Gudasheva T A, Deeva O A, Yarkova M A, Seredenin S B
Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences, ul. Baltiiskaya 8, Moscow, 125315, Russia.
Dokl Biochem Biophys. 2016 Jul;469(1):298-301. doi: 10.1134/S1607672916040165. Epub 2016 Sep 7.
The elevated plus maze test showed that GD-23 (N-carbobenzoxy-L-tryptophanyl-L-isoleucine amide), an original dipeptide ligand of TSPO, exerted anxiolytic effect when injected intraperitoneally at a dose of 0.5 mg/kg. This effect was completely blocked by the selective neurosteroid synthesis inhibitors, enzymes trilostane and finasteride. The same inhibitors do not prevent the anxiolytic effects of the benzodiazepine tranquillizer diazepam. The results of the study indicate the selective neurosteroidogenic mechanism of the anxiolytic action of GD-23.
高架十字迷宫试验表明,TSPO的原始二肽配体GD-23(N-苄氧羰基-L-色氨酰-L-异亮氨酸酰胺)以0.5mg/kg的剂量腹腔注射时具有抗焦虑作用。这种作用被选择性神经甾体合成抑制剂曲洛司坦和非那雄胺完全阻断。同样的抑制剂并不能阻止苯二氮䓬类镇静剂地西泮的抗焦虑作用。研究结果表明GD-23抗焦虑作用的选择性神经甾体生成机制。