In the search for compounds with potential for development as positron emission tomography radioligands for brain D3 receptor imaging, a series of N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides with appropriate lipophilicity (2 < logP < 3.5) were synthesized and tested in vitro. Some of the final compounds showed moderate-to-high dopamine D3 receptor affinities but lacked selectivity over D2 receptors.
Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II
LEOPOLDO, Marcello;LACIVITA, ENZA;CONTINO, MARIALESSANDRA;BERARDI, Francesco;PERRONE, Roberto
2009-01-01
Abstract
In the search for compounds with potential for development as positron emission tomography radioligands for brain D3 receptor imaging, a series of N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides with appropriate lipophilicity (2 < logP < 3.5) were synthesized and tested in vitro. Some of the final compounds showed moderate-to-high dopamine D3 receptor affinities but lacked selectivity over D2 receptors.File in questo prodotto:
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