Effect of chronic treatment of ohmefentanyl stereoisomers on cyclic AMP formation in Sf9 insect cells expressing human mu-opioid receptors
文献类型：期刊论文
| 作者 | Liu, ZH; He, Y; Jin, WQ; Chen, XJ; Shen, QX; Chi, ZQ
|
| 刊名 | LIFE SCIENCES
 |
| 出版日期 | 2004-04-30 |
| 卷号 | 74期号:24页码:3001-3008 |
| 关键词 | ohmefentanyl stereoisomer mu-opioid receptor binding affinity cyclic AMP Sf9 insect cell |
| ISSN号 | 0024-3205 |
| DOI | 10.1016/j.lfs.2003.10.027 |
| 文献子类 | Article |
| 英文摘要 | The binding affinity of ohmefentanyl stereoisomers for mu-opioid receptors and the effect of chronic ohmefentanyl stereoisomers pretreatments on intracellular cAMP formation were investigated in Sf9 insect cells expressing human mu-opioid receptors (Sf9-mu cells). Competitive assay of [H-3]ohmefentanyl binding revealed that these isomers had high affinity for mu-opioid receptors in Sf9-mu cells. Isomer F9204 had the highest affinity for mu-opioid receptors with the K-i value of 1.66 +/- 0.28 nM. After pretreated Sf9-mu cells with increasing concentrations of these isomers for 6 h, addition of naloxone (1 muM) precipitated an overshoot of foskolin-stimulated cAMP accumulation. The ability of these isomers to induce cAMP overshoot differed greatly with the order of F9202 > F9205 > F9208 > F9206 > F9204 > F9207. Of these isomers, F9202 was 2.7-fold less potent than F9204 in receptor binding affinity, but 71.5-fold more potent in ability to induce cAMP overshoot. These results suggested that there was a significant stereo-structural difference among ohmefentanyl stereoisomers in ability to induce naloxone-precipitated cAMP overshoot in Sf9-mu cells. (C) 2004 Published by Elsevier Inc. |
| WOS关键词 | ANALGESIC ACTIVITY ; ADENYLATE-CYCLASE ; DEPENDENCE ; MORPHINE ; MICE ; ACTIVATION ; AGONISTS ; PROTEINS ; EFFICACY ; DELTA |
| WOS研究方向 | Research & Experimental Medicine ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000220629100006 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274088]  |
| 专题 | 药理学第一研究室 |
| 通讯作者 | Jin, WQ |
| 作者单位 | 1.Shanghai Inst Planned Parenthood Res, Shanghai 200032, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Dept Pharmacol 2, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, ZH,He, Y,Jin, WQ,et al. Effect of chronic treatment of ohmefentanyl stereoisomers on cyclic AMP formation in Sf9 insect cells expressing human mu-opioid receptors[J]. LIFE SCIENCES,2004,74(24):3001-3008. |
| APA | Liu, ZH,He, Y,Jin, WQ,Chen, XJ,Shen, QX,&Chi, ZQ.(2004).Effect of chronic treatment of ohmefentanyl stereoisomers on cyclic AMP formation in Sf9 insect cells expressing human mu-opioid receptors.LIFE SCIENCES,74(24),3001-3008. |
| MLA | Liu, ZH,et al."Effect of chronic treatment of ohmefentanyl stereoisomers on cyclic AMP formation in Sf9 insect cells expressing human mu-opioid receptors".LIFE SCIENCES 74.24(2004):3001-3008. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。