Development of PET agent for cardiac parasympathetic nervous system
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摘要: 心脏副交感神经正电子显像剂的研发在评估心血管疾病中起着不可估量的作用，正电子发射断层显像能够高灵敏地反映心脏副交感神经的变化。本文旨在介绍烟碱类、毒蕈碱类和乙酰胆碱酯酶类三种心脏副交感神经显像剂的研究新进展。2-18F-氟-3-(2(S)-甲氧基氮杂环丁烷基)吡啶(2-18F-F-A-85380)、(R, S)-N-11C-甲基-二苯乙醇酸-3-奎宁环酯(11C-MQNB)和4-18F-氟苄基-右苄替米特(4-18F-FDEX)为烟碱类和毒蕈碱类副交感神经显像剂，11C-多奈哌齐(11C-DNP)和N-[11C]甲基-3[[(二甲氨基)羰基]氧基]-2-(2', 2'-二苯基丙氧基甲基)吡啶(11C-MDDP)为乙酰胆碱酯酶类副交感神经显像剂。其中11C-MQNB、2-18F-F-A-85380研究较为深入，而11C-DNP、11C-MDDP、4-18F-FDEX是具有良好临床应用潜质的显像剂。
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关键词:
- 放射性示踪剂 /
- 正电子发射断层显像术 /
- 心脏副交感神经系统
Abstract: The development of cardiac parasympathetic positron imaging agents plays an immeasurable role in the evaluation of cardiovascular disease, and positron- emission tomography can reflect changes in the parasympathetic nerves of the heart with high sensitivity. 2-[18F]fluoro-3-[2(S)-2-azetidinyl-methoxy]pyridine (2-18F-F-A-85380), (R, S)-N-[11C]-Methyl-quinuclidin-3-yl benzilate (11C-MQNB) and 4-18F- fluorobenzyl-dexetimide (4-18F-FDEX) are nicotinoid and muscarinic parasympathetic imaging agents, 11C-donepezil (11C-DNP) and N-[11C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2', 2'-diphenylpropio-noxymethyl) pyridinium (11C-MDDP) are acetylcholinesterase parasympathetic imaging agents. Among them, 11C-MQNB and 2-18F- F-A-85380 are more intensively studied, while 11C-DNP, 11C-MDDP and 4-18F-FDEX are imaging agents with good potential for clinical application. -
图 1 心脏副交感神经正电子显像剂及其作用靶点
CAT: 胆碱乙酰转移酶; VAChT: 囊泡乙酰胆碱转运蛋白; CHT: 钠依赖性载体; Ach: 乙酰胆碱; AchE: 乙酰胆碱酯酶; MR: 毒蕈碱受体; NR: 烟碱受体.
Figure 1. Cardiac parasympathetic positron imaging agents and their targets.
图 3 N-11C-甲基-3[[(二甲氨基)羰基]氧基]-2-(2', 2'-二苯基丙氧基甲基)吡啶
Figure 3. N-11C-methyl-3-[[(dimethylamino)carbonyl] oxy]-2-(2', 2'-diphenylpropi-onoxymethyl) pyridinium.
图 4 2-18F-氟-3-[2(S)-甲氧基氮杂环丁烷基]吡啶
Figure 4. 2-18F-fluoro-3-[2(S)-2-azetidinyl-methoxy] pyridine.
图 5 (R，S)-N-11C-甲基-二苯乙醇酸-3-奎宁环酯
Figure 5. (R, S)-N-11C-Methyl-quinuclidin-3-yl benzilate.
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