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K-Ⅱ系k阿片激动剂U-50488的同类物。通过部分离体和整体实验比较了K-Ⅱ与U-50488的药理作用。实验发现,K-Ⅱ抑制电刺激兔输精管收缩的IC50值为0.42 nmol/L,U-50488为26.5 nmol/L;K-Ⅱ抑制小鼠运动功能(横筛法)的ED50值为1.7 mg/g,U-50488为15.3 mg/kg;K-Ⅱ的小鼠LD50值为152.5 mg/kg,U-50488为118.4 mg/g;K-Ⅱ明显降低小鼠自发活动的作用比U-50488强5倍。结果表明,K-Ⅱ是一个药理作用较U-50488强的k受体激动剂。 相似文献
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反-2-(3,4-二氯苯基)-N-甲基-N-〔2-(1-吡咯烷基)环己基〕乙酰胺盐酸盐(U-50488H,1)是近年国外报道的一个高选择性K-型阿片受体激动剂。动物实验结果表明1 相似文献
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研究观察纳洛酮和狄普诺芬(M5050)对大肠杆菌内毒素休克狗血液动力学指标的影响。静脉注射纳洛酮(2mg/kg)和侧脑室注射M5050(40μg/狗),明显增加内毒素休克狗左心室内压、左心室内压最大上升速度、心脏每搏量及心输出量,平均动脉血压也显著回升。静脉注射M5050(2mg/kg)对内毒素休克狗血液动力学指标无明显作用。结果表明M5050改善内毒素休克狗的血液动力学的作用部位似在中枢神经系统,提示内毒素休克时中枢的内源性阿片样物质在休克发病学中的作用可能更为重要。 相似文献
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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. 相似文献
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3,4-Dichloro-N-methyl-N-[trans-2-(1-delta 3-pyrrolinyl)-cyclohexyl] benzenacetamide hydrochloride (K-II) is a novel analogue of U-50488H. Previous studies have demonstrated that K-II is more potent than U-50488H in analgesic activity in mice and in inhibitory effect on electrically induced contractions of the isolated rabbit vas deferens. In this paper, we determined the affinities of K-II and U-50488H for kappa opiate receptor in guinea pig cerebellum and frontal cortex using radioreceptor binding assay (saturation studies and competition studies), and calculated Ki values of K-II and U-50488H by the Cheng-Prusoff equation. The results indicate that the affinity of K-II for kappa opiate receptor is 6-42 times greater than that of U-50488H. The selectivity of K-II for opiate receptor subtypes is being studied. 相似文献
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N-[反式-2-(1-吡咯基)环己基]-N-甲基-3,4-二氯-苯乙酰胺盐酸盐(简称U-50488H(K-I))是近年来报道的高选择性的K-阿片受体激动剂,动物实验结果表明:该化合物具有较强的镇痛活性,且成瘾性较低,呼吸抑制较弱,无吗啡样副作用的新型麻醉镇痛剂。为研究它的药理作用,我们用氚标记了U-50488(K-I)。合成该化合物开始原料是N-甲基-反式-2-(1-△~3-吡咯啉基)环己基胺,按一般还原法以氧化铂为催化剂,通氚进行氚化反应,未经分离与3,4一二氯苯乙酸在二环己基碳二亚胺(DCC)存在下进行缩合脱水反应,生成N-[反式-2-(3,4-~3H-吡咯基)环己基]-N-甲基-3,4-二氯-苯乙酰胺,再用氯化氢乙醚处理,制得了氚化的U-50488(K-I)。合成途径如下: 相似文献
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