[H-3] OHMEFENTANYL PREFERENTIALLY BINDS TO MU-OPIOID RECEPTORS BUT ALSO LABELS SIGMA-SITES IN RAT-BRAIN SECTIONS
文献类型：期刊论文
| 作者 | WANG, H; PELAPRAT, D; ROQUES, BP; VANHOVE, A; CHI, ZQ ; ROSTENE, W
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| 刊名 | EUROPEAN JOURNAL OF PHARMACOLOGY
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| 出版日期 | 1991-02-14 |
| 卷号 | 193期号:3页码:341-350 |
| 关键词 | [H-3]OHMEFENTANYL MU-OPIOID RECEPTORS SIGMA-RECEPTORS BRAIN (RAT) |
| ISSN号 | 0014-2999 |
| DOI | 10.1016/0014-2999(91)90149-K |
| 文献子类 | Article |
| 英文摘要 | Ohmefentanyl has been shown to be 6300 times more potent than morphine for analgesia. The receptor binding characteristics and distribution of [H-3]ohmefentanyl in rat brain sections are presented. [H-3]Ohmefentanyl bound with high affinity to opioid receptors in a saturable manner (K(d) = 0.95 +/- 0.08 nM, B(max) = 337 +/- 14 fmol/mg protein). We used various currently available specific mu, delta and kappa-ligands to show that [H-3]ohmefentanyl has a high selectivity for the mu-opioid receptor. However, [D-Ala2,MePhe4,Gly-ol5]enkephalin (DAGO) was unable to completely inhibit [H-3]ohmefentanyl specific binding, while complete inhibition was observed with fentanyl derivatives and the benzomorphan derivative, ethylketocyclazocine. This remaining 20% DAGO-inaccessible [H-3]ohmefentanyl specific binding did not correspond to either mu-1, delta or kappa-sites. Haloperidol and 1,3-di-otolylguanidine were able to inhibit DAGO-inaccessible [H-3]ohmefentanyl specific binding, suggesting that [H-3]ohmefentanyl might also bind to haloperidol-sensitive sigma-sites. The topographical distribution of [H-3]ohmefentanyl found by autoradiography was generally similar to that of [H-3]DAGO. However, in agreement with the biochemical results, quantitative analysis revealed additional sites in several rat brain regions, the greatest discrepancies with [H-3]DAGO distribution being observed in cerebellum, central grey, hippocampal formation and locus coeruleus. Finally, our results suggest that this capacity of binding to both mu and sigma-sites is shared by various fentanyl derivatives. |
| WOS关键词 | CENTRAL NERVOUS-SYSTEM ; OPIATE RECEPTORS ; AUTORADIOGRAPHIC VISUALIZATION ; ANTIPSYCHOTIC-DRUGS ; DELTA-RECEPTORS ; MORPHINE-LIKE ; MOUSE-BRAIN ; GUINEA-PIG ; AGONIST ; LIGAND |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:A1991FA64200012 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275209]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | WANG, H |
| 作者单位 | 1.ACAD SINICA,SHANGHAI INST MAT MED,SHANGHAI 200031,PEOPLES R CHINA 2.INSERM,DEPT CHIM ORGAN,U266,F-75006 PARIS,FRANCE 3.CEA,SERV MOLEC MARQUEES,F-91191 GIF SUR YVETTE,FRANCE |
| 推荐引用方式 GB/T 7714 | WANG, H,PELAPRAT, D,ROQUES, BP,et al. [H-3] OHMEFENTANYL PREFERENTIALLY BINDS TO MU-OPIOID RECEPTORS BUT ALSO LABELS SIGMA-SITES IN RAT-BRAIN SECTIONS[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,1991,193(3):341-350. |
| APA | WANG, H,PELAPRAT, D,ROQUES, BP,VANHOVE, A,CHI, ZQ,&ROSTENE, W.(1991).[H-3] OHMEFENTANYL PREFERENTIALLY BINDS TO MU-OPIOID RECEPTORS BUT ALSO LABELS SIGMA-SITES IN RAT-BRAIN SECTIONS.EUROPEAN JOURNAL OF PHARMACOLOGY,193(3),341-350. |
| MLA | WANG, H,et al."[H-3] OHMEFENTANYL PREFERENTIALLY BINDS TO MU-OPIOID RECEPTORS BUT ALSO LABELS SIGMA-SITES IN RAT-BRAIN SECTIONS".EUROPEAN JOURNAL OF PHARMACOLOGY 193.3(1991):341-350. |
入库方式： OAI收割
来源：上海药物研究所
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