First structure-activity relationship study on dopamine D-3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]-arylcarboxamide structure

Leopoldo M; Lacivita E; Colabufo NA; Contino M; Berardi F; Perrone R

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First structure-activity relationship study on dopamine D-3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]-arylcarboxamide structure

机译：具有N- [4-（4-芳基哌嗪-1-基）丁基]-芳基甲酰胺结构的多巴胺D-3受体药物的第一构效关系研究

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Structure-affinity relationships of N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as D-3 receptor ligands have been well characterized but not structure-activity relationships. In a first attempt to clarify this issue, seven 1-(2,3dichlorophenyl)piperazine derivatives and their 2-methoxyphenyl counterparts were prepared by varying the arylcarbox-amide moiety. They were tested for D3 receptor binding affinities and in the Eu-GTP binding assay in order to evaluate their intrinsic activity. We have found that the intrinsic activity strongly depended on the nature of the arylearboxamide moiety.

机译：作为D-3受体配体的N- [4-（4-芳基哌嗪-1-基）丁基]芳基甲酰胺的结构亲和力关系已得到很好的表征，但没有结构活性关系。为了澄清这个问题，我们首先尝试通过改变芳基羧酰胺部分来制备七个1-（2,3-二氯苯基）哌嗪衍生物及其2-甲氧基苯基对应物。为了评估其内在活性，对它们进行了D3受体结合亲和力和Eu-GTP结合测定的测试。我们已经发现内在活性强烈地取决于芳基脂酰胺部分的性质。

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《Journal of Medicinal Chemistry》 |2005年第25期|共4页
作者
Leopoldo M; Lacivita E; Colabufo NA; Contino M; Berardi F; Perrone R;
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正文语种 eng
中图分类药学;
关键词
D-3 RECEPTOR LIGANDS; COCAINE-SEEKING BEHAVIOR; THERAPEUTIC AGENTS; PARTIAL AGONISTS; ANTAGONISTS; POTENT; INHIBITION; AFFINITY; BINDING; BP-897;

机译：D-3受体配体;可卡因的行为;治疗剂;RTI部激动剂;拮抗剂;药力;抑制作用;亲和力;结合力;BP-897;

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1. First structure-activity relationship study on dopamine D-3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]-arylcarboxamide structure [J] . Leopoldo M, Lacivita E, Colabufo NA, Journal of Medicinal Chemistry . 2005,第25期

机译：具有N- [4-（4-芳基哌嗪-1-基）丁基]-芳基甲酰胺结构的多巴胺D-3受体药物的第一构效关系研究
2. C-11-labeling of N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamide derivatives and evaluation as potential radioligands for PET imaging of dopamine D-3 receptors [J] . Turolla EA, Matarrese M, Belloli S, Journal of Medicinal Chemistry . 2005,第22期

机译：C-11-标记N- [4- [4-（2,3-二氯苯基）哌嗪-1-基]丁基]芳基甲酰胺衍生物并评估其作为多巴胺D-3受体PET成像的潜在放射性配体
3. Heterocyclic Analogues of N-(4-(4-(2,3-Dichlorophenyl)piperazin-l-yl)butyl)arylcarboxamides with Functionalized Linking Chains as Novel Dopamine D3 Receptor Ligands:Potential Substance Abuse Therapeutic Agents [J] . Peter Grundt, Katherine M.Prevatt, Jianjing Cao Journal of Medicinal Chemistry . 2007,第17期

机译：具有新型多巴胺D3受体配体的N-（4-（4-（2,3-二氯苯基）哌嗪-1-基）丁基）芳基羧酰胺的杂环类似物：潜在的药物滥用治疗剂
4. DFT studies on the quantitative structure-activity relationship of N-(2-chloroethyl)-N′-cyclohexyl-N-nitrosoureas as anticancer agents [C] . Cao Jun, Jin Shubin, Han Bing, 2010 3rd International Conference on Biomedical Engineering and Informatics . 2010

机译：DFT研究N-（2-氯乙基）-N'-环己基-N-亚硝基脲作为抗癌剂的定量构效关系
5. A structure-activity approach to drug action in pharmacology: (A) Structure-activity relationships involved in DT-diaphorase (NQO1) mediated reduction kinetics and mode of action of anticancer bioreductive benzoquinone alkylating agents. (B) Structural characteristics of novel NMDA receptor antagonists required for renal tubule organic cation secretion . [D] . Fourie, Jeanne. 2004

机译：一种在药理学中用于药物作用的结构活性方法：（A）DT-黄递酶（NQO1）介导的抗癌生物还原苯醌烷基化剂的还原动力学和作用方式的结构活性关系。（B）肾小管有机阳离子分泌所需的新型NMDA受体拮抗剂的结构特征。
6. Divergent Cytotoxic and Metabolically Stimulative Functions of Sigma-2 Receptors: Structure-Activity Relationships of 6-Acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzodoxazol-2(3H)-one (SN79) Derivatives [O] . Hilary E. Nicholson, Walid F. Alsharif, Anthony B. Comeau, -1

机译：Sigma-2受体的不同细胞毒性和代谢刺激功能：6-乙酰基-3-（4-（4-（4-（4-氟苯基）哌嗪-1-基）丁基）苯并d恶唑-2（）的结构-活性关系3H）-一（SN79）衍生物
7. Heterocyclic Analogues of N-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with Functionalized Linking Chains as Novel Dopamine D3 Receptor Ligands: Potential Substance Abuse Therapeutic Agents [O] . -1

机译：N-（4-（2,3-（4-二氯苯基）哌嗪-1-基）丁基）芳基甲酰酰胺的杂环类似物，其具有官能化连接链作为新型多巴胺D3受体配体：潜在的药物滥用治疗剂

First structure-activity relationship study on dopamine D-3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]-arylcarboxamide structure

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