Hardy S P, deFelipe C, Valverde M A
Department of Pharmacy, University of Brighton, UK.
FEBS Lett. 1998 Sep 4;434(3):236-40. doi: 10.1016/s0014-5793(98)00974-0.
The effect of the non-steroidal antioestrogens tamoxifen and toremifene on voltage-gated cationic currents was examined in primary cultures of rat hypothalamic neurones and the C1300 mouse neuroblastoma cell line using the whole-cell patch clamp technique. When applied to the external bathing solution both tamoxifen and toremifene were able to inhibit TTX-sensitive sodium currents with IC50 values of 1-2 microM and delayed rectifier type potassium currents (IC50, 2-3 microM). However, only toremifene showed a significant inhibition of the I(A) current (IC50 3 microM). Inhibition of voltage-gated cationic currents was significantly impaired when tamoxifen was applied in a serum-containing solution. The steroidal antioestrogen ICI 182,780 did not inhibit any of the currents at 10 microM.
使用全细胞膜片钳技术，在大鼠下丘脑神经元原代培养物和C1300小鼠神经母细胞瘤细胞系中检测了非甾体类抗雌激素他莫昔芬和托瑞米芬对电压门控阳离子电流的影响。当将他莫昔芬和托瑞米芬应用于细胞外浴液时，二者均能够抑制TTX敏感的钠电流，IC50值为1 - 2微摩尔，同时也能抑制延迟整流型钾电流（IC50为2 - 3微摩尔）。然而，只有托瑞米芬对I(A)电流表现出显著抑制作用（IC50为3微摩尔）。当在含血清的溶液中应用他莫昔芬时，电压门控阳离子电流的抑制作用明显受损。甾体类抗雌激素ICI 182,780在10微摩尔时不抑制任何电流。
