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Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D3 receptor ligands.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-07-11 , DOI: 10.1016/j.bmcl.2019.07.020 Peng-Jen Chen 1 , Michelle Taylor 2 , Suzy A Griffin 2 , Armaghan Amani 3 , Hamed Hayatshahi 3 , Kenneth Korzekwa 1 , Min Ye 1 , Robert H Mach 4 , Jin Liu 3 , Robert R Luedtke 2 , John C Gordon 1 , Benjamin E Blass 1
中文翻译：
设计，合成和评估N-（4-（4-苯基哌嗪-1-基）丁基）-4-（噻吩-3-基）苯甲酰胺作为选择性多巴胺D3受体配体。
更新日期：2019-07-11
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-07-11 , DOI: 10.1016/j.bmcl.2019.07.020 Peng-Jen Chen 1 , Michelle Taylor 2 , Suzy A Griffin 2 , Armaghan Amani 3 , Hamed Hayatshahi 3 , Kenneth Korzekwa 1 , Min Ye 1 , Robert H Mach 4 , Jin Liu 3 , Robert R Luedtke 2 , John C Gordon 1 , Benjamin E Blass 1
Affiliation
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As part of our on-going effort to explore the role of dopamine receptors in drug addiction and identify potential novel therapies for this condition, we have a identified a series of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamide D3 ligands. Members of this class are highly selective for D3 versus D2, and we have identified two compounds (13g and 13r) whose rat in vivo IV pharmacokinetic properties that indicate that they are suitable for assessment in in vivo efficacy models of substance use disorders.
中文翻译：
设计，合成和评估N-（4-（4-苯基哌嗪-1-基）丁基）-4-（噻吩-3-基）苯甲酰胺作为选择性多巴胺D3受体配体。
为了探索多巴胺受体在药物成瘾中的作用并确定针对这种情况的潜在新疗法，我们正在进行的工作包括确定一系列N-（4-（4-苯基哌嗪-1-基）丁基）-4-（噻吩-3-基）苯甲酰胺D 3配体。该类别的成员对D 3和D 2具有高度选择性，并且我们鉴定了两种化合物（13g和13r），它们的大鼠体内IV药代动力学特性表明它们适用于评估物质使用失调的体内功效模型。
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