韦那克林、他克林和毒扁豆碱对大鼠膈神经-半膈肌标本抽搐反应的比较效应。

Comparative effects of velnacrine, tacrine and physostigmine on the twitch responses in the rat phrenic-hemidiaphragm preparation.

Bosch F, Morales M, Badia A, Baños J E

Departament de Farmacologia i Psiquiatria, Facultat Medicina, Universitat Autònoma de Barcelona, Bellaterra, Spain.

Gen Pharmacol. 1993 Sep;24(5):1101-5. doi: 10.1016/0306-3623(93)90356-3.

Abstract

Cholinesterase inhibitors potentiated twitch responses induced by nerve stimulation, with physostigmine more potent than tacrine and velnacrine. However, at higher concentrations, tacrine decreased twitch responses in a concentration-dependent manner. 2. Tacrine strongly depressed directly-induced twitch responses, whereas the other drugs had minimal effects. 3. Physostigmine was the most potent drug in reversal of tubocurarine-induced blockade, but its antagonism index was similar to those obtained with tacrine and velnacrine at higher concentrations. When evaluating their ability to reverse neomycin-induced blockade, all drugs exhibited a similar effect. 4. It is concluded that tacrine and velnacrine are less potent than physostigmine in potentiating skeletal neuromuscular transmission. Additionally, the blocking effects of tacrine could limit its therapeutic efficacy.

摘要

胆碱酯酶抑制剂可增强神经刺激诱导的抽搐反应，毒扁豆碱比他克林和维那克林更有效。然而，在较高浓度下，他克林以浓度依赖的方式降低抽搐反应。2. 他克林强烈抑制直接诱导的抽搐反应，而其他药物的作用极小。3. 毒扁豆碱是逆转筒箭毒碱诱导的阻滞作用最强的药物，但其拮抗指数与较高浓度下他克林和维那克林的相似。在评估它们逆转新霉素诱导的阻滞作用的能力时，所有药物都表现出相似的效果。4. 得出的结论是，在增强骨骼肌神经肌肉传递方面，他克林和维那克林比毒扁豆碱的效力更低。此外，他克林的阻滞作用可能会限制其治疗效果。