Synthesis of radiotracers for studying muscarinic cholinergic receptors in the living human brain using positron emission tomography: [11C]dexetimide and [11C]levetimide |
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| Affiliation: | 1. Divisions of Nuclear Medicine and Radiation Health Sciences, The Johns Hopkins Medical Institutions, 615 North Wolfe Street, Baltimore, MD 21205-2179, U.S.A.;2. Department of Organic Chemistry, Institute of Chemistry, Uppsala University, S-751 21, Sweden |
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| Abstract: | Dexetimide (Fig. 1a), a potent muscarinic cholinergic receptor antagonist, and levetimide (Fig. 1b), its pharmacologically inactive enantiomer, were labeled with 11C for non-invasive in vivo studies of muscarinic cholinergic receptors in the human brain using positron emission tomography. The syntheses were completed in approximately 32 min using [α-11C]benzyl iodide as the precursor. The synthesis, purification, characterization and determination of specific activity are presented and discussed. |
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