Fully automated synthesis and initial PET evaluation of [ 11C]PBR28

• Published in: Bioorganic & medicinal chemistry letters Vol. 19; no. 19; pp. 5636 - 5639
• Main Authors: Wang, Min, Yoder, Karmen K., Gao, Mingzhang, Mock, Bruce H., Xu, Xiao-Ming, Saykin, Andrew J., Hutchins, Gary D., Zheng, Qi-Huang
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 01.10.2009; Elsevier
• Subjects: [ 11C]PBR28; Animals; Biological and medical sciences; Brain imaging; Carbon Radioisotopes; Carrier Proteins - antagonists & inhibitors; Carrier Proteins - metabolism; Contrast media. Radiopharmaceuticals; Female; GABA-A Receptor Antagonists; Ligands; Medical sciences; Pharmacology. Drug treatments; Positron emission tomography (PET); Positron-Emission Tomography; Pyrimidines - chemical synthesis; Pyrimidines - chemistry; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - chemistry; Radiosynthesis; Rats; Rats, Sprague-Dawley; Receptors, GABA-A - metabolism; Translocator protein (TSPO); Traumatic brain injury (TBI); [ 11C]PBR28; Positron emission tomography (PET); Traumatic brain injury (TBI); Brain imaging; Translocator protein (TSPO); Radiosynthesis; Intravenous administration; Rat; Nitrogen heterocycle; Ligand; Central nervous system; Carbon Isotopes; Encephalon; Scintigraphic agent; C]PBR28; Carbon 11; [; Chemical synthesis; Peripheral benzodiazepine receptor; Nervous system diseases; Automation; Ether; Radiolabelling; Rodentia; Vertebrata; Mammalia; Animal; Distribution; Phenols; Carboxamide; Benzenic compound; Iodomethane; Head trauma; Positron emission tomography
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2009.08.051

Fully automated synthesis and initial PET evaluation of a TSPO radioligand [ 11C]PBR28 are reported. Fully automated synthesis and initial PET evaluation of a TSPO radioligand, [ 11C]PBR28 ( N-(2-[ 11C]methoxybenzyl)- N-(4-phenoxypyridin-3-yl)acetamide), are reported. These results facilitate the potential preclinical and clinical PET studies of [ 11C]PBR28 in animals and humans.