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

Mingzhang Gao, Min Wang, Gary Hutchins, Qi-Huang Zheng

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

[11C]Dimebon (2-[11C]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-[11C]methylation of desmethyl-Domebon precursor with [11C]CH3OTf and purified with a semi-preparative HPLC method in 30-40% decay corrected radiochemical yield and 222-296 GBq/μmol specific activity at EOB. The measured lipophilicity coefficient (Log P) value of [11C]Dimebon was 2.53.

Original languageEnglish
Pages (from-to)2529-2532
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number8
DOIs
StatePublished - Apr 15 2010

Fingerprint

Huntington Disease
Alzheimer Disease
Imaging techniques
Carbolines
Methylation
High Pressure Liquid Chromatography
latrepirdine

Keywords

  • [C]Dimebon
  • Alzheimer's disease
  • Huntington's disease
  • Lipophilicity
  • Positron emission tomography (PET)
  • Radiosynthesis

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

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abstract = "[11C]Dimebon (2-[11C]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-[11C]methylation of desmethyl-Domebon precursor with [11C]CH3OTf and purified with a semi-preparative HPLC method in 30-40{\%} decay corrected radiochemical yield and 222-296 GBq/μmol specific activity at EOB. The measured lipophilicity coefficient (Log P) value of [11C]Dimebon was 2.53.",
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author = "Mingzhang Gao and Min Wang and Gary Hutchins and Qi-Huang Zheng",
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AU - Wang, Min

AU - Hutchins, Gary

AU - Zheng, Qi-Huang

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