Synthesis and in vivo evaluation of [11C]MPTQ: A potential PET tracer for alpha2A-adrenergic receptors |
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| Authors: | Jaya Prabhakaran Vattoly J. Majo Matthew S. Milak Pratap Mali Lyudmila Savenkova J. John Mann Ramin V. Parsey J.S. Dileep Kumar |
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| Affiliation: | 1. Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University, New York, United States;2. New York State Psychiatric Institute, New York, United States;3. Department of Radiology, Columbia University, New York, NY 10032, United States |
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| Abstract: | Radiosynthesis and in vivo evaluation of [N-methyl-11C] 5-methyl-3-[4-(3-phenylallyl)-piperazin-1-ylmethyl]-3,3a,4,5-tetrahydroisoxazolo[4,3-c]quinoline (1), a potential PET tracer for alpha2-adrenergic receptors is described. Syntheses of nonradioactive standard 1 and corresponding desmethyl precursor 2 were achieved from 2-aminobenzaldehyde in 40% and 65% yields, respectively. Methylation using [11C]CH3I in presence of aqueous potassium hydroxide in DMSO afforded [11C]1 in 25% yield (EOS) with >99% chemical and radiochemical purities with a specific activity ranged from 3–4 Ci/μmol (n = 6). The total synthesis time was 30 min from EOB. PET studies in anesthetized baboon show that [11C]1 penetrates BBB and accumulates in alpha2A-AR enriched brain areas. |
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