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目的 :建立M1受体筛选模型 ,用于抗早老性痴呆药物的筛选。方法 :在人胚肾细胞上表达人源M1受体 ,通过检测胞内cAMP来监测受体的激动情况。使用外源性的3H cAMP竞争胞内的cAMP结合位点。使用氯化乙酰胆碱作为阳性药来确证模型的可靠性。结果 :初步建立了M1受体人胚肾细胞表达体系。使用不同浓度的氯化乙酰胆碱 (10 -9～ 10 -4mol/L) ,胞内的cAMP浓度有相关性变化 (10 3 43× 10 -4 ～ 3 3 75 4× 10 -4 pmol/ μl)。 结论 :本筛选模型对M1受体激动剂有阳性反应 ,可用于抗早老性痴呆药物的筛选
Objective: To establish a M1 receptor screening model for the screening of anti-Alzheimer’s drugs. METHODS: Human M1 receptor was expressed on human embryonic kidney cells and receptor agonist activity was monitored by measuring intracellular cAMP. Exogenous 3H cAMP is used to compete for intracellular cAMP binding sites. Acetylcholine is used as a positive drug to confirm the reliability of the model. Results: The M1 receptor human embryonic kidney cell expression system was initially established. The intracellular concentration of cAMP correlated with the concentration of 10 -9 ~ 10 -4 mol / L with different concentrations of acetylcholine (10 3 43 × 10 -4 ~ 3 3 75 4 × 10 -4 pmol / μl). Conclusion: This screening model has a positive response to M1 receptor agonist, which can be used in the screening of anti-Alzheimer’s drug