ArticleBioorganic & medicinal chemistry2014
Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.
Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 22 citations in OpenAlex.
- Synthesis and in vivo biological characterization of six carbon-11 sigma-1 receptor radiotracers in rodent and nonhuman primate.Bioorganic & medicinal chemistry · 2025Article
- Radiation dosimetry of [EJNMMI research · 2025Article
- Challenges on Cyclic Nucleotide Phosphodiesterases Imaging with Positron Emission Tomography: Novel Radioligands and (Pre-)Clinical Insights since 2016.International journal of molecular sciences · 2021Review
- In Vivo Characterization of TwoACS chemical neuroscience · 2018Article
- Synthesis, resolution, and in vitro evaluation of three vesicular acetylcholine transporter ligands and evaluation of the lead fluorine-18 radioligand in a nonhuman primate.Organic & biomolecular chemistry · 2017Article
- Comparison of [Pharmacology research & perspectives · 2016Article
- A novel thermoregulatory role for PDE10A in mouse and human adipocytes.EMBO molecular medicine · 2016Article
- Novel Radioligands for Cyclic Nucleotide Phosphodiesterase Imaging with Positron Emission Tomography: An Update on Developments Since 2012.Molecules (Basel, Switzerland) · 2016Review
- Kinetics modeling and occupancy studies of a novel C-11 PET tracer for VAChT in nonhuman primates.Nuclear medicine and biology · 2016Article
- Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate.Journal of medicinal chemistry · 2015Article
- Preclinical evaluation of a promising C-11 labeled PET tracer for imaging phosphodiesterase 10A in the brain of living subject.NeuroImage · 2015Article
- Molecular Imaging of PDE10A Knockout Mice with a Novel PET Radiotracer: [(11)C]T-773.Molecular imaging and biology · 2015Article
- Radiosynthesis andMedChemComm · 2014Article
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
The radiosyntheses and in vivo evaluation of four carbon-11 labeled quinoline group-containing radioligands are reported here. Radiolabeling of [(11)C]1-4 was achieved by alkylation of their corresponding desmethyl precursors with [(11)C]CH3I. Preliminary biodistribution evaluation in Sprague-Dawley rats demonstrated that [(11)C]1 and [(11)C]2 had high striatal accumulation (at peak time) for [(11)C]1 and [(11)C]2 were 6.0-fold and 4.5-fold at 60 min, respectively. Following MP-10 pretreatment, striatal uptake in rats of [(11)C]1 and [(11)C]2 was reduced, suggesting that the tracers bind specifically to PDE10A. MicroPET studies of [(11)C]1 and [(11)C]2 in nonhuman primates (NHP) also showed good tracer retention in the striatum with rapid clearance from non-target brain regions. Striatal uptake (SUV) of [(11)C]1 reached 1.8 at 30 min with a 3.5-fold striatum:cerebellum ratio. In addition, HPLC analysis of solvent extracts from NHP plasma samples suggested that [(11)C]1 had a very favorable metabolic stability. Our preclinical investigations suggest that [(11)C]1 is a promising candidate for quantification of PDE10A in vivo using PET.
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