A novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist:: 1-Propyl-1,2,3,4,4a,5,10,10-aoctahydrobenzo[g]quinoline-6,7-diol

被引:4
|
作者
Liu, Danyang [1 ]
Dijkstra, Durk [1 ]
de Vries, Jan B. [1 ]
Wikstrom, Hakan V. [1 ]
机构
[1] Univ Groningen, Dept Med Chem, Univ Ctr Pharm, NL-9713 AV Groningen, Netherlands
关键词
catecholamine; enone prodrug; microdialysis; Parkinson's disease;
D O I
10.1016/j.bmc.2007.06.036
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
Previously, we have demonstrated that enone prodrugs of dopaminergic catecholamines represent a new type of dopamine (DA) agonist. Trans-1-propyl-1,2, 3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol (TL-334), the active form oftrans-1-propyl-2,3,4,4a,5,7,8,9,10,10a-decahydro-1H-benzo[g]quinolin-6-one (GMC-6650), in vivo showed an extremely potent dopaminergic activity. Here, we report a novel synthesis and a pharmacological evaluation of TL-334 by means of microdialysis. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3438 / 3444
页数:7
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