Synthesis and neuropharmacological evaluation of R(-)-N-alkyl-11-hydroxynoraporphines and their esters

被引：35

作者：

Csutoras, C

Zhang, A

Zhang, KH

Kula, NS

Baldessarini, RJ

Neumeyer, JL

机构：

[1] Harvard Univ, Sch Med, McLean Div, Massachusetts Gen Hosp,Alcohol & Drug Abuse Res C, Belmont, MA 02478 USA

[2] Harvard Univ, Sch Med, Massachusetts Gen Hosp, McLean Div,Mailman Res Ctr, Belmont, MA 02478 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 13期

关键词：

apomorphine; 11-hydroxyaporphine; Parkinson's disease; dopamine receptor; motor activity; bioavailablity;

D O I：

10.1016/j.bmc.2004.04.029

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We synthesized several N-substituted-11-hydroxynoraporphines and their esters of varying chain length, evaluated their binding affinity at dopamine (DA) receptor sites in rat caudate-putamen membranes, and quantified their effects on motor activity in normal adult male rats. The 11-hydroxyaporphines showed similar neuropharmacological properties to the corresponding 10,11-catecholaporphines. At moderate doses, their esters proved to have more prolonged behavioral actions and superior oral bioavailability. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：3553 / 3559

页数：7

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