【摘要】 目的:探索阿米洛利类化合物与α2C-AR的作用位点及别构调节作用。方法:采用分子对接方法,预测阿米洛利类化合物与α2C-AR的潜在结合位点;采用受体表达实验检测α2C-AR的活性及表达量;通过配体受体解离动力学实验检测阿米洛利类化合物对3H-RX821002解离速度的影响。结果:阿米洛利的作用位点包括Glu377和Phe380;Benzamil的作用位点包括Asn160和Thr241。阿米洛利和Benzamil对3H-RX821002的解离速度均没有影响。结论:阿米洛利和Benzamil对α2C-AR不具有别构调节作用。更多还原

【Abstract】 Objective: To explore the interacting sites and the allosteric effects of amiloride derivatives on α2 C-AR. Methods: Molecular docking was used to predict the potential interacting sites. Receptor expression assay was performed to detect the activity and expression of α2 C-AR. Dissociation kinetics assay was used to evaluate the effect of amiloride derivatives on the dissociation rate of 3 H-RX821002. Results: The interacting sites between amiloride and α2 C-AR inluded Glu377 and Phe380. The interacting sites between Benzamil and α2 C-AR were Asn160 and Thr241. Amiloride and Benzamil had no effect on the dissociation rate of 3 H-RX821002. Conclusion: Both Amiloride and Benzamil have no allosteric effect on α2 C-AR.更多还原