Vv Zakusov Research Institute Of Pharmacology Of Rams

Moscow, Russia

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Povarnina P.Y.,Vv Zakusov Research Institute Of Pharmacology Of Rams | Yarkov S.A.,Vv Zakusov Research Institute Of Pharmacology Of Rams | Gudasheva T.A.,Vv Zakusov Research Institute Of Pharmacology Of Rams | Yarkova M.A.,Vv Zakusov Research Institute Of Pharmacology Of Rams | Seredenin S.B.,Vv Zakusov Research Institute Of Pharmacology Of Rams
Acta Naturae | Year: 2015

The translocator protein (TSPO) promotes the translocation of cholesterol to the inner mitochondrial membrane and mediates steroid formation. In this study, we first report on a biological evaluation of the dipeptide GD-23 (N-carbobenzoxy-L tryptophanyl-L isoleucine amide), a structural analogue of Alpidem, the principal TSPO ligand. We show that GD-23 in a dose range of 0.05 to 0.5 mg/kg (i.p.) exhibits anxiolytic activity in the elevated plus maze test and nootropic activity in the object recognition test in scopolamine-induced amnesia in rodents. It was shown that GD-23 did not affect spontaneous locomotor activity, holding promise as a nonsedative anxiolytic agent. The anxiolytic and nootropic activities of GD-23 were abrogated by the TSPO specific ligand PK11195, which thus suggests a role for TSPO in mediating the pharmacological activity of GD-23. © 2015 Park-media, Ltd.


PubMed | Vv Zakusov Research Institute Of Pharmacology Of Rams
Type: Journal Article | Journal: Acta naturae | Year: 2015

The translocator protein (TSPO) promotes the translocation of cholesterol to the inner mitochondrial membrane and mediates steroid formation. In this study, we first report on a biological evaluation of the dipeptide GD-23 (N-carbobenzoxy-L tryptophanyl-L isoleucine amide), a structural analogue of Alpidem, the principal TSPO ligand. We show that GD-23 in a dose range of 0.05 to 0.5 mg/kg (i.p.) exhibits anxiolytic activity in the elevated plus maze test and nootropic activity in the object recognition test in scopolamine-induced amnesia in rodents. It was shown that GD-23 did not affect spontaneous locomotor activity, holding promise as a nonsedative anxiolytic agent. The anxiolytic and nootropic activities of GD-23 were abrogated by the TSPO specific ligand PK11195, which thus suggests a role for TSPO in mediating the pharmacological activity of GD-23.

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