Анксиолитическое действие оригинальных производных пирроло[1,2- a ]пиразина, лигандов TSPO, зависит от биосинтеза нейростероидов
2016
Investigation of original derivatives of pyrrolo[1,2- a ]pyrazine representing ligands of 18 kDa translocator protein (TSPO) revealed compounds with high TSPO affinity and pronounced anxiolytic activity, in particular, N-benzyl-N-methyl-1-phenylpyrrolo[1,2- a ]pyrazin-3-carboxamide (GML-1) and N-butyl-N-methyl-1-phenylpyrrolo[1,2- a ]pyrazin-3-carboxamide (GML-3). In the elevated plus maze test, the anxiolytic effect of GML-1 and GML-3 was completely blocked by neurosteroidogenic enzyme inhibitors trilostane and finasteride.
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