Effect of the myeloperoxidase inhibitor AZD3241 on microglia: a PET study in Parkinson’s disease

• Published in: Brain (London, England : 1878) Vol. 138; no. 9; pp. 2687 - 2700
• Main Authors: Jucaite, Aurelija, Svenningsson, Per, Rinne, Juha O., Cselényi, Zsolt, Varnäs, Katarina, Johnström, Peter, Amini, Nahid, Kirjavainen, Anna, Helin, Semi, Minkwitz, Margaret, Kugler, Alan R., Posener, Joel A., Budd, Samantha, Halldin, Christer, Varrone, Andrea, Farde, Lars
• Format: Journal Article
• Language: English
• Published: England 01.09.2015
• Subjects: Aged; Dose-Response Relationship, Drug; Double-Blind Method; Enzyme Inhibitors - therapeutic use; Female; Fluorine Radioisotopes; Follow-Up Studies; Humans; Male; Microglia - diagnostic imaging; Microglia - drug effects; Middle Aged; Parkinson Disease - diagnostic imaging; Parkinson Disease - drug therapy; Parkinson Disease - pathology; Polymorphism, Single Nucleotide - genetics; Positron-Emission Tomography; Protein Binding - drug effects; Pyrimidines - blood; Pyrimidinones - pharmacology; Pyrimidinones - therapeutic use; Pyrroles - pharmacology; Pyrroles - therapeutic use; Receptors, GABA - genetics; Severity of Illness Index; 18kDa translocator protein; positron emission tomography; microglia; Parkinson’s disease

Impaired mitochondrial function, oxidative stress and formation of excessive levels of reactive oxygen species play a key role in neurodegeneration in Parkinson's disease. Myeloperoxidase is a reactive oxygen generating enzyme and is expressed by microglia. The novel compound AZD3241 is a selec...