目的研究人类三型酸敏感离子通道(hASIC3)的生理学和药理学特性。方法应用全细胞电压钳技术检测转染在COS-7细胞上的hASIC3通道的生理学和药理学特性。结果hASIC3通道能通过迅速降低胞外pH值而被激活,并在酸性环境中迅速脱敏。脱敏后的hASIC3通道恢复到50%备用状态时所需的时间为(618±21)ms。胞外pH值在(6.40±0.05)时可使50%的hASIC3通道激活。pH值低于8时hASIC3通道的利用率降低,在生理状态pH值条件下,通道利用率降低了大约50%。阿米洛利能特异性阻断快速激活快速失活hASIC3通道且半数抑制浓度为(12.5±3.0)μmol/L。hASIC3通道的电流电压(Ⅰ-Ⅴ)关系曲线在很宽广的电压范围内呈线性关系(-80~+80mV),翻转电位为(+43±5)mV。结论hASIC3通道作为一种酸感受器,可能对感受人体pH值的变化起很重要的作用。
Objective To investigate the physiological and pharmacological characterizations of human ASIC3 (hASIC3) expressed in COS-7 cells. Methods By using cell culture, gene transfection and whole cell patch clamp technique, the characterizations of human ASIC3 (hASIC3) expressed in COS-7 cells were studied. Results hASIC3 currents were activated by changing the pH of the bathing solution and exhibited rapid desensitization upon exposure to acidic solutions; Time of 50% hASIC3 channel recovering from desensitization was (618±21) ms. Fast activated and fast inactivated hASIC3 currents were inhibited by amiloride with IC50 values of (12.5±3.0) μmol/L. In COS-7 cells the ASIC3 Ⅰ-Ⅴ relationship was linear over a wide voltage range (-80-+80 mV) and the current reversal potential was (+43±5) mV, Conclusion hASIC3 is an acid sensor and might play an important role in the detection of pH change in human.