吡啶基和哌啶基1,3 -二氧戊环衍生物对神经肌肉传递影响的研究。

An investigation of the effects of a pyridyl and a piperidyl 1, 3-dioxolane derivative on neuromuscular transmission.

作者信息

Pinson R A, Dretchen K L, Kruger G O

出版信息

Arch Int Pharmacodyn Ther. 1976 Jan;219(1):52-63.

Abstract

2-(4'-pyridyl)-1,3-dioxolane methiodide (KCL-301-14) and 2-(1'-methyl-4' piperidyl)-1,3-dioxolane hydroiodide (KCL-301-39) facilitated the force of contraction in low doses and blocked it in higher doses in the in vivo cat soleus muscle preparation. Both drugs in the cat also reversed d-tubocurarine and succinylcholine blockade, produced post-drug repetitive activity, blocked post-tetanic potentiation (PTP), had no direct muscle affect and reversed the PTP suppression caused by d-tubocurarine and succinylcholine. In the rat phrenic nerve-diaphragm and the chick biventer cervicis preparations in vitro, facilitation, then blockade of the contraction were seen as concentrations increased. However, KCL-301-14 reversed d-tubocurarine and increased succinylcholine blockades in the rat and chick. KCl-301-39 increased both d-tubocurarine and succinylcholine blockades in the rat and chick. The different effects seen in the cat vs. the rat and chick with these drugs are probably due to species variation.

摘要

2-(4'-吡啶基)-1,3-二氧戊环甲碘化物（KCL-301-14）和2-(1'-甲基-4'-哌啶基)-1,3-二氧戊环氢碘化物（KCL-301-39）在低剂量时促进体内猫比目鱼肌的收缩力，而在高剂量时则阻断收缩力。在猫体内，这两种药物还能逆转筒箭毒碱和琥珀酰胆碱的阻断作用，产生药物后重复活动，阻断强直后增强（PTP），对肌肉无直接影响，并能逆转由筒箭毒碱和琥珀酰胆碱引起的PTP抑制。在体外大鼠膈神经-膈肌和鸡双颈肌制备中，随着浓度增加，先出现收缩力增强，随后出现收缩力阻断。然而，KCL-301-14能逆转大鼠和鸡体内筒箭毒碱的作用，并增强琥珀酰胆碱的阻断作用。KCl-301-39能增强大鼠和鸡体内筒箭毒碱和琥珀酰胆碱的阻断作用。这些药物在猫与大鼠和鸡身上产生的不同效应可能是由于物种差异。