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偏头痛是临床的常见病和多发病,研究表明,5-羟色胺(5-HT)受体在偏头痛的发病中起重要作用。实验通过大鼠纹状体组织制备得到色谱固定相,并利用细胞膜色谱与液相色谱的离线联用来特异性地识别川芎-白芷药对中可与固定相上受体相互作用的配体,发现了欧前胡素是其中潜在的活性成分。以不同浓度(2.42×10-8~4.84×10-7mol·L-1)的5-HT1D受体激动剂舒马普坦为模型药物,记录样品在模型中的容量因子,测得欧前胡素与5-HT1D受体作用的平衡解离常数为(4.59±0.33)×10-6mol·L-1,并采用硝酸甘油致大鼠偏头痛模型验证其药理活性。该研究为体外快速有效地研究药物与受体之间的相互作用提供了一种新方法。
Migraine is a common clinical disease and frequently-occurring disease, studies have shown that 5-HT (5-HT) receptors play an important role in the development of migraine. Chromatography was performed on the striatum of rats. Chromatography was performed on the striatum of rats. The ligand of Chuanxiong - Angelica Chinensis was also identified by the combination of cell membrane chromatography and liquid chromatography. Imperatorin was found to be one of the potential active ingredients. The sumatriptan 5-HT1D receptor agonist sumatriptan with different concentrations (2.42 × 10-8 ~ 4.84 × 10-7 mol·L-1) was used as a model drug and the capacity factor of the sample in the model was recorded. The equilibrium dissociation constants of the 5-HT1D receptor were (4.59 ± 0.33) × 10-6 mol·L-1. The pharmacological activities of the migraine model were validated by nitroglycerin. This study provides a new method for the rapid and effective study of drug-receptor interaction in vitro.