In vivo measurement of PDE10A enzyme occupancy by positron emission tomography (PET) following single oral dose administration of PF-02545920 in healthy male subjects

Phosphodiesterase 10A (PDE10A) is an enzyme highly enriched in the striatal medium spiny neurons. It is involved in the regulation of cytoplasmic levels of cAMP and cGMP and signaling within the basal ganglia. This study with PDE10A radioligand [18F]MNI-659 was designed to measure the enzyme occupan...

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Bibliographic Details
Published in:	Neuropharmacology Vol. 117; pp. 171 - 181
Main Authors:	Delnomdedieu, Marielle, Forsberg, Anton, Ogden, Adam, Fazio, Patrik, Yu, Ching-Ray, Stenkrona, Per, Duvvuri, Sridhar, David, William, Al-Tawil, Nabil, Vitolo, Ottavio V., Amini, Nahid, Nag, Sangram, Halldin, Christer, Varrone, Andrea
Format:	Journal Article
Language:	English
Published:	England Elsevier Ltd 01.05.2017
Subjects:	Adult Corpus Striatum - metabolism Enzyme occupancy Fluorine Radioisotopes - metabolism Healthy volunteer Humans Male Middle Aged Models, Biological PDE10 inhibitor PF-02545920 Phosphoric Diester Hydrolases - metabolism Phthalimides - blood Phthalimides - metabolism Positron emission tomography Pyrazoles - adverse effects Pyrazoles - pharmacokinetics Pyrazoles - pharmacology Quinazolinones - blood Quinazolinones - metabolism Quinolines - adverse effects Quinolines - pharmacokinetics Quinolines - pharmacology Radioligand [18F]MNI-659 Radioligand Assay - methods Single dose Enzyme occupancy PDE10 inhibitor Radioligand [18F]MNI-659 PF-02545920 Healthy volunteer Single dose Positron emission tomography Radioligand [F]MNI-659
ISSN:	0028-3908, 1873-7064
Online Access:	Get full text
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