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.
MeSH terms
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Animals
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Autoradiography
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Binding, Competitive / drug effects
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Blood Proteins / metabolism
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Cell Line
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Chemical Phenomena
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Chemistry, Physical
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Cricetinae
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Excitatory Amino Acid Agonists / pharmacology
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Humans
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In Vitro Techniques
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Indicators and Reagents
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Injections, Intravenous
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Ligands
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Male
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Mass Spectrometry
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Microsomes, Liver / drug effects
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Microsomes, Liver / metabolism
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Oximes / pharmacokinetics*
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Oximes / pharmacology*
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Phosphatidylinositols / metabolism
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Positron-Emission Tomography
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Protein Binding
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Pyridines / pharmacokinetics*
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Pyridines / pharmacology*
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Quisqualic Acid / antagonists & inhibitors
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Quisqualic Acid / pharmacology
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Radiopharmaceuticals / chemical synthesis
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Rats
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Rats, Sprague-Dawley
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Rats, Wistar
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Receptors, Kainic Acid / drug effects*
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Tissue Distribution
Substances
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3-(6-methylpyridin-2-ylethynyl)cyclohex-2-enone-O-methyloxime
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Blood Proteins
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Excitatory Amino Acid Agonists
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Gluk1 kainate receptor
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Indicators and Reagents
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Ligands
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Oximes
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Phosphatidylinositols
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Pyridines
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Radiopharmaceuticals
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Receptors, Kainic Acid
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6-methyl-2-(phenylethynyl)pyridine
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Quisqualic Acid