D-4 dopamine receptor-selective compounds from the Chinese plant Phoebe chekiangensis

被引：20

作者：

Hegde, VR

Dai, P

Ladislaw, C

Patel, MG

Puar, MS

Pachter, JA

机构：

[1] Schering Plough Research Institute, Kenilworth, NJ 07033

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(97)00194-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Hydroxy-indoline (1), tyramine (2), N-norarmepavine (3), and a novel glycosylated tetrahydroisoquinoline analog SCH 71450 (4) were all isolated from a methanol extract from the fruit of the Chinese plant Phoebe chekiangensis based on their activity in displacing D-4 dopaminergic receptor ligand binding. These compounds and related natural products were evaluated for D-4 receptor selectivity relative to D-2 receptor binding displacement. Compounds 1 and 4 exhibited better D-4 selectivity than standard dopaminergic antagonists including the clinically useful compound clozapine. GppNHp shifts in displacement curves indicated that compound 1 is an agonist while compound 4 is an antagonist. (C) 1997 Elsevier Science Ltd.

引用

页码：1207 / 1212

页数：6

共 17 条

[1]

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