氨基吡啶对猫非去极化神经肌肉阻滞的拮抗作用

Antagonism of non-depolarising neuromuscular blockade by aminopyridines in cats.

作者信息

Riesz M, Kápáti E, Szporny L

出版信息

J Pharm Pharmacol. 1986 Feb;38(2):156-8. doi: 10.1111/j.2042-7158.1986.tb04535.x.

DOI:10.1111/j.2042-7158.1986.tb04535.x

Abstract

The antagonism of pipecuronium- and vecuronium-induced neuromuscular blockade by 4-aminopyridine (4AP), 3,4-diaminopyridine (3,4AP) and 3-[(dimethylamino)-carbonyl] amino-4-aminopyridine (LF14) were studied in anaesthetized cats during constant infusion of the relaxants. Aminopyridines were administered cumulatively at steady state 90% block level. The ED50 values of 4AP, 3,4AP and LF14 were 243, 106 and 254 micrograms kg-1 in pipecuronium, and 232, 195 and 235 micrograms kg-1 in vecuronium blockade. It has been assumed that in cats the anticurare effect of aminopyridines is mainly a result of K+ channel blockade on motor nerve terminals which enhances the evoked release of acetylcholine.

摘要

在麻醉猫持续输注哌库溴铵和维库溴铵期间，研究了4-氨基吡啶（4AP）、3,4-二氨基吡啶（3,4AP）和3-[(二甲氨基)-羰基]氨基-4-氨基吡啶（LF14）对它们所致神经肌肉阻滞的拮抗作用。氨基吡啶在稳态90%阻滞水平时进行累积给药。4AP、3,4AP和LF14对哌库溴铵所致阻滞的ED50值分别为243、106和254微克/千克，对维库溴铵所致阻滞的ED50值分别为232、195和235微克/千克。据推测，在猫中氨基吡啶的抗箭毒作用主要是运动神经末梢钾通道阻滞的结果，这增强了乙酰胆碱的诱发释放。