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

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 21, 2015, Pages 4893-4898

  Cox, Christopher D ^a   Hostetler, Eric D ^a   Flores, Broc A ^a   Evelhoch, Jeffrey L ^a   Fan, Hong ^a   Gantert, Liza ^a   Holahan, Marie ^a   Eng, Waisi ^a   Joshi, Aniket ^a   McGaughey, Georgia ^a   Meng, Xiangjun ^a   Purcell, Mona ^a   Raheem, Izzat T ^a   Riffel, Kerry ^a   Yan, Youwei ^a   Renger, John J ^a   Smith, Sean M ^a   Coleman, Paul J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Huntington's disease; Imaging; PDE10A; PET tracer; Phosphodiesterase 10A; Positron emission tomography; Schizophrenia

Indexed keywords

CARBON 11; MK 8193 C 11; PHOSPHODIESTERASE; PHOSPHODIESTERASE 10A; PHOSPHODIESTERASE 10A INHIBITOR; PHOSPHODIESTERASE INHIBITOR; TRACER; UNCLASSIFIED DRUG; CARBON; FUSED HETEROCYCLIC RINGS; MK-8193;

ARTICLE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HIGH THROUGHPUT SCREENING; LIGAND BINDING; LIPOPHILICITY; NONHUMAN; NUCLEAR MAGNETIC RESONANCE IMAGING; ONE POT SYNTHESIS; PLASMA PROTEIN BINDING; POSITRON EMISSION TOMOGRAPHY; RAT; RHESUS MONKEY; STRUCTURE ACTIVITY RELATION; ANIMAL; BLOOD; BRAIN; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; METABOLISM; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

ANIMALS; BRAIN; CARBON RADIOISOTOPES; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HETEROCYCLIC COMPOUNDS, 2-RING; MACACA MULATTA; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PHOSPHODIESTERASE INHIBITORS; PHOSPHORIC DIESTER HYDROLASES; POSITRON-EMISSION TOMOGRAPHY; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84944168763     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.05.080     Document Type: Article

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