FURTHER CHARACTERIZATION OF [H-3] U69593 BINDING-SITES IN THE RAT-HEART
文献类型：期刊论文
| 作者 | JIN, WQ; TAI, KK; CHAN, TKY; WONG, TM |
| 刊名 | JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY
 |
| 出版日期 | 1995-08 |
| 卷号 | 27期号:8页码:1507-1511 |
| 关键词 | KAPPA-1 BINDING SITES OPIOID RECEPTOR RAT HEART CATIONS U-50488H U-69593 ETORPHINE MET(5)-ENKEPHALIN-ARG(6)-PHE(7) |
| ISSN号 | 0022-2828 |
| DOI | 10.1016/S0022-2828(95)90227-9 |
| 文献子类 | Article |
| 英文摘要 | K binding sites in the crude membrane preparation of the rat heart homogenate were further characterized by a displacement binding assay of [H-3]-U69593 with specific kappa ligands and a direct binding assay with [H-3]-etorphine. Scatchard analysis of specific [H-3]-U69593 binding showed that the K-d and B-max were 6.4 +/- 1.0 nM and 97 +/- 8 fmol/mg protein, respectively. The binding of [H-3]-U69593 was effectively displaced by the selective kappa(1) ligands, U-69593 and U-50488H, but only weakly displaced by Met(5)-enkephalin-Arg(6)-Phe(7), a selective kappa(2) ligand, which showed only 11 +/- 3% inhibition of [H-3]-U69593 binding at the concentration of 1 mu M. In addition, there was no binding site for [H-3]-etorphine, known to bind to mu, delta and kappa(2) binding sites, but not kappa(1) binding sites. The findings suggest that the kappa binding sites in the rat heart most likely belong to the kappa(1) subtype, The binding sites have high and low affinity components as nonlinear regression analysis of the competition curves is best fit by two components with IC50 values of 11 +/- 2 and 62 +/- 7 nM for U-69593, and 9.9 +/- 1.5 and 414 +/- 108 nM for U-50488H. Furthermore, the binding of [H-3]-U69593 were inhibited by both monovalent cations (Na+, Li+) and divalent cations (Mg2+, Mn2+ and Ca2+). (C) 1995 Academic Press Limited |
| WOS关键词 | GUINEA-PIG BRAIN ; BOVINE ADRENAL-MEDULLA ; OPIOID RECEPTORS ; KAPPA-SITES ; SUBTYPE ; MEMBRANES ; PEPTIDES ; DRUGS |
| WOS研究方向 | Cardiovascular System & Cardiology ; Cell Biology |
| 语种 | 英语 |
| WOS记录号 | WOS:A1995RR07500005 |
| 出版者 | ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275036]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.CHINESE ACAD SCI, SHANGHAI INST MAT MED, SHANGHAI, PEOPLES R CHINA 2.UNIV HONG KONG, FAC MED, DEPT PHYSIOL, HONG KONG, HONG KONG |
| 推荐引用方式 GB/T 7714 | JIN, WQ,TAI, KK,CHAN, TKY,et al. FURTHER CHARACTERIZATION OF [H-3] U69593 BINDING-SITES IN THE RAT-HEART[J]. JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY,1995,27(8):1507-1511. |
| APA | JIN, WQ,TAI, KK,CHAN, TKY,&WONG, TM.(1995).FURTHER CHARACTERIZATION OF [H-3] U69593 BINDING-SITES IN THE RAT-HEART.JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY,27(8),1507-1511. |
| MLA | JIN, WQ,et al."FURTHER CHARACTERIZATION OF [H-3] U69593 BINDING-SITES IN THE RAT-HEART".JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY 27.8(1995):1507-1511. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。