New 3-[4-(3-substiluted phenyl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)-propanol derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants

被引：0
|
作者：
Orús, L
Martínez, J
Pérez, S
Oficialdegui, AM
Del Castillo, JC
Mourelle, M
Lasheras, B
del Río, J
Monge, A
机构：
[1] Univ Navarra, Dept Med Chem, CIFA, E-31080 Pamplona, Spain
[2] Univ Navarra, Dept Pharmacol, CIFA, E-31080 Pamplona, Spain
[3] Vita Invest SA, Barcelona, Spain
来源：
PHARMAZIE | 2002年 / 57卷 / 08期
关键词：
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In this paper a series of new, 3-[4-(3-substituted phenylpiperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propanol derivatives is presented as a new class of antidepressant drugs with dual activity at 5-HT1A serotonin receptors and serotonin transporter. The 5-HT1A receptor and 5-HT transporter binding affinities of hydroxylic compounds 4 a-e have been determined. The new compounds present nanomolar affinity for both activities, and 1-(benzo[b]thiophen-3-yl)-3-[4-(3-methoxyphenyl)piperazin-1-yl]propan-1-ol (4d) shows values (nM) of K-i = 86 for 5-HT1A receptors and K-i = 76 for the serotonin transporter, respectively.
引用
收藏
页码：515 / 518
页数：4
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