Analysis of binding domain and function of chimeric mu/kappa opioid receptors to ohmefentanyl stereoisomers
文献类型：期刊论文
| 作者 | Feng, YP; Chen, LW; Zhou, DH; Chen, J ; Xu, XJ; Chi, ZQ
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2001-11 |
| 卷号 | 22期号:11页码:981-985 |
| 关键词 | mu opioid receptors kappa opioid receptors COS-1 cell line ohmefentanyl stereoisomerism U50488 binding sites cyclic AMP |
| ISSN号 | 0253-9756 |
| 文献子类 | Article |
| 英文摘要 | AIM: To investigate specific domains in mu opioid receptors that accounted for selective binding of three stereoisomers of ohmefentanyl (Ohm9204, Ohm9202, and Ohm9203) and study the function of chimera tt. METHODS: Rat mu and kappa opioid receptors (RMOR, RKOR) and four mu/kappa chimeric receptors (chimeras) I, II, III, and IV were transiently expressed in COS-1 cells. The binding ability and binding domain of receptor to ligands were determined by radioactive ligand and receptor binding experiments. Through measuring cellular cAMP levels, we studied the function of chimera If in mediating signal transduction. RESULTS: Binding affinities of four chimeric receptors were similar to wild type opioid receptors RMOR and RKOR). The binding affinities of Ohm9204 and Ohm9202 to chimera II were similar to that of RMOR. The binding affinities of Ohm9203 to all six receptors were low. U50488 possessed high binding affinity to chimera I, however dynorphie A(1-9) had some binding affinity to chimera II that was similar to RKOR, which indicated the domains of RKOR accounting for selectively binding to peptide ligand dynorphie A(1-9) and nonpeptide ligand U50488 were different. The efficacy of Ohm9204 and Ohm9203 on inhibiting forskolin-stimulated cAMP accumulation in cells transfected with chimera II was similar to that in cells transfected with RMOR. CONCLUSION: Replacing 194 - 268 residues of RMOR with 185 - 262 residues of RKOR does not influence the ability of mu opioid receptor to bind Ohm9204 and Ohm9202 and the receptor mediated inhibition of cellular cAMP level. |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000171991900005 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274432]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhou, DH |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Shanghai 200031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Feng, YP,Chen, LW,Zhou, DH,et al. Analysis of binding domain and function of chimeric mu/kappa opioid receptors to ohmefentanyl stereoisomers[J]. ACTA PHARMACOLOGICA SINICA,2001,22(11):981-985. |
| APA | Feng, YP,Chen, LW,Zhou, DH,Chen, J,Xu, XJ,&Chi, ZQ.(2001).Analysis of binding domain and function of chimeric mu/kappa opioid receptors to ohmefentanyl stereoisomers.ACTA PHARMACOLOGICA SINICA,22(11),981-985. |
| MLA | Feng, YP,et al."Analysis of binding domain and function of chimeric mu/kappa opioid receptors to ohmefentanyl stereoisomers".ACTA PHARMACOLOGICA SINICA 22.11(2001):981-985. |
入库方式： OAI收割
来源：上海药物研究所
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