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

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

Affiliation

  • 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.

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Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-110141
    98.02%, human mGluR5 antagonist