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Design, Synthesis, Lipophilic Properties, and Binding Affinities of Potential Ligands in Positron Emission Tomography (PET) for Visualization of Brain Dopamine D 4 Receptors
Author(s) -
Lacivita Enza,
De Giorgio Paola,
Colabufo Nicola A.,
Berardi Francesco,
Perrone Roberto,
Niso Mauro,
Leopoldo Marcello
Publication year - 2014
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201300194
Subject(s) - chemistry , lipophilicity , ligand (biochemistry) , receptor , affinities , stereochemistry , dopamine , sch 23390 , dopamine receptor d2 , dopamine receptor , neuroscience , biochemistry , psychology
We report the synthesis of compounds structurally related to the high‐affinity dopamine D 4 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 D 4 receptor visualization, having lipophilicity within a range for brain uptake and weak non‐specific binding (0.75100‐fold), but its D 4 receptor affinity was suboptimal for imaging of brain D 4 receptors ( K i =30 n M ).
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