CHARACTERIZATION AND DISTRIBUTION OF [H-3] OHMEFENTANYL BINDING-SITES IN THE HUMAN BRAIN
文献类型：期刊论文
| 作者 | WANG, H; SARRIEAU, A; PELAPRAT, D; ROQUES, BP; VANHOVE, A; KOPP, N; CHI, ZQ ; ROSTENE, W
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| 刊名 | SYNAPSE
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| 出版日期 | 1991-07 |
| 卷号 | 8期号:3页码:177-184 |
| 关键词 | [H-3]OHMEFENTANYL MU-OPIOID RECEPTOR HUMAN BRAIN QUANTITATIVE AUTORADIOGRAPHY |
| ISSN号 | 0887-4476 |
| DOI | 10.1002/syn.890080305 |
| 文献子类 | Article |
| 英文摘要 | Binding properties and localization of [H-3]ohmefentanyl, a new ligand for mu-opioid receptors, were investigated on normal human brain sections. Binding assays performed at the level of the basal ganglia revealed: (1) a steady-state binding reached after 60 min incubation at room temperature, (2) the presence, in saturation experiments, of an apparent single class of binding sites with a K(d) = 1.68 +/- 0.45 nM and a B(max) = 162 +/- 9 fmol/mg protein, (3) an order of potency to inhibit [H-3]ohmefentanyl binding as follows: ohmefentanyl > [D-Ala2, MePhe4, Gly-ol5]enkephalin (DAGO) > ethylketocyclazocine (EKC) >> Tyr-D-Ser(OtBu)-Gly-Phe-Leu-Thr(OtBu) (BUBU) and U-50,488H. Quantitative autoradiography showed an heterogeneous distribution of [H-3]ohmefentanyl binding sites with the highest densities in amygdala, medial geniculate body, thalamus, and caudate nucleus. Binding characteristics and anatomical distribution also show that [H-3]ohmefentanyl may bind to a small proportion of additional sites called "DAGO-inaccessible [H-3]ohmefentanyl specific binding sites." [H-3]Ohmefentanyl binding to these sites can be partly inhibited by sigma-ligands such as 1,3-di-o-tolylguanidine (DTG) and haloperidol. However, unlabeled DAGO inhibited more than 80% of [H-3]ohmefentanyl specific binding in most of the human brain regions studied, suggesting that the major population of sites labeled by [H-3]ohmefentanyl represented mu-opioid receptors. |
| WOS关键词 | OPIOID RECEPTOR-BINDING ; OPIATE RECEPTORS ; REGIONAL DISTRIBUTION ; METHIONINE-ENKEPHALIN ; ANTIPSYCHOTIC-DRUGS ; SPECIES-DIFFERENCES ; SELECTIVE LIGAND ; SUBSTANCE-P ; MU ; AUTORADIOGRAPHY |
| WOS研究方向 | Neurosciences & Neurology |
| 语种 | 英语 |
| WOS记录号 | WOS:A1991FR90600004 |
| 出版者 | WILEY-LISS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275197]  |
| 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.HOP EDOUARD HERRIOT,CENT ANAT & CYTOL PATHOL LAB,F-69437 LYONS 03,FRANCE 2.ACAD SINICA,SHANGHAI INST MAT MED,SHANGHAI 200031,PEOPLES R CHINA 3.FAC PHARM PARIS,INSERM,U266,F-75270 PARIS 06,FRANCE 4.CENS,CEA,DEPT BIOL,SERV MOLEC MARQUEES,F-91191 GIF SUR YVETTE,FRANCE |
| 推荐引用方式 GB/T 7714 | WANG, H,SARRIEAU, A,PELAPRAT, D,et al. CHARACTERIZATION AND DISTRIBUTION OF [H-3] OHMEFENTANYL BINDING-SITES IN THE HUMAN BRAIN[J]. SYNAPSE,1991,8(3):177-184. |
| APA | WANG, H.,SARRIEAU, A.,PELAPRAT, D.,ROQUES, BP.,VANHOVE, A.,...&ROSTENE, W.(1991).CHARACTERIZATION AND DISTRIBUTION OF [H-3] OHMEFENTANYL BINDING-SITES IN THE HUMAN BRAIN.SYNAPSE,8(3),177-184. |
| MLA | WANG, H,et al."CHARACTERIZATION AND DISTRIBUTION OF [H-3] OHMEFENTANYL BINDING-SITES IN THE HUMAN BRAIN".SYNAPSE 8.3(1991):177-184. |
入库方式： OAI收割
来源：上海药物研究所
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