Baker T, Aguero A, Stanec A, Lowndes H E
Anesthesiology. 1986 Nov;65(5):480-4. doi: 10.1097/00000542-198611000-00005.
This study explored the prejunctional actions of vecuronium using the in vivo cat soleus nerve-muscle preparation. Vecuronium doses of 1 to 5 micrograms/kg iv suppressed the repetitive firing of the motor nerve endings, and the obligatory potentiation of the twitch response following high-frequency conditioning at 400 Hz for 10 s without attenuating neuromuscular transmission at 0.4 Hz. It was also found that extremely low doses of vecuronium had excitatory effects at the cat soleus motor nerve endings: doses of 0.5 and 1 microgram/kg iv evoked a modest postdrug repetitive firing of the nerve endings and a concomitant potentiation of the muscle responses. These dose-related agonist and antagonist activities suggest that at the motor nerve endings, vecuronium is a weak partial agonist. The major action of vecuronium at the motor nerve endings, however, was suppressive, and this antagonist action contributed to the neuromuscular blocking action of this muscle relaxant.
本研究利用体内猫比目鱼肌神经-肌肉标本探讨了维库溴铵的接头前作用。静脉注射1至5微克/千克的维库溴铵剂量可抑制运动神经末梢的重复放电,并且在400赫兹高频条件刺激10秒后,单收缩反应的必然增强,而在0.4赫兹时不减弱神经肌肉传递。还发现极低剂量的维库溴铵对猫比目鱼肌运动神经末梢有兴奋作用:静脉注射0.5和1微克/千克的剂量可引起给药后神经末梢适度的重复放电以及肌肉反应的相应增强。这些与剂量相关的激动剂和拮抗剂活性表明,在运动神经末梢,维库溴铵是一种弱部分激动剂。然而,维库溴铵在运动神经末梢的主要作用是抑制性的,这种拮抗剂作用促成了这种肌肉松弛剂的神经肌肉阻滞作用。