Tetrahydroprotoberberine analogs antagonize alpha(1)-adrenoceptors and inhibit mobilization of intracellular calcium

	Tetrahydroprotoberberine analogs antagonize alpha(1)-adrenoceptors and inhibit mobilization of intracellular calcium
	Han, CD; Lu, ZZ; Wei, X; Jin, GZ
刊名	DRUG DEVELOPMENT RESEARCH
	1996-10
卷号	39 期号:2 页码:191-196
关键词	herbs adrenergic alpha-antagonists calcium blood vessel
ISSN号	0272-4391
文献子类	Article
英文摘要	Effect of tetrahydroprotoberberine (THPB) analogues 1-stepholidine (1-SPD), 1-tetrahydropalmatine (1-HTP), tetrahydroberberine (THB), and tetrahydroproberberine-18 (THPB-18) on alpha(1)-adrenoceptors and cellular Ca2+ dynamics were studied by radioligand binding assay and vascular contractile functional determination. In membrane preparations of rat cerebral cortex 1-SPD, 1-THP, THB, or THPB-18 inhibited I-125-BE 2254 binding to alpha(1)-adrenoceptors with PKi values (-log K-i) of 5.54+/-0.36, 5.56+/-0.47, 6.01+/-0.60, and 5.75+/-0.56, respectively. The Hill coefficients for the 4 analogs were not significantly different to unity. The computer analysis showed that the competitive curves for the 4 analogs were fit to a one binding site model. In isolated rat aortae 1-SPD, 1-THP, THB, or THPB-18 inhibited phenylephrine-induced contraction with pA(2) values of 5.48+/-0.58, 5.66+/-0.54, 5.45+/-0.76, and 5.64+/-0.34, respectively; the slopes of the Schild plot were not significantly different from unity. 1-SPD (10 mu M) and THE (10 mu M) did not affect the CaCl2-induced contraction in calcium free Krebs solution containing 100 mM KCl. However, both of them noncompetitively inhibited vasocontraction induced by intracellular Ca2+ mobilizers phenylephrine, 5-HT, angiotensin II, or bradykinin. These results suggest that THPB analogs can non-subtype selectively antagonize alpha(1)-adrenoceptors and inhibit intracellular Ca2+ mobilization. (C) 1997 Wiley-Liss, Inc.
WOS关键词	ALPHA-1-ADRENERGIC RECEPTOR SUBTYPES ; (-)-STEPHOLIDINE
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	WILEY-LISS
WOS记录号	WOS:A1996WL63800013
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/274956]
专题	中国科学院上海药物研究所
通讯作者	Han, CD
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	Han, CD,Lu, ZZ,Wei, X,et al. Tetrahydroprotoberberine analogs antagonize alpha(1)-adrenoceptors and inhibit mobilization of intracellular calcium[J]. DRUG DEVELOPMENT RESEARCH,1996,39(2):191-196.
APA	Han, CD,Lu, ZZ,Wei, X,&Jin, GZ.(1996).Tetrahydroprotoberberine analogs antagonize alpha(1)-adrenoceptors and inhibit mobilization of intracellular calcium.DRUG DEVELOPMENT RESEARCH,39(2),191-196.
MLA	Han, CD,et al."Tetrahydroprotoberberine analogs antagonize alpha(1)-adrenoceptors and inhibit mobilization of intracellular calcium".DRUG DEVELOPMENT RESEARCH 39.2(1996):191-196.