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

  • Bioorg Med Chem. 2007 Jan 15;15(2):903-14. doi: 10.1016/j.bmc.2006.10.038.
Samuel Hintermann  1 ,  Ivo Vranesic ,  Hans Allgeier ,  Armin Brülisauer ,  Daniel Hoyer ,  Michel Lemaire ,  Thomas Moenius ,  Stephan Urwyler ,  Steven Whitebread ,  Fabrizio Gasparini ,  Yves P Auberson
Affiliations
  • 1. Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland.
PMID: 17110115 DOI: 10.1016/j.bmc.2006.10.038
Abstract

[(11)C]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 [(3)H]ABP688, and show that its high affinity (K(d)=2nM), selectivity, and pharmacokinetic properties fulfill all requirements for development as a PET tracer for clinical imaging of the mGlu5 receptor.

Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-110141
    ABP688
    98.02%, human mGluR5 antagonist
    target: mGluR
    Research Areas: Others