Diadiusha G P, Tugaĭ V A, Zemlianaia N N
Ukr Biokhim Zh (1978). 1988 May-Jun;60(3):52-6.
The initial fast phase of Ca2+ efflux from vesicles of sarcoplasmic reticulum (SR) loaded with Ca2+ passively or in ATP-dependent process and the initial fast phase of Ca2+ influx into the SR vesicles are inhibited by 0.5 mM tetracaine. The inhibitory action of tetracaine observed both with the heavy and light SR fractions is competitive with Ca2+, decreased with varying pH from 5.8 to 7.8 and temperature from 20 degrees C to 37 degrees C. Choline chloride in the concentration of 150 mM at 37 degrees C prevents the inhibitory action of tetracaine. It is supposed that electrostatic interaction plays an essential role in tetracaine-inhibition of passive Ca2+ fluxes through the membrane.
0.5 mM的丁卡因可抑制通过被动方式或ATP依赖过程装载Ca2+的肌浆网(SR)囊泡中Ca2+外流的初始快速阶段以及Ca2+流入SR囊泡的初始快速阶段。在重质和轻质SR组分中均观察到丁卡因的抑制作用,该作用与Ca2+具有竞争性,随pH从5.8变化至7.8以及温度从20℃变化至37℃而降低。37℃时浓度为150 mM的氯化胆碱可防止丁卡因的抑制作用。据推测,静电相互作用在丁卡因抑制Ca2+通过膜的被动通量中起重要作用。