Ojewole J A
Methods Find Exp Clin Pharmacol. 1984 Feb;6(2):91-101.
The actions of diethylcarbamazine citrate (DECC) have been examined on agonist- and electrically-induced contractures and twitches of the isolated chick biventer cervicis and rat phrenic nerve-hemidiaphragm muscle preparations in order to analyse the effects of this commonly-prescribed anthelmintic drug at the neuromuscular junction. DECC (5 x 10(-1)-1.5 mM) produced a concentration-dependent initial augmentation of the indirect electrically-evoked twitches followed by a sustained, longer-lasting secondary depression of the twitches of all the skeletal muscle-nerve preparations examined. The DECC-induced twitch depression was competitively reversed by increasing the bathing fluid calcium ion concentration (Ca2+). DECC (10(-3)-2.5 x 10(-2) M) caused marked augmentation of the contractural responses of innervated chick biventer muscle preparations induced by bath-applied low concentrations of carbachol, acetylcholine or nicotine, and depressed those contractural responses of the muscle elicited by hgh concentrations of the agonists. On their own accord, high concentrations of DECC (10(-1)-2.5 mM) dose-dependently contracted isolated chick biventer cervicis muscle preparations, and demonstrated measurable anticholinesterase activity. It is concluded that DECC has both direct (post-junctional) and indirect (pre-junctional) effects at the neuromuscular junction, and that the neuromuscular blockade produced by this anthelmintic agent is probably post-junctional in origin.
为了分析这种常用驱虫药在神经肌肉接头处的作用，研究了枸橼酸乙胺嗪（DECC）对分离的鸡双腹颈肌和大鼠膈神经 - 半膈肌标本中激动剂诱导和电诱导的挛缩及抽搐的影响。DECC（5×10⁻¹ - 1.5 mM）产生浓度依赖性的间接电诱发抽搐的初始增强，随后在所检查的所有骨骼肌 - 神经标本中出现持续时间更长的继发性抽搐抑制。通过增加浴液钙离子浓度（Ca²⁺）可竞争性逆转DECC诱导的抽搐抑制。DECC（10⁻³ - 2.5×10⁻² M）使浴加低浓度卡巴胆碱、乙酰胆碱或尼古丁诱导的支配鸡双腹肌标本的挛缩反应明显增强，并抑制高浓度激动剂引起的肌肉挛缩反应。高浓度的DECC（10⁻¹ - 2.5 mM）可使分离的鸡双腹颈肌标本剂量依赖性收缩，并表现出可测量的抗胆碱酯酶活性。结论是，DECC在神经肌肉接头处具有直接（接头后）和间接（接头前）作用，并且这种驱虫药产生的神经肌肉阻滞可能起源于接头后。
