bindingaffinitytoanddependenceonsomeopioidsinsf9insectcellsexpressinghumanopioidreceptor
文献类型：期刊论文
| 作者 | Liu Zhonghua1; He You1; Jin Wenqiao1; Chen Xinjian1; Zhang Hongping1; Shen Qingxiang2; Chi Zhiqiang1
|
| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2003 |
| 卷号 | 024期号:009页码:859 |
| 关键词 | 阿片类药物 Sf9昆虫细胞 μ阿片受体 受体亲和力 受体依赖性 |
| ISSN号 | 1671-4083 |
| 英文摘要 | AIM: To investigate the receptor binding affinity and naloxone-precipitated cAMP overshoot of dihydroetorphine,fentanyl, heroin, and pethidine in Sf9 insect cells expressing human μ-opioid receptor (Sf9-μ cells). METHODS:Competitive binding assay of ^3Hohmefentanyl was used to reveal the affinity for μ-opioid receptor in Sf9-μ cells.^3HcAMP RIA was used to determine cAMP level. Antinociceptive activity was evaluated using 55℃ mouse hotplate test. Naloxone-precipitated withdrawal jumping was used to reflect physical dependence in mice. RESULTS:All drugs displayed antinociceptive activity and produced physical dependence in mice. The Ki values ofdihydroetorphine, fentanyl, heroin, and pethidine in competitive binding assay were (0.85±0.20)nmol, (59.1±11.7)nmol, (0.36±0.13)μmol, and (12.2±3.8) μmol respectively. The binding affinities of these drugs for μ-opioidreceptor in Sf9-μ cells were paralleled to their antinociceptive activities in mice. After chronic pretreatment withthese drugs, naloxone induced cAMP withdrawal overshoot in Sf9-μ cells. The dependence index in Sf9-μ cellswas calculated as Ki value in competitive binding assay over ECs0 value in naloxone-precipitated cAMP assay, Thephysical dependence index in mice was calculated as antinociceptive ED50/withdrawal jumping cumulative EDs0.There was a good linear correlation between dependence index in Sf9-μ cells and physical dependence index inmice. CONCLUSION: The Sf9-μ cells could be used as a cell model to evaluate the receptor binding affinity andphysical dependent liability of analgesic agents. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/284957]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国科学院上海药物研究所 2.Institute of Planned Parenthood Research |
| 推荐引用方式 GB/T 7714 | Liu Zhonghua,He You,Jin Wenqiao,et al. bindingaffinitytoanddependenceonsomeopioidsinsf9insectcellsexpressinghumanopioidreceptor[J]. actapharmacologicasinica,2003,024(009):859. |
| APA | Liu Zhonghua.,He You.,Jin Wenqiao.,Chen Xinjian.,Zhang Hongping.,...&Chi Zhiqiang.(2003).bindingaffinitytoanddependenceonsomeopioidsinsf9insectcellsexpressinghumanopioidreceptor.actapharmacologicasinica,024(009),859. |
| MLA | Liu Zhonghua,et al."bindingaffinitytoanddependenceonsomeopioidsinsf9insectcellsexpressinghumanopioidreceptor".actapharmacologicasinica 024.009(2003):859. |
入库方式： OAI收割
来源：上海药物研究所
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