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

Hintermann, Samuel and Vranesic, Ivan-Toma and Allgeier, Hans and Bruelisauer, Armin and Hoyer, Daniel and Lemaire, Michel and Moenius, Thomas and Urwyler, Stephan and Whitebread, Steven and 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
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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
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Date Deposited: 14 Dec 2009 13:57
Last Modified: 31 Jan 2013 01:13
URI: https://oak.novartis.com/id/eprint/569

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