Leander S, Arner A, Johansson B
Eur J Pharmacol. 1977 Dec 15;46(4):351-61. doi: 10.1016/0014-2999(77)90229-1.
4-Aminopyridine (4-AP) increased the spontaneous mechanical activity of the isolated rat portal vein. Since denervation and adrenergic receptor blockade failed to prevent this effect of 4-AP it is suggested that the drug enhances the electrical excitability of the muscle membrane. 4-AP significantly increased the response of the muscle to electrical nerve stimulation in most experiments but had little effect on the response to applied noradrenaline (NA). Both spontaneous and evoked release of 3H-activity, following preincubation in 3H-noradrenaline, were increased in the presence of 4-AP (10(-3) M). The present results with 4-AP can be explained by its known ability to block the transient potassium conductance which accompanies the action potential in excitable tissues.
4-氨基吡啶(4-AP)增强了离体大鼠门静脉的自发机械活性。由于去神经支配和肾上腺素能受体阻断未能阻止4-AP的这种作用,提示该药物增强了肌膜的电兴奋性。在大多数实验中,4-AP显著增强了肌肉对电神经刺激的反应,但对应用去甲肾上腺素(NA)的反应影响很小。在4-AP(10⁻³ M)存在的情况下,预先在³H-去甲肾上腺素中孵育后,³H活性的自发释放和诱发释放均增加。4-AP的当前结果可以用其已知的阻断伴随可兴奋组织动作电位的瞬时钾电导的能力来解释。