Document Report Card

ID: ALA1140426

Journal: J Med Chem

Title: First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.

Authors: Leopoldo M, Lacivita E, Colabufo NA, Contino M, Berardi F, Perrone R.

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.

CiteXplore: 16335915

DOI: 10.1021/jm050729o