Radiosynthesis and initial preclinical evaluation of [11C]AZD1283 as a potential P2Y12R PET radiotracer

• Published in: Nuclear medicine and biology Vol. 114-115; pp. 143 - 150
• Main Authors: Jackson, Isaac M., Buccino, Pablo J., Azevedo, E. Carmen, Carlson, Mackenzie L., Luo, Audrey S.Z., Deal, Emily M., Kalita, Mausam, Reyes, Samantha T., Shao, Xia, Beinat, Corinne, Nagy, Sydney C., Chaney, Aisling M., Anders, David A., Scott, Peter J.H., Smith, Mark, Shen, Bin, James, Michelle L.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.11.2022; Elsevier BV
• Subjects: Alzheimer's disease; Animals; Biocompatibility; Biomarkers; Blood; Blood plasma; Brain; Caco-2 Cells; Carbon-11; Cyanation; Dynamic stability; Efflux; Half-life; High performance liquid chromatography; Humans; In vivo methods and tests; Incubation; Inflammation; Injection; Liquid chromatography; Liver; Macaca mulatta; Medical imaging; Metabolism; Metabolites; Mice; Mice, Knockout; Microglia; Microsomes; Multiple sclerosis; Neurodegenerative diseases; Neuroimaging; Neuroinflammation; Neurological diseases; P2Y12R; Permeability; PET; Positron emission; Positron emission tomography; Positron-Emission Tomography - methods; Radioactive half-life; Radioactive tracers; Radiochemical analysis; Radiolabelling; Stability analysis; Neuroinflammation; Carbon-11; Cyanation; PET; P2Y12R; Microglia

Chronic neuroinflammation and microglial dysfunction are key features of many neurological diseases, including Alzheimer's Disease and multiple sclerosis. While there is unfortunately a dearth of highly selective molecular imaging biomarkers/probes for studying microglia in vivo, P2Y12R has eme...