摘要
A.Arnold等合成了一系列具有抗胆硷酯酶作用的二羧酸氨基烃酰胺的季铵盐(Quaternary salts of amino alkyamides of dicarboxylic acid)。酶抑宁(Win8077、Mytelase Ambenoniurn)是代表性的高效化合物,用于治疗重症肌无力。经实验证明:酶抑宁的药理作用与抗胆硷酯酶强度无平行关系。
It is known that Win 8078 has an unique activity upon the end plate receptors.We assumed that it may be used to antagonize the neuromuscular block induced by soman.Our results support this assumption.In anaesthetized cat,Win 8078(50 or 450 r/kg i.v)antagonizes the blocking effect induced by soman(150r/kg i.m.)at the sciatic gastrocnemius preparation.Similar results were obtained in rabhits.The present experiment also demonstrated that Win 8078 reversed the striated muscle paralysis initiated by Gand d-T.C.The augmented sensitivity of end plate receptors accounts for the antagonizing effect on the paralysis induced by C,d-T.C and soman at neuromuscular junctions.In another group of experiments,it was evidenced that,Win 8078 has therapeutic effect upon the soman poisoned animals,when the soman(215 r/kg im,3LD)poisoned rats were treated with compound consisting of cholinolytics and oximes,the survival rate was 2/10.But when Win 8078(1.5mg/kg im)was used in combination with the compound mentioned above,the survival rate was 8/10.It was also showed that Win 8078 had some therapeutic effect on soman(60--90 r/kg im 2--3 LD)poisoned rabbits,but the effect was lesser than that on the poisoned rats.In the untreated rats,soman(70r/kg s.c.LD)inhibited the spontaneous electrical activity of diaphragm.But in the rats treated with Win 8078 and other drugs(cholinergics and oximes)the po-tentials of diaphragm were not inhibited even when the dose of soman was increased to 215r/kg im(3LD).This results were observed in 5 out of 7 treated animals.To overcome the diaphragm paralysis seems to contribute its therapeutic effects.
出处
《军事医学科学院院刊》
1982年第1期85-91,共7页
Bulletin of the Academy of Military Medical Sciences
