Four 2‐(1H‐indol‐3‐yl)ethylthiourea derivatives were prepared by condensation of 2‐(1H‐indol‐3‐yl)ethanamine with the corresponding aryl/alkylisothiocyanates in a medium‐polarity solvent. Their structures were confirmed by spectral techniques, and the molecular structure of 3 was determined by X‐ray crystal analysis. For all derivatives, the binding affinities at the 5‐HT2A and 5‐HT2C receptors, as well as their functional activities at the 5‐HT1A and D2 receptors, were determined. The arylthioureas 1 and 4 were the most active at the 5‐HT1A receptor, showing, at the same time, significant selectivity over the studied 5‐HT2 and D2 receptor subtypes. The compounds were tested for their pharmacological activities within the central nervous system in relevant mouse models. The involvement of the serotonergic system in the activity of 1 and 4 was indicated. The antinociceptive action of 4 was linked to its anti‐inflammatory activity.

中文翻译：

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吲哚衍生的硫脲化合物的 G 蛋白偶联受体结合和药理学评价

通过 2-(1H-indol-3-yl) 乙胺与相应的芳基/烷基异硫氰酸酯在中等极性溶剂中缩合制备了四种 2-(1H-indol-3-yl)ethylthiourea 衍生物。通过光谱技术确认了它们的结构，通过X射线晶体分析确定了3的分子结构。对于所有衍生物，测定了对 5-HT2A 和 5-HT2C 受体的结合亲和力，以及它们对 5-HT1A 和 D2 受体的功能活性。芳基硫脲 1 和 4 对 5-HT1A 受体的活性最强，同时显示出对所研究的 5-HT2 和 D2 受体亚型的显着选择性。在相关小鼠模型中测试了这些化合物在中枢神经系统内的药理活性。表明血清素能系统参与了 1 和 4 的活动。4 的镇痛作用与其抗炎活性有关。