Hintermann, Samuel, Vranesic, Ivan-Toma, Allgeier, Hans, Bruelisauer, Armin, Hoyer, Daniel, Lemaire, Michel, Moenius, Thomas, Urwyler, Stephan, Whitebread, Steven, Gasparini, Fabrizio and Auberson, Yves (2007) ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies. Bioorganic & Medicinal Chemistry, 15 (2). pp. 903-914. ISSN 0968-0896

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.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmc.2006.10.038
Additional Information:	author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords:	Metabotropic glutamate receptor subtype 5; [3H]ABP688; ABP688; PET imaging
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmc.2006.10.038
Date Deposited:	14 Dec 2009 13:57
Last Modified:	31 Jan 2013 01:13
URI:	https://oak.novartis.com/id/eprint/569