Further characterization of structural requirements for ligands at the dopamine D2 and D3 receptor:: Exploring the thiophene moiety

被引：19

作者：

Dijkstra, D

Rodenhuis, N

Vermeulen, ES

Pugsley, TA

Wise, LD

Wikström, HV

机构：

[1] Univ Groningen, Dept Med Chem, NL-9713 AV Groningen, Netherlands

[2] Pfizer Global Res & Dev, Ann Arbor Labs, CNS Chem & Pharmacol, Ann Arbor, MI 48105 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 14期

关键词：

D O I：

10.1021/jm001015a

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present study describes the synthesis and in vitro pharmacology of a novel series of dopaminergic agents in which the classical phenylethylamine pharmacophore is replaced by a thienylethylamine moiety. In general, the novel compounds showed a moderate affinity for the dopamine (DA) D-2 and D-3 receptors. When the thienylethylamine moiety is fixed in a rigid system, the affinity for the DA receptor is significantly increased. However, in the tricyclic hexahydrothianaphthoxazine structure, the affinity for the DA receptors is diminished.

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页码：3022 / 3031

页数：10

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