以组胺受体3为靶点的高通量药物筛选细胞模型的建立
Establishment of high-throughput drug screening modeltargeting human histamine receptor 3 in cell
目的 建立稳定表达组胺受体3（hH3R445）和Ga15蛋白的高通量药物筛选细胞模型，通过FlexStation工作平台，可应用该细胞模型筛选治疗失眠、精神分裂和老年痴呆症等中枢神经系统性疾病的药物先导化合物。方法 用分子生物学的方法，亚克隆得到组胺受体3基因和Ga15基因。将体外培养的HEK-293细胞株用Ga15基因重组质粒进行稳定转染，得到稳定表达Ga15蛋白的母细胞系，然后在母细胞系中稳定转染组胺受体3基因重组质粒，筛选得到稳定表达组胺受体3和Ga15蛋白的细胞模型，并对所建立的筛选细胞模型进行功能性检测。结果 建立了稳定、高效的高通量药物筛选细胞模型。结论 建立的细胞模型可以应用于以组胺受体3为靶点的高通量药物筛选。
im To screen new drug for the treatment of insomnia, schizophrenia, Alzheimer’s disease and other central nerve system’s disorder, high-throughput drug screening cell model which were transfected with human histamine receptor 3 gene（hH3R445）and Ga15 gene, and were detected by FlexStation have been established. Methods we obtained histamine receptor 3 gene and Ga15 gene by subclone. We transfected HEK-293 cell with Ga15 gene, gained HEK-293- Ga15 parental cell line which stable expressing Ga15 protein, and subsequently parental cell line was stable transfected with human histamine receptor 3 gene. Cell clones expressing of histamine receptor 3 gene（hH3R445）and Ga15 gene were selected by antibiotics screening. Then we made different ligands dose response curves on the cell model. Results A high throughput screening cell model with stable, good reproducibility has been established. Conclusion This drug screening cell model can be used for histamine receptor 3 target high-throughput drug screening.
尹琪、张以琳、蒋亚琴、刘红茹
药学基础医学神经病学、精神病学
组胺受体3，细胞模型，高通量药物筛选
histamine receptor 3cell model high-throughput screening
尹琪,张以琳,蒋亚琴,刘红茹.以组胺受体3为靶点的高通量药物筛选细胞模型的建立[EB/OL].(2006-01-19)[2025-08-18].http://www.paper.edu.cn/releasepaper/content/200601-235.点此复制
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