ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors:: Identification, in vitro pharmacology, pharmacokinetic and biodistribution studies

[C-11]ABP688 (2) has recently been demonstrated to be a useful PET tracer for in vivo imaging of the metabotropic glutamate receptors type 5 (mGluR5) in rodents. We describe here the identification and preclinical profiling of ABP688 and its tritiated version [H-3]ABP688, and show that its high affinity (K-d = 2 nM), selectivity, and pharmacokinetic properties fulfill all requirements for development as a PET tracer for clinical imaging of the mGlu5 receptor. (c) 2006 Elsevier Ltd. All rights reserved.