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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。
This article reports the comprehensive screening of anticholinergic compounds and the screening results of some compounds. On the five indexes, the ED50 value of the compound effect was measured, that is, anti-arecoline tremor and salivary secretion, prevention of PP10 poisoning, the effect of dilated pupils and the impact on the training of jumper in mice. Analysis and comparison of these results can determine the anticholinergic properties of the compounds, their potency, the selectivity of central and peripheral effects, the potency of prophylaxis against OP_ (10) toxicity and the magnitude of the side effects predicted. The compounds included in this review show that most compounds have fairly strong anticholinergic activity at the center and periphery, a small group of compounds with a strong central anticholinergic activity or peripheral anticholinergic activity. These results lay the foundation for further selection. The article discusses the selection of screening indicators.