Analgesic activity and selectivity of isothiocyanate derivatives of fentanyl analogs for opioid receptors
文献类型：期刊论文
| 作者 | Chen, BY; Jin, WQ; Chen, J ; Chen, XJ; Zhu, YC; Chi, ZQ
|
| 刊名 | LIFE SCIENCES
 |
| 出版日期 | 1999-09-03 |
| 卷号 | 65期号:15页码:1589-1595 |
| 关键词 | isothiocyanate derivatives fentanyl analogs analgesia opioid receptors binding selectivity bioassay |
| ISSN号 | 0024-3205 |
| DOI | 10.1016/S0024-3205(99)00404-X |
| 文献子类 | Article |
| 英文摘要 | The analgesic activity and opioid receptor binding characteristics were studied for the isothiocyanate ohmefentanyl (OMFIT), and isothiocyanate carfentanil (CarFIT), isothiocyanate 4-methoxymethylfentanyl (MethoFIT), isothiocyanate 3-methylfentanyl (superFIT) and their amide analogs. Antinociceptive activity was evaluated using the mouse hot plate test; selectivity for opioid receptor was determined in bioassay and binding assay. SuperFIT, CarFIT, OMFIT and MethoFIT exhibited an analgesic ED50 lower than those of their parent compounds without isothiocyanate (SCN) group. Furthermore these compounds exhibited potent inhibitory actions on the electrically evoked contractions of mouse vas deferens, which could, be antagonized by naloxone, but their actions were weaker than those of their parent compounds without SCN-group. The inhibitory actions of these compounds on binding of [H-3]OMF to mouse brain membrane was weaker than those of their parent compounds without SCN-group. CarFIT and MethoFIT showed weaker inhibitory actions on the binding of [H-3] DADLE than their parent compounds without SCN-group, but SuperFIT and OMFIT stronger than their parent compounds, 3-methylfentanyl and ohmefentanyl. The selectivity of these isothiocyanate derivatives for delta opioid receptors increased. In conclusion, introducing isothiocyanato-group into 1-position of phenyl ring of ohmefentanyl and other fentanyl analogs would enhance the selectivity of these compounds for delta-opioid receptors, but decrease their analgesic activity. |
| WOS关键词 | MU-OPIATE ; CIS-(+)-3-METHYLFENTANYL ISOTHIOCYANATE ; MEDIATED PHENOMENA ; DELTA-OPIATE ; ANTAGONISTS ; MORPHINE ; LIGANDS ; BINDING ; AGONIST ; PROBES |
| WOS研究方向 | Research & Experimental Medicine ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000082453100009 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274696]  |
| 专题 | 药理学第一研究室 |
| 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 | Chen, BY,Jin, WQ,Chen, J,et al. Analgesic activity and selectivity of isothiocyanate derivatives of fentanyl analogs for opioid receptors[J]. LIFE SCIENCES,1999,65(15):1589-1595. |
| APA | Chen, BY,Jin, WQ,Chen, J,Chen, XJ,Zhu, YC,&Chi, ZQ.(1999).Analgesic activity and selectivity of isothiocyanate derivatives of fentanyl analogs for opioid receptors.LIFE SCIENCES,65(15),1589-1595. |
| MLA | Chen, BY,et al."Analgesic activity and selectivity of isothiocyanate derivatives of fentanyl analogs for opioid receptors".LIFE SCIENCES 65.15(1999):1589-1595. |
入库方式： OAI收割
来源：上海药物研究所
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