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  • Title: First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.
    Author: Leopoldo M, Lacivita E, Colabufo NA, Contino M, Berardi F, Perrone R.
    Journal: J Med Chem; 2005 Dec 15; 48(25):7919-22. PubMed ID: 16335915.
    Abstract:
    Structure-affinity relationships of N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as D3 receptor ligands have been well characterized but not structure-activity relationships. In a first attempt to clarify this issue, seven 1-(2,3-dichlorophenyl)piperazine derivatives and their 2-methoxyphenyl counterparts were prepared by varying the arylcarboxamide 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 arylcarboxamide moiety.
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