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.
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.
Leopoldo
Marcello
M
Università degli Studi di Bari, Dipartimento Farmaco-Chimico, via Orabona, 4, 70125 Bari, Italy. leopoldo@farmchim.uniba.it
Lacivita
Enza
E
De Giorgio
Paola
P
Contino
Marialessandra
M
Berardi
Francesco
F
Perrone
Roberto
R
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
D000577:Amides; D008024:Ligands; D010879:Piperazines; D019275:Radiopharmaceuticals; D050637:Receptors, Dopamine D3