KLE Academy of Higher Education and Research, College of Pharmacy, II-Block Rajajinagar, Bangalore 560010, Karnataka, India.
Steroids. 2010 Apr;75(4-5):323-9. doi: 10.1016/j.steroids.2010.01.009. Epub 2010 Jan 25.
The interonium distance plays a major role in neuromuscular blocking activity of bis-quaternary ammonium compounds. In this study we tried to alter the distance between two quaternary nitrogens in some of the steroidal derivatives synthesized and evaluated them for neuromuscular blocking activity using in vivo (in chicks) and in vitro models (rectus abdominus and chick biventer cervis muscle) for their mechanism of action. All the synthesized compounds have shown to possess good depolarizing, competitive neuromuscular blocking activity, particularly the 17-acetoxy derivative and the increase in the distance between two quaternary nitrogens decreased the activity.
季铵间隔在双季铵类化合物的神经肌肉阻滞活性中起着重要作用。在这项研究中，我们试图改变一些甾体衍生物中两个季铵氮之间的距离，并使用体内（小鸡）和体外（直肌和小鸡双颈肌）模型评估它们的神经肌肉阻滞活性，以研究其作用机制。所有合成的化合物都表现出良好的去极化、竞争性神经肌肉阻滞活性，特别是 17-乙酰氧基衍生物，而两个季铵氮之间距离的增加则降低了活性。
