Serotonin (5-HT) receptors are important in health and disease, but the existence of 14 subtypes necessitates selective ligands. Previously, the pulicatins were identified as ligands that specifically bound to the subtype 5-HT_2B in the 500 nM to 10 μM range and that exhibited in vitro effects on cultured mouse neurons. Here, we examined the structure–activity relationship of 30 synthetic and natural pulicatin derivatives using binding, receptor functionality, and in vivo assays. The results reveal the 2-arylthiazoline scaffold as a tunable serotonin receptor-targeting pharmacophore. Tests in mice show potential antiseizure and antinociceptive activities at high doses without motor impairment.

中文翻译：

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调节普利他汀天然产物的5-羟色胺受体光谱

5-羟色胺（5-HT）受体在健康和疾病中很重要，但是14种亚型的存在需要选择性配体。以前，普利卡汀被鉴定为在500 nM至10μM范围内特异性结合亚型5-HT _2B的配体，并且对培养的小鼠神经元表现出体外作用。在这里，我们使用结合，受体功能和体内测定法研究了30种合成和天然普利他汀衍生物的结构-活性关系。结果表明2-芳基噻唑啉支架是靶向5-羟色胺受体的可调药效团。小鼠试验显示，大剂量无运动损伤时具有潜在的抗癫痫和抗伤害感受活性。