半胱氨酰白三烯受体2拮抗剂筛选方法的建立及化合物初筛
Q256%Q421; 目的:建立半胱氨酰白三烯受体2(CysLT_2受体)拮抗剂筛选的细胞模型及方法,初筛系列合成化合物.方法:选用高表达CysLT_2受体的大鼠C6胶质瘤细胞,激动剂LTD_4攻击后检测细胞内钙浓度变化,作为CysLT_2受体拮抗剂的筛选方法,初步筛选有拮抗剂活性的化合物.采用CysLT1/CysLT_2受体非选择性拮抗剂Bay u9773和CysLT_2受体选择性拮抗剂AP-100984作为参照.结果:RT-PCR鉴定表明C6细胞高表达CysLT_2受体.LTD_4 1 μmol/L能显著升高C6细胞内钙,其作用约为阳性对照ATP的37 5%.CysLT_2受体拮抗剂抑制L...
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| Published in | 浙江大学学报（医学版） Vol. 38; no. 6; pp. 598 - 604 |
|---|---|
| Main Authors | , , , , , , , |
| Format | Journal Article |
| Language | Chinese |
| Published |
浙江大学医学院药理学系,浙江,杭州,310058%浙江大学药学院药物研究所,浙江,杭州,310058
2009
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| Subjects | |
| Online Access | Get full text |
| ISSN | 1008-9292 |
| DOI | 10.3785/j.issn.1008-9292.2009.06.008 |
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| Abstract | Q256%Q421; 目的:建立半胱氨酰白三烯受体2(CysLT_2受体)拮抗剂筛选的细胞模型及方法,初筛系列合成化合物.方法:选用高表达CysLT_2受体的大鼠C6胶质瘤细胞,激动剂LTD_4攻击后检测细胞内钙浓度变化,作为CysLT_2受体拮抗剂的筛选方法,初步筛选有拮抗剂活性的化合物.采用CysLT1/CysLT_2受体非选择性拮抗剂Bay u9773和CysLT_2受体选择性拮抗剂AP-100984作为参照.结果:RT-PCR鉴定表明C6细胞高表达CysLT_2受体.LTD_4 1 μmol/L能显著升高C6细胞内钙,其作用约为阳性对照ATP的37 5%.CysLT_2受体拮抗剂抑制LTD_4诱导的C6细胞内钙升高,CysLT_1受体选择性拮抗剂无抑制作用.化合物中DXW-1、2、13、23、29、30能抑制LTD_4诱导的细胞内钙升高.结论:LTD_4诱导的C6细胞的钙信号变化可作为CysLT_2受体拮抗剂的筛选方法;化合物DXW-1、2、13、23、29、30具有CysLT_2受体拮抗活性. |
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| AbstractList | Q256%Q421; 目的:建立半胱氨酰白三烯受体2(CysLT_2受体)拮抗剂筛选的细胞模型及方法,初筛系列合成化合物.方法:选用高表达CysLT_2受体的大鼠C6胶质瘤细胞,激动剂LTD_4攻击后检测细胞内钙浓度变化,作为CysLT_2受体拮抗剂的筛选方法,初步筛选有拮抗剂活性的化合物.采用CysLT1/CysLT_2受体非选择性拮抗剂Bay u9773和CysLT_2受体选择性拮抗剂AP-100984作为参照.结果:RT-PCR鉴定表明C6细胞高表达CysLT_2受体.LTD_4 1 μmol/L能显著升高C6细胞内钙,其作用约为阳性对照ATP的37 5%.CysLT_2受体拮抗剂抑制LTD_4诱导的C6细胞内钙升高,CysLT_1受体选择性拮抗剂无抑制作用.化合物中DXW-1、2、13、23、29、30能抑制LTD_4诱导的细胞内钙升高.结论:LTD_4诱导的C6细胞的钙信号变化可作为CysLT_2受体拮抗剂的筛选方法;化合物DXW-1、2、13、23、29、30具有CysLT_2受体拮抗活性. |
| Abstract_FL | Objective: To establish a method for screening cysteinyl leukotriene receptor 2 (CysLT_2) antagonists and to preliminarily screen a series of synthetic compounds. Methods: Rat glioma cell line (C6 cells) highly expressing CysLT_2 receptor was used.Intracellular calcium concentration was measured after stimulation with the agonist LTD_4,which was used to screen compounds with antagonist activity for CysLT_2 receptor.Bay u9773,a CysLT_1/CysLT_2 receptor non-selective antagonist,and AP-100984,a CysLT_2 receptor antagonist,were used as control. Results: PT-PCR showed a higher expression of CysLT_2 receptor in C6 cells.LTD_4 at 1 μmol/L significantly increased intracellular calcium in C6 cells;the maximal effect was about 37.5% of ATP,a positive stimulus.LTD_4-induced increase of intracellular calcium was blocked by CysLT_2 receptor antagonists,but not by CysLT_1 receptor antagonists.Among the synthetic compounds,DXW-1,2,13,23,29 and 30 inhibited LTD_4-induced increase of intracellular calcium. Conclusions: LTD_4-induced change in intracellular calcium in C6 cells can be used as a screening method for CysLT_2 receptor antagonists.The compounds,DXW-1,2,13,23,29 and 30,possess antagonist activity for CysLT_2 receptor. |
| Author | 魏尔清 张纬萍 蔡蓓蕾 黄雪琴 方三华 胡永洲 董晓武 卢韵碧 |
| AuthorAffiliation | 浙江大学医学院药理学系,浙江,杭州,310058%浙江大学药学院药物研究所,浙江,杭州,310058 |
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| Author_FL | HUANG Xue-qin LU Yun-bi ZHANG Wei-ping CAI Bei-lei HU Yong-zhou DONG Xiao-wu FANG San-hua WEI Er-qing |
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| DocumentTitle_FL | Method for screening cysteinyl leukotriene receptor 2 antagonists and preliminary screening of compounds |
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| Keywords | 半胱氨酰白三烯 半胱氨酸/遗传 白三烯/遗传 CysLT_2 receptor C6细胞 Calcium Cysteinyl leukotriene 钙离子 Receptors 受体 C6 cells Cysteine/genet receptor antagonist leukotriene/genet CysLT_2受体 受体拮抗剂 |
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| Title | 半胱氨酰白三烯受体2拮抗剂筛选方法的建立及化合物初筛 |
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