Radiosynthesis and in vivo evaluation of [ 11C]MP-10 as a positron emission tomography radioligand for phosphodiesterase 10A

• Published in: Nuclear medicine and biology Vol. 38; no. 6; pp. 875 - 884
• Main Authors: Plisson, Christophe, Salinas, Cristian, Weinzimmer, David, Labaree, David, Lin, Shu-Fei, Ding, Yu-Shin, Jakobsen, Steen, Smith, Paul W., Eiji, Kawanishi, Carson, Richard E., Gunn, Roger N., Rabiner, Eugenii A.
• Format: Journal Article
• Language: English
• Published: New York, NY Elsevier Inc 01.08.2011; Elsevier
• Subjects: Animals; Biological and medical sciences; Brain; Carbon Radioisotopes; Carbon-11; Contrast media. Radiopharmaceuticals; Enzyme Inhibitors - chemical synthesis; Enzyme Inhibitors - metabolism; Female; Humans; In vivo; Kinetics; Ligands; Medical sciences; MP-10; Papio; PDE10A; PET; Pharmacology. Drug treatments; Phosphoric Diester Hydrolases - metabolism; Positron-Emission Tomography - methods; Pyrazoles - chemical synthesis; Pyrazoles - metabolism; Quinolines - chemical synthesis; Quinolines - metabolism; Radiochemistry - methods; Radiology; Substrate Specificity; Swine; In vivo; Brain; PDE10A; MP-10; Carbon-11; PET; Radionuclide study; Nuclear medicine; Central nervous system; Monkey; Esterases; Phosphoric diester hydrolases; Encephalon; Primates; Radioisotopic product; Chemical synthesis; Ungulata; Biomedical engineering; 3',5'-Cyclic-nucleotide phosphodiesterase; Radiolabelling; Enzyme; Enzyme inhibitor; Pig; Vertebrata; Mammalia; Animal; Hydrolases; Artiodactyla; Positron emission tomography; Emission tomography

The aim of this study was to evaluate a newly reported positron emission tomography (PET) radioligand [ 11C]MP-10, a potent and selective inhibitor of the central phosphodiesterase 10A enzyme (PDE10A) in vivo, using PET. A procedure was developed for labeling MP-10 with carbon-11. [ 11C]MP-10 was ev...