Grechishkin L L, Krasnova E I, Indenbom M L
Farmakol Toksikol. 1979 Jul-Aug;42(4):362-5.
In experiments on the cat neuromuscular preparation the authors investigated the anticurare action of the new compound IEM-931 having sulphonate-anionic groups 20 A apart. The new compound administered in a dose of 184 mkM/kg prevents and removes the curare effect of rythetronium which is its structural analogue. Regarding tubocurarine the antagonism is displayed, however, only from the dose of 384 mkM/kg. This indicates that efficacy of the anticurare action of IEM-931 is directly related to complimentarity of the interacting molecule structure. The experiment with regional relaxation of the cat muscles shows that the anticurare action of IEM-931 is realized both in the blood and on the cholinoreceptor. Moreover, as a result of molecular interaction the inactive complex is formed.
在对猫神经肌肉制剂进行的实验中,作者研究了具有间隔20埃磺酸根阴离子基团的新化合物IEM - 931的抗箭毒作用。以184微摩尔/千克的剂量给药时,该新化合物可预防并消除其结构类似物藜芦碱的箭毒效应。然而,对于筒箭毒碱,只有在剂量达到384微摩尔/千克时才表现出拮抗作用。这表明IEM - 931抗箭毒作用的功效与相互作用分子结构的互补性直接相关。猫肌肉局部松弛实验表明,IEM - 931的抗箭毒作用在血液中和胆碱受体上均得以实现。此外,分子相互作用的结果是形成了无活性复合物。