[(11)C]Dimebon, radiosynthesis and lipophilicity of a new potential PET agent for imaging of Alzheimer's disease and Huntington's disease.

Abstract

[(11)C]Dimebon (2-[(11)C]methyl-8-methyl-5-(2-(6-methylpyridin-3-yl)ethyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole), a new potential PET agent for imaging of Alzheimer's disease and Huntington's disease, was prepared by N-[(11)C]methylation of desmethyl-Domebon precursor with [(11)C]CH(3)OTf and purified with a semi-preparative HPLC method in 30-40% decay corrected radiochemical yield and 222-296GBq/mumol specific activity at EOB. The measured lipophilicity coefficient (LogP) value of [(11)C]Dimebon was 2.53.

• Authors: Mingzhang Gao, Min Wang, Gary D Hutchins, Qi-Huang Zheng
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 8 Pg. 2529-32 (Apr 15 2010) ISSN: 1464-3405 [Electronic] England
• PMID: 20299213 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S.)
• Copyright: Copyright 2010 Elsevier Ltd. All rights reserved.

Chemical References

• Carbon Radioisotopes
• Indoles
• latrepirdine

Topics

• Alzheimer Disease (diagnostic imaging)
• Carbon Radioisotopes
• Chromatography, High Pressure Liquid
• Humans
• Huntington Disease (diagnostic imaging)
• Indoles (chemical synthesis, pharmacology)
• Positron-Emission Tomography