(dipropylamino)tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists

被引：4

作者：

Stjernlof, P

Lin, CH

Sonesson, C

Svensson, K

Smith, MW

机构：

[1] PHARMACIA & UPJOHN INC,STRUCT ANALYT & MED CHEM RES,KALAMAZOO,MI 49001

[2] PHARMACIA & UPJOHN INC,CNS,DIS RES & DISCOVERY TECHNOL,KALAMAZOO,MI 49001

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(97)10068-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

CNS-active aminotetralins containing phenolic moieties were transformed in a simple two-step procedure to the corresponding benzofurans. The compounds were tested in in vitro binding studies at serotonin 5-HT1A and 5-HT2 and dopamine D-2, D-3 and D-4 receptors. These studies revealed that the furan homologs showed overall lower affinities than the phenol counterparts. This was also reflected in vivo in biochemical studies. The benzofuran compounds retained most of the agonist/antagonist activities but with lower potency.

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页码：2759 / 2764

页数：6

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