Abstract:
:Gene therapy based on gene delivery is a promising strategy for the treatment of various human diseases such as cancer. Cationic lipids represent one of the important synthetic gene delivery systems. There is a great interest in imaging of gene therapy using the biomedical imaging technique positron emission tomography (PET). Carbon-11-labeled cholesterol-based cationic lipids were first designed and synthesized as new potential PET probes for imaging of gene delivery in cancer. The [(11)C-methyl]quaternary amine target tracers, N-[(11)C]methyl-N-[4-(cholest-5-en-3beta-yloxycarbonyl)butyl]pyrrolidinium iodide ([(11)C]4a), N-[(11)C]methyl-N'-[4-(cholest-5-en-3beta-yloxycarbonyl)butyl]imidazolium iodide ([(11)C]4b), N-[(11)C]methyl-N-[4-(cholest-5-en-3beta-yloxycarbonyl)butyl]piperidinium iodide ([(11)C]4c), N-[(11)C]methyl-N-[4-(cholest-5-en-3beta-yloxycarbonyl)butyl]-4-methylpiperidinium iodide ([(11)C]4d), and N-[(11)C]methyl-N-[4-(cholest-5-en-3beta-yloxycarbonyl)butyl]morpholinium iodide ([(11)C]4e), were prepared from their corresponding tertiary amine precursors with [(11)C]methyl iodide ([(11)C]CH(3)I) through N-[(11)C]methylation and isolated by a simplified solid-phase extraction (SPE) method using a Silica Sep-Pak cartridge in 50-60% radiochemical yields decay corrected to end-of-bombardment (EOB), based on [(11)C]CO(2), and 111-185GBq/mumol specific activity at the end of synthesis (EOS).
journal_name
Steroidsjournal_title
Steroidsauthors
Gao M,Wang M,Miller KD,Sledge GW,Hutchins GD,Zheng QHdoi
10.1016/j.steroids.2010.04.009subject
Has Abstractpub_date
2010-10-01 00:00:00pages
715-20issue
10eissn
0039-128Xissn
1878-5867pii
S0039-128X(10)00114-5journal_volume
75pub_type
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