Abstract
[11C]L-159,884 ([11C] N-[[4'[(2-ethyl-5,7-dimethyl-3H- imidazo[4,5-b]pyridin-3-yl) methyl] [1,1'-biphenyl]-2-yl] sulfonyl]-4-methoxybenzamide) and [11C]L-162,574 ([11C] N-[[4'[2-ethyl-5,7- dimethyl-3H-imidazo[4,5-b] pyridin-3-yl)methyl] [1,1'-biphenyl]-2-yl]sulfonyl]-3- methoxybenzamide), both potent and selective ligands for the AT1 receptor, were prepared by C-11 methylation of the corresponding desmethyl phenolic precursors. The radiotracers were purified by semi-preparative reverse-phase HPLC. Non-decay corrected radiochemical yields were 5 and 3% for L-159,884 and L-162,574 respectively, and the average specific activity was 2979 mCi/mumol at end-of-synthesis (EOS). The average time of synthesis was 18 min.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Angiotensin I / metabolism*
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Angiotensin II / antagonists & inhibitors*
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Angiotensin Receptor Antagonists
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Carbon Radioisotopes / chemistry*
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Chromatography, High Pressure Liquid
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Hydrocarbons, Iodinated / chemistry
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Image Processing, Computer-Assisted
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Imidazoles / chemical synthesis
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Imidazoles / metabolism*
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Isotope Labeling / methods
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Pyridines / chemical synthesis
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Pyridines / metabolism*
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Receptors, Angiotensin / metabolism*
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Tomography, Emission-Computed
Substances
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Angiotensin Receptor Antagonists
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Carbon Radioisotopes
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Hydrocarbons, Iodinated
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Imidazoles
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L 162574
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Pyridines
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Receptors, Angiotensin
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Angiotensin II
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L 159884
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Angiotensin I
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methyl iodide