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.
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收藏
页码：3063 / 3066
页数：4
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