Dipartimento NEUROFARBA, Sezione Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Italy.
Dipartimento NEUROFARBA, Sezione Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Italy.
Bioorg Med Chem. 2018 May 15;26(9):2475-2487. doi: 10.1016/j.bmc.2018.04.011. Epub 2018 Apr 4.
A comparison between compounds with pyrazolo[1,5-a]pyrimidine structure (series 4-6) and pyrazolo[5,1-c][1,2,4]triazine core (series 9) as ligands at GABA-receptor subtype, was evaluated. Moreover, for pyrazolotriazine derivatives having binding recognition, the interaction on recombinant rat α(1-3,5) GABA receptor subtypes, was performed. Among these latter, emerge compounds 9c, 9k, 9l, 9m and 9n as α1-selective and 9h as α2-selective ligands.
对具有吡唑并[1,5-a]嘧啶结构(系列 4-6)和吡唑并[5,1-c][1,2,4]三嗪核心(系列 9)的化合物作为 GABA 受体亚型配体进行了比较。此外,对于具有结合识别能力的吡唑并三嗪衍生物,在重组大鼠 α(1-3,5)GABA 受体亚型上进行了相互作用。在这些化合物中,出现了化合物 9c、9k、9l、9m 和 9n 作为 α1 选择性配体,而 9h 作为 α2 选择性配体。