EVANS E R, WILSON H
Br J Pharmacol Chemother. 1964 Jun;22(3):441-52. doi: 10.1111/j.1476-5381.1964.tb01699.x.
Hemicholinium No. 3 (HC-3; alpha,alpha'-dimethylaminoethanol-4, 4'-biacetophenone) produced neuromuscular block of the tibialis anterior muscle-sciatic nerve preparation of the anaesthetized cat which was of slow onset, of long duration and dependent on the nerve stimulus frequency. The failure of the compound to modify the response of the tibialis muscle to close-arterial injections of acetylcholine suggested that the sensitivity of the motor endplate was not changed by it. The neuromuscular block produced by hemicholinium was antagonized by choline but only partly relieved by anticholinesterase drugs. The response to tetanic stimulation of the nerve during the neuromuscular block was well sustained and was followed by a slight posttetanic potentiation. The neuromuscular blocking action of hemicholinium could be relieved by temporary suspension of stimulation. These results suggest that the mode of action of hemicholinium at the neuromuscular junction is different from that of tubocurarine, and indicate that the action of hemicholinium is presynaptic, probably arising from a reduction in acetylcholine released by nerve stimulation.
3号半胆碱(HC - 3;α,α'-二甲基氨基乙醇 - 4,4'-二乙酰苯)可使麻醉猫的胫前肌 - 坐骨神经标本产生神经肌肉阻滞,其起效缓慢、持续时间长且依赖于神经刺激频率。该化合物未能改变胫前肌对动脉内注射乙酰胆碱的反应,这表明运动终板的敏感性并未因它而改变。半胆碱产生的神经肌肉阻滞可被胆碱拮抗,但仅被抗胆碱酯酶药物部分缓解。在神经肌肉阻滞期间,对神经强直刺激的反应维持良好,随后有轻微的强直后增强。半胆碱的神经肌肉阻滞作用可通过暂时停止刺激而解除。这些结果表明,半胆碱在神经肌肉接头处的作用方式与筒箭毒碱不同,表明半胆碱的作用是突触前的,可能源于神经刺激释放的乙酰胆碱减少。