[11C]MPTQ 的合成与体内评价：一种潜在的用于检测 α2A-肾上腺素能受体的 PET 示踪剂。
Synthesis and in vivo evaluation of [11C]MPTQ: a potential PET tracer for alpha2A-adrenergic receptors.
机构信息
Division of Molecular Imaging and Neuropathology, Department of Psychiatry, Columbia University, New York, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3654-7. doi: 10.1016/j.bmcl.2010.04.099. Epub 2010 May 22.
Radiosynthesis and in vivo evaluation of [N-methyl-(11)C] 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 [(11)C]CH(3)I in presence of aqueous potassium hydroxide in DMSO afforded [(11)C]1 in 25% yield (EOS) with >99% chemical and radiochemical purities with a specific activity ranged from 3-4 Ci/micromol (n=6). The total synthesis time was 30 min from EOB. PET studies in anesthetized baboon show that [(11)C]1 penetrates BBB and accumulates in alpha2A-AR enriched brain areas.
[N-甲基-（11）C]5-甲基-3-[4-（3-苯丙基）-哌嗪-1-基甲基]-3,3a,4,5-四氢异恶唑[4,3-c]喹啉（1）的放射性合成及其作为潜在的α2-肾上腺素能受体 PET 示踪剂的体内评价。非放射性标准品 1 和相应的脱甲基前体 2 分别可从 2-氨基苯甲醛以 40%和 65%的产率合成。在 DMSO 中的水合氢氧化钾存在下，用[（11）C]CH3I 进行甲基化，可得到 25%的[（11）C]1（EOS），化学和放射化学纯度均大于 99%，比活度范围为 3-4 Ci/μmol（n=6）。从 EOB 开始，总合成时间为 30 分钟。在麻醉狒狒中进行的 PET 研究表明，[（11）C]1 穿透 BBB 并在富含α2A-AR 的脑区积聚。
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