Characteristics of tetrahydroprotoberberines on dopamine D-1 and D-2 receptors in calf striatum
文献类型：期刊论文
| 作者 | Guo, X; Wang, LM; Liu, J ; Jin, GZ
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 1997-05 |
| 卷号 | 18期号:3页码:225-230 |
| 关键词 | tetrahydroprotoberberines Sch-23390 spiperone guanosine triphosphate corpus striatum dopamine D-1 receptors dopamine D-2 receptors radioligand assay stepholidine 12-chloroscoulerine |
| ISSN号 | 0253-9756 |
| 文献子类 | Article |
| 英文摘要 | AIM: To study the characteristics of tetrahydroprotoberberines (THPB) on dopamine D-1 and D-2 receptors and elucidate their structure-activity relationship. METHODS: Radioligand assay in vitro with a two-site model program analysis. RESULTS: Four THPB with two hydroxyl groups on C-2 and C-9 or C-2 and C-10 exhibited R-H and R-L two binding sites to D-1 receptors and guanosine triphosphate regulated the R-H binding site of SPD and THPB-132A in competition assay, while eleven THPB including nonhydroxy-THPB, monohydroxy-THPB, and THPB with two hydroxyl groups attaching to C-3 and C-10 showed one binding site to D-1 receptors under the same conditions. However, the tested eleven THPB all manifested one binding site to D-2 receptors in competition assay, and the 2-hydroxy-THPB had the most potent affinity for D-2 receptors. CONCLUSION: Dihydroxy-THPB with two hydroxyl groups attaching to C-2 and C-9 or C-2 and C-10 possess the intrinsic activity of agonist to D-1 receptors, while the other THPB do not. The tested eleven THPB all are the antagonists of D-2 receptors. |
| WOS关键词 | ANTAGONISTS ; BRAIN |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:411908 |
| WOS记录号 | WOS:A1997WX76200009 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274913]  |
| 专题 | 分析化学研究室 药物发现与设计中心 上海药物代谢研究中心 院士及顾问专家 |
| 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 | Guo, X,Wang, LM,Liu, J,et al. Characteristics of tetrahydroprotoberberines on dopamine D-1 and D-2 receptors in calf striatum[J]. ACTA PHARMACOLOGICA SINICA,1997,18(3):225-230. |
| APA | Guo, X,Wang, LM,Liu, J,&Jin, GZ.(1997).Characteristics of tetrahydroprotoberberines on dopamine D-1 and D-2 receptors in calf striatum.ACTA PHARMACOLOGICA SINICA,18(3),225-230. |
| MLA | Guo, X,et al."Characteristics of tetrahydroprotoberberines on dopamine D-1 and D-2 receptors in calf striatum".ACTA PHARMACOLOGICA SINICA 18.3(1997):225-230. |
入库方式： OAI收割
来源：上海药物研究所
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