1612178-96-7Relevant academic research and scientific papers
Design, synthesis, lipophilic properties, and binding affinities of potential ligands in positron emission tomography (PET) for visualization of brain dopamine D4 receptors
Lacivita, Enza,De Giorgio, Paola,Colabufo, Nicola A.,Berardi, Francesco,Perrone, Roberto,Niso, Mauro,Leopoldo, Marcello
, p. 299 - 310 (2014/03/21)
We report the synthesis of compounds structurally related to the high-affinity dopamine D4 receptor ligand N-{2-[4-(3-cyanopyridin-2- yl)piperazin-1-yl]ethyl}-3-methoxybenzamide (1e). All compounds were specifically designed as potential PET radioligands for brain D4 receptor visualization, having lipophilicity within a range for brain uptake and weak non-specific binding (0.75a substituent for easy access to labeling with the positron emitter isotope 11C or 18F. The best compound of the series, N-{2-[4-(4-chlorophenyl)piperazin-1-yl]ethyl}-6- fluoropyridine-3-carboxamide (7a), displayed excellent selectivity over D 2 and D3 receptors (>100-fold), but its D4 receptor affinity was suboptimal for imaging of brain D4 receptors (Ki=30 nm).
