Discovery of [11C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors

[Display omitted] Phosphodiesterase 10A (PDE10A) inhibition has recently been identified as a potential mechanism to treat multiple symptoms that manifest in schizophrenia. In order to facilitate preclinical development and support key proof-of-concept clinical trials of novel PDE10A inhibitors, it...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-11, Vol.25 (21), p.4893-4898
Hauptverfasser:	Cox, Christopher D., Hostetler, Eric D., Flores, Broc A., Evelhoch, Jeffrey L., Fan, Hong, Gantert, Liza, Holahan, Marie, Eng, Waisi, Joshi, Aniket, McGaughey, Georgia, Meng, Xiangjun, Purcell, Mona, Raheem, Izzat T., Riffel, Kerry, Yan, Youwei, Renger, John J., Smith, Sean M., Coleman, Paul J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Brain - metabolism Carbon Radioisotopes Crystallography, X-Ray Dose-Response Relationship, Drug Drug Discovery Heterocyclic Compounds, 2-Ring - chemical synthesis Heterocyclic Compounds, 2-Ring - chemistry Huntington’s disease Imaging Macaca mulatta Models, Molecular Molecular Structure PDE10A PET tracer Phosphodiesterase 10A Phosphodiesterase Inhibitors - chemical synthesis Phosphodiesterase Inhibitors - chemistry Phosphodiesterase Inhibitors - metabolism Phosphodiesterase Inhibitors - pharmacology Phosphoric Diester Hydrolases - blood Phosphoric Diester Hydrolases - metabolism Positron emission tomography Rats Schizophrenia Structure-Activity Relationship
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