新合成抗胆碱药物的筛选

本文报道了抗胆碱化合物的综合筛选方法和部分化合物的初筛结果。在五个指标上,测定化合物效应的ED_(50)值,即抗槟榔碱震颤和唾液分泌、预防PP_(10)中毒、扩瞳效应和影响小鼠跳杆训练。分析比较这些结果,可以确定化合物的抗胆碱性质、作用强度、中枢和外周作用的选择性、预防OP_(10)中毒效价和预测副作用的大小。列入本文的化合物评选结果可见:大部分化合物的中枢和外周抗胆碱作用强度相当,小部分化合物的中枢抗胆碱作用较强或外周抗胆碱作用较强。这些结果为进一步评选打下基础。文中讨论了筛选指标的选择问题。

PRELIMINARY EVALUATION OF NEW ANTICHOLINERGIC COMPOUNDS

A complex method for the screening of anticholinergic compounds and some preliminary results of their applicaton are reported. In this method,the ED_(50) of anticholinergic compound is estimated with the following effects:anti-tremor and anti-salivation effects in mice given arecoline, preventive effect against organophosphate poisoning, mydriatic effect, effect on the "jum ping over a pole" training in mice. The results of determination of these effects may be used to evaluate the anticholinergic activity of the compound tested, its selective control and peripheral actions, its protective effect against organophosphate poisoning and its side effects. Most of the compounds studied by us showed equal central and peripheral anticholinergic actions, only a few showed stronger central or peripheral effect.