Analgesic activity and selectivity for opioid receptors of enantiomers of ohmefentanyl
文献类型：期刊论文
| 作者 | Jin, WQ; Wang, ZX; Chen, J ; Chen, XJ; Chi, ZQ
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 1996-09 |
| 卷号 | 17期号:5页码:421-424 |
| 关键词 | ohmefentanyl stereoisomers pain measurement mu opioid receptors delta opioid receptors radioligand assay structure-activity relationship |
| ISSN号 | 0253-9756 |
| 文献子类 | Article |
| 英文摘要 | AIM: 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) mu g . kg(-1). These enantiomers selectively acted on ct opioid receptors. K-i values (mu) 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(delta)/K-i(mu) 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 mu opioid receptors. F-9204 showed the strongest analgesic activity and the highest selectivity for mu opioid receptors. |
| WOS关键词 | VAS-DEFERENS ; AGONIST ; LIGAND |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:355592 |
| WOS记录号 | WOS:A1996VF91900010 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274960]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Jin, WQ |
| 作者单位 | CHINESE ACAD SCI,SHANGHAI INST MAT MED,SHANGHAI 200031,PEOPLES R CHINA. |
| 推荐引用方式 GB/T 7714 | Jin, WQ,Wang, ZX,Chen, J,et al. Analgesic activity and selectivity for opioid receptors of enantiomers of ohmefentanyl[J]. ACTA PHARMACOLOGICA SINICA,1996,17(5):421-424. |
| APA | Jin, WQ,Wang, ZX,Chen, J,Chen, XJ,&Chi, ZQ.(1996).Analgesic activity and selectivity for opioid receptors of enantiomers of ohmefentanyl.ACTA PHARMACOLOGICA SINICA,17(5),421-424. |
| MLA | Jin, WQ,et al."Analgesic activity and selectivity for opioid receptors of enantiomers of ohmefentanyl".ACTA PHARMACOLOGICA SINICA 17.5(1996):421-424. |
入库方式： OAI收割
来源：上海药物研究所
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