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本文报道20个取代羟乙酸哌啶醇酯类化合物的合成及其中枢及外周抗胆碱作用。初步药理结果表明:其中一部份化合物具有较强的中枢及外周抗胆碱作用,尤以化合物Ⅲ的生理活性最强,其抗震颤素引起震颤的ED_(50)0.173 mg/kg,稍强或相当于著名的中枢抗M-胆碱作用的代表化合物——二苯羟乙酸-3-喹咛酯(QNB)的强度,值得进一步研究。
This paper reports the synthesis of 20 substituted piperidinyl glycolates and their central and peripheral anticholinergic effects. The preliminary pharmacological results showed that some of the compounds had strong central and peripheral anticholinergic activity, especially compound Ⅲ which had the strongest physiological activity and its ED_ (50) 0.173 mg / kg of tremor induced by anti-tremor tremor was slightly stronger Or the equivalent of the famous center of anti-M-choline role of the representative compound - 3-benzbutyric acid (QNB) intensity, worth further study.