title: 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.
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.
authors.affiliation: Università degli Studi di Bari, Dipartimento Farmaco-Chimico, via Orabona, 4, 70125 Bari, Italy. leopoldo@farmchim.uniba.it
authors.forename: Marcello
authors.initials: M
authors.lastname: Leopoldo
authors.forename: Enza
authors.initials: E
authors.lastname: Lacivita
authors.forename: Paola
authors.initials: P
authors.lastname: De Giorgio
authors.forename: Marialessandra
authors.initials: M
authors.lastname: Contino
authors.forename: Francesco
authors.initials: F
authors.lastname: Berardi
authors.forename: Roberto
authors.initials: R
authors.lastname: Perrone
mesh_terms: D000577:Amides / Q000138:chemical synthesis*; D015195:Drug Design; D006801:Humans; D008024:Ligands; D010879:Piperazines / Q000138:chemical synthesis*; D049268:Positron-Emission Tomography / Q000379:methods*; D011485:Protein Binding; D019275:Radiopharmaceuticals; D050637:Receptors, Dopamine D3 / Q000032:analysis* / Q000378:metabolism
chemical_list: D000577:Amides; D008024:Ligands; D010879:Piperazines; D019275:Radiopharmaceuticals; D050637:Receptors, Dopamine D3