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• W2039949587 abstract "Novel N,N-disubstituted indol-3-ylglyoxylamides (1−56), bearing different combinations of substituents R1−R5, were synthesized and evaluated as ligands of the translocator protein (TSPO), the 18 kDa protein representing the minimal functional unit of the “peripheral-type benzodiazepine receptor” (PBR). Most of the new compounds showed a nanomolar/subnanomolar affinity for TSPO and stimulated steroid biosynthesis in rat C6 glioma cells with a potency similar to or higher than that of classic TSPO ligands such as PK 11195. Moreover, when evaluated in vivo by means of the elevated-plus-maze (EPM) paradigm in the rat, compound 32, the best-performing derivative in terms of TSPO affinity and pregnenolone production, showed clear anxiolytic effects. The results of this study suggested that the novel N,N-disubstituted indol-3-ylglyoxylamides may represent a promising class of compounds potentially suited for the treatment of anxiety disorders." @default.
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• W2039949587 date "2008-08-26" @default.
• W2039949587 modified "2023-09-26" @default.
• W2039949587 title "Anxiolytic-like Effects of <i>N</i>,<i>N</i>-Dialkyl-2-phenylindol-3-ylglyoxylamides by Modulation of Translocator Protein Promoting Neurosteroid Biosynthesis" @default.
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• W2039949587 doi "https://doi.org/10.1021/jm8003224" @default.
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