Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics

被引：17

作者：

Alvarado, M

Coelho, A

Masaguer, CF

Raviña, E

Brea, J

Padín, JF

Loza, MI

机构：

[1] Univ Santiago de Compostela, Dept Quim Organ, Lab Quim Farmaceut, Fac Farm, E-15782 Santiago De Compostela, Spain

[2] Univ Santiago de Compostela, Dept Farmacol, Fac Farm, E-15782 Santiago De Compostela, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 12期

关键词：

aminoethyltetralones; valerophenones; dopamine receptors; serotonin receptors; antipsychotics;

D O I：

10.1016/j.bmcl.2005.04.022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-aminoethyl-1-tetralones, conformationally constrained higher homologues of haloperidol (standard for typical antipsychotic profile), have been obtained by a four-step route from valerolactone. Their binding affinities at dopamine D-2 and serotonin 5-HT2A and 5-HT2C receptors were determined, showing in some cases an atypical antipsychotic profile. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：3063 / 3066

页数：4

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