Characteristics of tetrahydroprotoberberines on dopamine D-1 and D-2 receptors in calf striatum

	Characteristics of tetrahydroprotoberberines on dopamine D-1 and D-2 receptors in calf striatum
	Guo, X; Wang, LM; Liu, J; Jin, GZ
刊名	ACTA PHARMACOLOGICA SINICA
	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
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:A1997WX76200009
内容类型	期刊论文
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.