Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR

Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR
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DOI:
10.1016/j.bmcl.2006.10.076
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发表时间:
2007-02-01
影响因子:
2.7
通讯作者:
Newman, Amy Hauck
Newman, Amy Hauck
中科院分区:
医学4区
文献类型:
--
作者:
Grundt, Peter;Husband, Sarah Little Jane;Newman, Amy Hauck

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合成了多巴胺D2受体拮抗剂L741,626的一系列类似物,并评价了其在D2家族受体亚型上的结合和功能。几种类似物显示出与母体配体相当的结合特征,然而,一般而言,化学修饰有助于降低D2结合亲和力和选择性。(c)2006爱思唯尔有限公司保留所有权利。
A series of analogues of the dopamine D2 receptor antagonist L741,626 were synthesized and evaluated for binding and function at D2 family receptor subtypes. Several analogues showed comparable binding profiles to the parent ligand, however, in general, chemical modification served to reduce D2 binding affinity and selectivity. (c) 2006 Elsevier Ltd. All rights reserved.