Journal article
ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: Identification, in vitro pharmacology, pharmacokinetic and biodistribution studies
S Hintermann, I Vranesic, H Allgeier, A Brülisauer, D Hoyer, M Lemaire, T Moenius, S Urwyler, S Whitebread, F Gasparini, YP Auberson
Bioorganic and Medicinal Chemistry | Published : 2007
Abstract
[11C]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 [3H]ABP688, and show that its high affinity (Kd = 2 nM), selectivity, and pharmacokinetic properties fulfill all requirements for development as a PET tracer for clinical imaging of the mGlu5 receptor. © 2006 Elsevier Ltd. All rights reserved.