Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands

被引：21

作者：

Banister, Samuel D. ^{[1
]}

Moussa, Iman A. ^{[1
]}

Beinat, Corinne ^{[1
]}

Reynolds, Aaron J. ^{[1
]}

Schiavini, Paolo ^{[1
]}

Jorgensen, William T. ^{[1
]}

Kassiou, Michael ^{[1
,2
,3
]}

机构：

[1] Univ Sydney, Sch Chem, Sydney, NSW 2006, Australia

[2] Brain & Mind Res Inst, Sydney, NSW 2050, Australia

[3] Univ Sydney, Discipline Med Radiat Sci, Sydney, NSW 2006, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 01期

关键词：

Trishomocubanes; Monoamine transporters; Sigma receptors; CNS; Structure-activity relationships; MONOAMINE TRANSPORTERS; IN-VIVO; PHARMACOLOGICAL CHARACTERIZATION; HIGH-AFFINITY; COCAINE; ANALOGS; RADIOLIGAND; CHEMISTRY; PET;

D O I：

10.1016/j.bmcl.2010.11.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In our continued exploration of trishomocubane derivatives with central nervous system (CNS) activity, N-arylalkyl-8-aminopentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecanes (10-13) displaying affinity for the sigma (sigma) receptor were also found, in several cases, to interact with the dopamine transporter (DAT). Compound 12 was identified as the first trishomocubane-derived high affinity DAT ligand (K-1 = 1.2 nM), with greater than 8300-fold selectivity over the monoamine transporters NET and SERT, and only low to moderate affinity for sigma(1) and sigma(2) receptors. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：38 / 41

页数：4

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