| 某些取代羟乙酸哌啶醇酯类化合物的合成及抗胆碱作用的研究 |
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| 引用本文： | 葛邦錀,吴瑞琴,唐琴梅,仇达萍,黄忠明,陈新建. 某些取代羟乙酸哌啶醇酯类化合物的合成及抗胆碱作用的研究[J]. 药学学报, 1985, 20(6): 427-432 |
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| 作者姓名： | 葛邦錀 吴瑞琴 唐琴梅 仇达萍 黄忠明 陈新建 |
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| 作者单位： | 中国科学院上海药物研究所，中国科学院上海药物研究所，中国科学院上海药物研究所，中国科学院上海药物研究所，中国科学院上海药物研究所，中国科学院上海药物研究所 |
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| 摘 要： | 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ED500.173 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。
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| 关 键 词： | 抗M-胆碱能药物 取代羟乙酸哌啶醇酯 |
SYNTHESIS AND ANTICHOLINERGIC ACTIVITY OF SOME DERIVATIVES OF SUBSTITUTED GLYCOLATES |
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| GE Bang-Lun,WU Rui-Qin,TANG Qin-Mei,CHOU Da-Ping,HUANG Zhong-Ming and CHEN Xin-Jian. SYNTHESIS AND ANTICHOLINERGIC ACTIVITY OF SOME DERIVATIVES OF SUBSTITUTED GLYCOLATES[J]. Acta pharmaceutica Sinica, 1985, 20(6): 427-432 |
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| Authors: | GE Bang-Lun WU Rui-Qin TANG Qin-Mei CHOU Da-Ping HUANG Zhong-Ming CHEN Xin-Jian |
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| Abstract: | In the present paper a total of 20 derivatives of substituted piperidyl glycolate as anticholinergic agent were synthesized. preliminary pharmacological results showed that some of them possessed potent anticholinergic activity inmice both in central and peripheral nervous systems. Compouod Ⅲ was found to be the most potent anticholinergic agent in this series. Its central anticholinergic ED50 value was 0.173mg/kg (in mice). It was somewhat more potent than or equal to the famous anticholinergic agent QNB. |
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| Keywords: | Substituted piperidinol glycolate Anticholinergic activity |
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