Klinge E, Alaranta S, Parkkisenniemi U M, Kostiainen E, Sjöstrand N O
Department of Pharmacy, University of Helsinki, Finland.
J Pharmacol Toxicol Methods. 1993 Dec;30(4):197-202. doi: 10.1016/1056-8719(93)90017-9.
Inhibition of relaxation of strips of the bovine retractor penis muscle induced by a standard dose of nicotine (30 microM) was used for quantitative assessment of the ganglion-blocking activity of eight neuromuscular blocking agents that are in clinical use. The order of potency of the drugs studied was (+)-tubocurarine >> alcuronium > vecuronium > metocurine >> pancuronium > atracurium >>> suxamethonium > gallamine. The results have been compared to those obtained with other methods. On the basis of the present results, it is concluded that inhibition of the nicotine-induced relaxation of the bovine retractor penis muscle can be used as an alternative, sensitive in vitro method for the assessment of the ganglion-blocking activity of a neuromuscular blocking agent relative to that of, for example, (+)-tubocurarine. Earlier results have showed that this method is useful also for the assessment of the ganglion-blocking activity of other drugs, because it has yielded comparable and reproducible results at the quantitation of this property of actual ganglion-blocking and various antimuscarinic agents. In addition, this method may be useful for rapid screening of ganglion-blocking activity.
采用标准剂量尼古丁(30微摩尔)诱导的牛阴茎退缩肌条松弛抑制作用,对8种临床使用的神经肌肉阻滞剂的神经节阻断活性进行定量评估。所研究药物的效力顺序为:(+)-筒箭毒碱 >> 阿库氯铵 > 维库溴铵 > 美索卡铵 >> 泮库溴铵 > 阿曲库铵 >>> 琥珀胆碱 > 加拉明。已将结果与其他方法所得结果进行比较。根据目前的结果,得出结论:抑制尼古丁诱导的牛阴茎退缩肌松弛可作为一种替代的、灵敏的体外方法,用于评估神经肌肉阻滞剂相对于例如(+)-筒箭毒碱的神经节阻断活性。早期结果表明,该方法也可用于评估其他药物的神经节阻断活性,因为在定量实际神经节阻断剂和各种抗毒蕈碱剂的这一特性时,它产生了可比且可重复的结果。此外,该方法可能有助于快速筛选神经节阻断活性。