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Radiotracer Development
UPMC radiochemistry research has focused on neuroscience imaging with particular attention to the serotonin receptor system. Dr. Mathis, senior chemist and director of the PET neuroscience program, has led these efforts. His long-term collaboration with Dr. Klunk (Department of Psychiatry) has produced a novel agent for in vivo imaging of amyloid deposition in Alzheimer’s disease, known as PIB or {N-methyl-[11C]}2-(4’-methylaminophenyl)-6-hydroxybenzothiazole. Recently [18F]FLT was approved for human use and this will be applied to study tumor proliferation. In addition, about 100 other compounds have been radiolabeled and are available for non-human research including [18F]fallypride (dopamine-D2), [11C]MDL 100907 (serotonin-2A), [11C]DASB (serotonin transporter), [18F]FAU and [11C]acetate (tumor proliferation).
Human Use Compounds
Publications
Klunk WE, Wang Y, Huang G-F, Debnath ML, Holt DP, Mathis CA. Uncharged Thioflavin-T Derivatives Bind to Amyloid-Beta Protein with High Affinity and Readily Enter the Brain. Life Sciences 69:1471-1484 (2001).Klunk WE, Bacskai BJ, Mathis CA, Kajdasz ST, McLellan ME, Frosch MP, Debnath ML, Holt DP, Wang Y, and Hyman BT. Imaging Ab plaques in living transgenic mice with multiphoton microscopy and methoxy-X04, a systemically administered Congo red derivative. J. Neuropath. Exptl. Neurol. 61: 797-805 (2002).
Wang Y, Klunk WE, Huang G-F, Debnath ML, Holt DP, and Mathis CA. Synthesis and evaluation of 2-(3'-iodo-4'-amino)-6-hydroxy-benzothiazole for in vivo quantitation of amyloid deposits in Alzheimer's disease. J. Mol. Neurosci. 19: 11-16 (2002).
Bacskai BJ, Klunk WE, Mathis CA, and Hyman BT. Imaging Amyloid-b Deposits In Vivo. J. Cerebral Blood Flow Metab., 22:1035-1041 (2002).
Mathis CA, Bacskai BJ, Kajdasz ST, McLellan ME, Frosch MP, Hyman BT, Holt DP, Wang Y, Huang G-F, Debnath ML, Klunk WE. A Lipophilic Thioflavin T Derivative for Positron Emission Tomography (PET) Imaging of Amyloid in Brain. Bioorganic and Medicinal Chemistry Letters 12: 295-298 (2002).
Mathis CA, Wang Y, Holt DP, Huang G-F, Debnath ML, Klunk WE. Synthesis and Evaluation of 11C-Labeled 6-Substituted 2-Aryl Benzothiazoles as Amyloid Imaging Agents. J. Med. Chem. 46:2740-2755 (2003).
Huang Y, Mahmood K, Mathis CA. An Efficient Synthesis of the Precursors of [C-11]MDL 100907 Labeled in Two Different Positions. J Label Compd Radiopharm 42:949-957 (1999).
Book Chapter: Mason NS, Mathis CA. Radiohalogens for PET imaging. In: Valk PE, Townsend DW, Bailey DB, Maisey MN, Editors. Positron Emission Tomography Basic Science and Clinical Practice. Springer. p. 217-236, 2003.
radiologypethelpdesk@msx.upmc.edu Updated: 7/22/03