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Bioorg Med Chem. 2009 Jan 15;17(2):758-66. doi: 10.1016/j.bmc.2008.11.044. Epub 2008 Nov 24.

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.

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1
Università degli Studi di Bari, Dipartimento Farmaco-Chimico, via Orabona, 4, 70125 Bari, Italy. leopoldo@farmchim.uniba.it

Abstract

In the search for compounds with potential for development as positron emission tomography radioligands for brain D(3) 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 D(3) receptor affinities but lacked selectivity over D(2) receptors.

PMID:
19081257
DOI:
10.1016/j.bmc.2008.11.044
[Indexed for MEDLINE]

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