ArticleClinical psychopharmacology and neuroscience : the official scientific journal of the Korean College of Neuropsychopharmacology2012
In Vivo Evaluation of (11)C-labeled Three Radioligands for Glycine Transporter 1 in the Mouse Brain.
Article in Clinical psychopharmacology and neuroscience : the official scientific journal of the Korean College of Neuropsychopharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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- Prediction of Locomotor Activity by Infrared Motion Detector on Sleep-wake State in Mice.Clinical psychopharmacology and neuroscience : the official scientific journal of the Korean College of Neuropsychopharmacology · 2021Article
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5 authors at 2 institutions in 1 country.
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Abstract
objectiveGlycine transporter 1 (GlyT-1) is one of the most attractive therapeutic targets for schizophrenia. There is great interest in developing radioligands for in vivo imaging of GlyT-1 in the brain using positron emission tomography. Here, we report the properties of three novel non-sarcosine-based radioligands [(11)C]CHIBA-3007, [(11)C]CHIBA-3009, and [(11)C]CHIBA-3011, for GlyT-1 imaging in the mouse brain in vivo.
methodsThe three radioligands were synthesized by N-[(11)C] methylation of the corresponding desmethyl precursor. A pharmacological characterization of these radioligands for in vivo imaging of GlyT-1 in the brain was conducted using male ddY mice.
results[(11)C]CHIBA-3009 and [(11)C]CHIBA-3011 were scarcely incorporated into the brain, whereas [(11)C]CHIBA-3007 showed slight but considerable brain uptake. Regional brain uptake of [(11)C]CHIBA-3007 (medulla oblongata>cerebellum>cortex) was similar to the distribution of the GlyT-1 protein. However, pretreatment with CHIBA-3007 (1 mg/kg) or the GlyT-1 selective inhibitor ALX5407 (N-[(3R)-3-([1,1'-Biphenyl]-4-yloxy)-3-(4-fluorophenyl)propyl]-N-methylglycine) (30 mg/kg) did not significantly decrease brain uptake of [(11)C]CHIBA-3007, suggesting low specific binding to GlyT-1. Pretreatment with cyclosporin A significantly increased brain uptake of [(11)C]CHIBA-3009 and [(11)C]CHIBA-3011, suggesting a role for P-glycoprotein in the brain uptake of these ligands. All three radioligands were rapidly degraded intact forms were 3-18% in plasma and 15-74% in the brain at 15 min after injection.
conclusionThe results suggest that these three radioligands are not suitable for in vivo imaging of GlyT-1 in the brain because of low brain uptake and rapid metabolism. Further structural refinement is necessary to enhance brain uptake.
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