Martin R E, Donahue M J
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1987;87(1):23-9. doi: 10.1016/0742-8413(87)90174-5.
Four different muscle relaxants were compared as to their effects on tonic Ascaris suum muscle to: physiological activity, intracellular response to regulatory light chain phosphorylation, and receptor pharmacology. Perfusion of Ascaris suum muscle with each relaxant, gamma-aminobutyric acid, avermectin, piperazine and chlorpromazine resulted in a dose-dependent loss of muscle tone. Comparison of intracellular effects indicated that gamma-aminobutyric acid and avermectin perfusion initiated an increase in the levels of dephosphorylated regulatory light chain while piperazine increased first site phosphorylation and chlorpromazine increased second site phosphorylation. Receptor pharmacology studies were used to compare the actions of gamma-aminobutyric acid and piperazine. It was found that bicuculline-methiodide and picrotoxin inhibited the effects of gamma-aminobutyric acid in a dose-dependent manner, but these drugs had no effect on muscle relaxation stimulated with piperazine.
比较了四种不同的肌肉松弛剂对猪蛔虫强直肌的影响，包括：生理活性、细胞内对调节性轻链磷酸化的反应以及受体药理学。用每种松弛剂（γ-氨基丁酸、阿维菌素、哌嗪和氯丙嗪）灌注猪蛔虫肌肉，导致肌张力呈剂量依赖性丧失。细胞内效应的比较表明，γ-氨基丁酸和阿维菌素灌注会使去磷酸化调节性轻链水平升高，而哌嗪会增加第一位点磷酸化，氯丙嗪会增加第二位点磷酸化。受体药理学研究用于比较γ-氨基丁酸和哌嗪的作用。发现甲磺酸荷包牡丹碱和印防己毒素以剂量依赖性方式抑制γ-氨基丁酸的作用，但这些药物对哌嗪刺激的肌肉松弛没有影响。
