5-HT_(1A)受体细胞膜色谱模型的构建

Establishment of chromatography model of 5-HT_(1A)R cell membrane

目的:构建5-羟色胺1A(5-HT_(1A))受体细胞膜色谱模型并对其药物筛选能力进行考察。方法:用体外培养的T淋巴细胞,以硅胶为载体制备5-HT_(1A)受体细胞膜固定相,构建5-HT_(1A)受体细胞膜色谱模型,以5-羟色胺(5-HT)、丁螺环酮和8-羟基-丙胺-四氢萘(8-OH-DPAT)3种5-HT_(1A)受体激动剂验证该色谱模型的有效性,并以分别含有上述3种激动剂的枸杞提取液考察该模型的药物筛选能力。结果:3种激动剂在硅胶柱与细胞膜色谱模型上的色谱行为存在显著差异,利用制备的细胞膜色谱模型可以快速准确地将每种激动剂从混合溶液中筛选出来。结论:5-HT_(1A)受体细胞膜色谱模型建立成功,且具备较强的药物筛选能力,可用于特异性地筛选具有5-HT_(1A)受体结合能力的药物。

Objective： To establish 5-hydroxytryptamine 1A receptor （5-HT1AR） cell membrane chromatography （ CMC ） model and evaluate its screening ability. Methods： T lymphocytes with 5-HT1AR expression were cultured in vitro, the cell membrane stationary phase was prepared by adsorption of cell membrane suspension on silica gel to establish the CMC model. 5-HT1AR agonists [ 5-hydroxytryptamine （ 5-HT ） , buspirone, and 8-OH-DPAT ] were used to validate its effectiveness, three wolfberry extracts which contained three agonists respectively were used to investigate its drug screening ability. Results： The chromatographic behavior was significantly different between CMC model and silica column, and each agonist was screened from the mixed solution quickly and accurately. Conclusion： 5-HT1AR CMC model was established successfully with prominent screening ability and could be used to screen compounds specifically binding to 5-HT1AR.