Minakuchi C, Itoh H
Department of Anesthesiology, School of Medicine, Juntendo University, Tokyo.
Masui. 1991 Aug;40(8):1204-9.
With regard to the inhibition of contractility, dose-response curves of ryanodine and nickel were produced, and in these curves ID50 values were 10(-6) M and 2 x 10(-3) M, respectively. ID50 of bupivacaine was similar to ryanodine's and that of lidocaine was between ryanodine and nickel. On the post-rest potentiation (PRP) elicited after 2 s of rest following a train of stimulation at 3 Hz, ryanodine and bupivacaine had similar depressing effects, but lidocaine depressed it moderately and nickel showed no effect. These results suggest that bupivacaine could cause a direct inhibitory effect on sarcoplasmic reticulum (SR) function like ryanodine, but lidocaine could cause mainly a reduction in trans-sarcolemmal Ca influx and induce a slight inhibitory effect on SR function.
关于收缩性的抑制，绘制了ryanodine和镍的剂量-反应曲线，在这些曲线中，半数抑制剂量（ID50）值分别为10⁻⁶ M和2×10⁻³ M。布比卡因的ID50与ryanodine相似，利多卡因的ID50介于ryanodine和镍之间。在3 Hz的一串刺激后休息2 s所引发的后休息增强（PRP）方面，ryanodine和布比卡因具有相似的抑制作用，但利多卡因对其有中度抑制作用，而镍则无作用。这些结果表明，布比卡因可能像ryanodine一样对肌浆网（SR）功能产生直接抑制作用，但利多卡因可能主要导致跨肌膜钙内流减少，并对SR功能产生轻微抑制作用。
