马斯才, 陆苏南, 李可中, 王崇铨. 3,4-二氯-N-甲基-N-反式-2-(1-△3-吡咯啉基)环己基-苯乙酰胺盐酸盐的合成及其镇痛活性的研究J. 药学学报, 1986, 21(11): 861-863.
引用本文: 马斯才, 陆苏南, 李可中, 王崇铨. 3,4-二氯-N-甲基-N-反式-2-(1-△3-吡咯啉基)环己基-苯乙酰胺盐酸盐的合成及其镇痛活性的研究J. 药学学报, 1986, 21(11): 861-863.
MA Si-Cai, LU Su-Nan, LI Ke-Zhong , WANG Chong-Quan, . SYNTHESIS AND ANALGESIC ACTIVITY OF 3, 4-DICHLORO-N-METHYL-N- TRANS-2-(1-△3-PYRROLINYL )-CYCLOHEXYL-BENZENACETAMIDE HYDROCHLORIDEJ. Acta Pharmaceutica Sinica, 1986, 21(11): 861-863.
Citation: MA Si-Cai, LU Su-Nan, LI Ke-Zhong , WANG Chong-Quan, . SYNTHESIS AND ANALGESIC ACTIVITY OF 3, 4-DICHLORO-N-METHYL-N- TRANS-2-(1-△3-PYRROLINYL )-CYCLOHEXYL-BENZENACETAMIDE HYDROCHLORIDEJ. Acta Pharmaceutica Sinica, 1986, 21(11): 861-863.

3,4-二氯-N-甲基-N-反式-2-(1-△3-吡咯啉基)环己基-苯乙酰胺盐酸盐的合成及其镇痛活性的研究

SYNTHESIS AND ANALGESIC ACTIVITY OF 3, 4-DICHLORO-N-METHYL-N- TRANS-2-(1-△3-PYRROLINYL )-CYCLOHEXYL-BENZENACETAMIDE HYDROCHLORIDE

  • Abstract: 3, 4-Dichloro-N-methyl-N-trans-2- (1-△3-pyrrolinyl)-cyclohexyl-benzenacetamide hydrochloride (K-Ⅱ) was synthesized from N-methyl-7-azabicyclo 4.1.0 heptane by treatment with 2,5-dihydropyrrole to give N-trans-2(1-△3-pyrrolinyl)-cyclohexyl-N-methylamine which was amidated with 3,4-dichlorophenyl-acetic acid. K-Ⅱ is an analogue of U-50488 H(K-Ⅰ), a known kappa receptor agonist.The results of animal tests showed that K-Ⅱ is 3 times as potent as K-Ⅰ as an analgesic in the mouse hot plate test and 5 times in the mouse writhing test and that the affinity of K-Ⅱ for kappa receptor may be higher than that of K-Ⅰ. The general behavioural effects of these two agents are similar in mice.

     

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