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Bioorg Med Chem. 2007 Jan 15;15(2):903-14. Epub 2006 Oct 21.

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

Author information

1
Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland.

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.

PMID:
17110115
DOI:
10.1016/j.bmc.2006.10.038
[Indexed for MEDLINE]

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