Discovery of selective dopamine D4 receptor antagonists: 1-aryloxy-3-(4-aryloxypiperidinyl)-2-propanols

被引：33

作者：

Wright, JL ^{[1
]}

Gregory, TF ^{[1
]}

Heffner, TG ^{[1
]}

MacKenzie, RG ^{[1
]}

Pugsley, TA ^{[1
]}

Meulen, SV ^{[1
]}

Wise, LD ^{[1
]}

机构：

[1] WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES DIV,DEPT THERAPEUT,ANN ARBOR,MI 48105

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(97)00233-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

High volume screening identified 3-(4-benzylpiperidinyl)-1-naphthoxy-2-propanol as a selective dopamine D4 receptor Ligand. A systematic structure-activity study revealed that the benzyl group could be replaced with phenoxy and the naphthalene with phenyl to improve potency almost tenfold. The (R) enantiomer of this compound had a D4 affinity of 2 nM and was over 100-fold weaker at dopamine D2 and D3 receptors. (C) 1997 Elsevier Science Ltd.

引用

页码：1377 / 1380

页数：4

共 8 条

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