Discovery of Bishomo(hetero)arylpiperazines as Novel Multifunctional Ligands Targeting Dopamine D3 and Serotonin 5-HT1A and 5-HT2A Receptors

被引：26

作者：

Butini, Stefania ^{[1
,2
]}

Campiani, Giuseppe ^{[1
,2
]}

Franceschini, Silvia ^{[1
,2
]}

Trotta, Francesco ^{[1
,2
]}

Kumar, Vinod ^{[1
,2
]}

Guarino, Egeria ^{[1
,2
]}

Borrelli, Giuseppe ^{[1
,2
]}

Fiorini, Isabella ^{[1
,2
]}

Novellino, Ettore ^{[1
,3
,4
]}

Fattorusso, Caterina ^{[1
,3
,4
]}

Persico, Marco ^{[1
,3
,4
]}

Orteca, Nausicaa ^{[1
,3
,4
]}

Sandager-Nielsen, Karin ^{[5
]}

Jacobsen, Thomas Amos ^{[5
]}

Madsen, Kim ^{[5
]}

Scheel-Kruger, Jorgen ^{[5
]}

Gemma, Sandra ^{[1
,2
]}

机构：

[1] Univ Siena, European Res Ctr Drug Discovery & Dev, I-53100 Siena, Italy

[2] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy

[3] Univ Naples Federico II, Dipartimento Chim Sostanze Nat, I-80131 Naples, Italy

[4] Univ Naples Federico II, Dipartimento Chim Farmaceut & Tossicol, I-80131 Naples, Italy

[5] NeuroSearch AS, DK-2750 Ballerup, Denmark

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 12期

关键词：

ATYPICAL ANTIPSYCHOTIC AGENTS; DESIGN;

D O I：

10.1021/jm100294b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

As a continuation of our efforts to develop innovative ligands for D-3, 5-HT1A, and 5-HT2A receptors with low propensity to block hERG channels, we propose a series bishetero(homo)arylpiperazines 5a-m as novel and potent multifunctional ligands characterized by low occupancy at D-2 and 5-HT2C receptors.

引用

页码：4803 / 4807

页数：5

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