细胞膜色谱法定量分析5-羟色胺受体的别构效应

发布时间：2018-07-03 17:33

本文选题：细胞膜色谱 + -羟色胺受体　；参考：《色谱》2017年02期

【摘要】：建立了大鼠纹状体细胞膜色谱法研究5-羟色胺(5-hydroxytryptamine)受体1D亚型(5-HT1D)的别构效应。利用大鼠纹状体制备得到细胞膜色谱固定相,特异性地识别混合对照品中的尼群地平、欧前胡素和藁本内酯。以不同浓度(4.62×10-7~4.62×10-5mol/L)的欧前胡素为竞争剂平衡细胞膜色谱柱,考察流动相浓度的变化对样品保留行为的影响。结果表明,欧前胡素的添加可使藁本内酯与受体作用的平衡解离常数(KD)增大2.06倍,说明欧前胡素结合5-HT1D受体后会影响藁本内酯在受体上的结合强度。在流动相中添加藁本内酯(5.26×10-7~5.26×10-5mol/L),考察欧前胡素保留因子的变化,测得藁本内酯的KD为(4.15±0.12)μmol/L,与文献报道值基本一致。该方法为定量研究受体的别构效应提供了一种全新思路。
[Abstract]:The isomorphism of 5-hydroxytryptamine (5-hydroxytryptamine) receptor 1D subtype (5-HT 1D) in rat striatum was studied by cell membrane chromatography. The chromatographic stationary phase of membrane was prepared from rat striatum, and the nitrendipine, Euglandin and ligustilide in the mixed reference substance were specifically identified. The effect of the concentration of mobile phase on the retention behavior of the samples was investigated by using different concentrations (4.62 脳 10 ~ (-7) 4.62 脳 10 ~ (-5) mol / L of Ephedrin as a competitive equilibrium cell membrane column. The results showed that the equilibrium dissociation constant (KD) of ligustilide and its receptor was increased by 2.06 times, which indicated that the binding strength of ligustilide on the receptor was affected by the binding of euglandin to 5-HT1D receptor. Ligustilide (5.26 脳 10-7 ~ 5.26 脳 10 ~ (-5) mol / L) was added to the mobile phase, and the change of the retention factor was investigated. The KD of ligustilide was (4.15 卤0.12) 渭 mol / L, which was consistent with the reported values. This method provides a new way to quantitatively study the allosteric effects of receptors.
【作者单位】：西安市食品药品检验所;
【基金】：陕西省中医药管理局科研课题(13-ZY005)~~
【分类号】：R96;O657.7

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