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羟甲芬太尼对映异构体的镇痛活性及对阿片受体的选择性

Analgesic activity and selectivity for opioid receptors of enantiomers of ohmefentanyl 1
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摘要 羟甲芬太尼对映异构体的镇痛活性及对阿片受体的选择性金文桥,王智贤,陈洁,陈新建,池志强(中国科学院上海药物研究所,上海200031,中国)关键词羟甲芬太尼;立体异构体;痛测定;μ阿片受体;δ阿片受体;放射配位体测定;结构活性关系目的:研究羟甲芬太尼... IM: To study analgesic activity and selectivity for opioid receptor subtypes of 8 enantomers of ohmefentanyl (Ohm). METHODS: Analgesic activity was evaluated using the hot plate test in mice. Selectivity for opioid receptors was determined in binding assay and bioassay. RESULTS: Among the 8 enantiomers of Ohm, the most potent isomer was F 9204, (+) cis (3R,4S,2′S ) Ohm, with an analgesic ED 50 (ip) value of 1 1 (0 8-1 3) μg·kg -1 . These enantiomers selectively acted on μ opioid receptors. K i values (μ) of enantiomers F 9204 and F 9202, (-) cis (3R,4S,2 ′R) Ohm were 4 0±2 0 and 5±4 pmol·L -1 , respectively. Their K i(δ)/ K i(μ) ratios were 22 500 and 22 800 , respectively. On guinea pig ileum and mouse vas deferens F 9202, F 9204, F 9205, F 9206, F 9207 , and F 9208 exhibited very potent inhibitons, which were antagonized by naloxone. In rabbit vas deferens these enantiomers had no effect. CONCLUSION: Eight enantiomers of Ohm selectively acted on μ opioid receptors. F 9204 showed the strongest analgesic activity and the highest selectivity for μ opioid receptors.
出处 《中国药理学报》 CSCD 1996年第5期421-424,共4页 Acta Pharmacologica Sinica
关键词 羟甲芬太尼 立体异构体 阿片 受体 镇痛 ohmefentanyl stereoisomers pain measurement mu opioid receptors delta opioid receptors radioligand assay structure activity relationship
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参考文献6

  • 1王智贤,药学学报,1994年,29卷,433页
  • 2金文桥,中国药理学报,1989年,10卷,205页
  • 3金文桥,Sci Chin B,1987年,30卷,176页
  • 4Xu H,Sci Chin B,1985年,28卷,504页
  • 5金文桥,Sci Chin B,1981年,24卷,710页
  • 6Zhao Y,药学学报,1956年,4卷,97页

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