用于正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）的中枢体内烟碱型乙酰胆碱受体成像剂。

Central in vivo nicotinic acetylcholine receptor imaging agents for positron emission tomography (PET) and single photon emission computed tomography (SPECT).

作者信息

Ogawa Mikako, Tsukada Hideo, Hatano Kentaro, Ouchi Yasuomi, Saji Hideo, Magata Yasuhiro

机构信息

Photon Medical Research Center, Hamamatsu University School of Medicine, Japan.

出版信息

Biol Pharm Bull. 2009 Mar;32(3):337-40. doi: 10.1248/bpb.32.337.

DOI:10.1248/bpb.32.337

PMID:19252274

Abstract

Positron emission tomography (PET) and single photon emission computed tomography (SPECT) are useful for non-invasive investigation of brain receptors. With these imaging techniques, changes in brain receptor densities and distributions during chronic drug treatments and disease progressions can be tracked for a long period. Appropriate radiolabeled imaging agents are necessary for PET and SPECT molecular imaging. Nicotinic acetylcholine receptors (nAChRs) play important roles in brain functions. The alpha4beta2 and alpha7 are the major nAChR subtypes in the brain. To date, several subtype selective radiolabeled ligands for nAChR have been reported. For the alpha4beta2 subtype, some agents are already applied for human studies, but only a few agents are developed for the alpha7 subtype. Here, we overview our results of [(125/123)I]5-iodo-3-(2(S)-azetidinylmethoxy)pyridine and 5-[11C]methyl-3-(2-(S)-azetidinylmethoxy)pyridine ([11C]5MA) for alpha4beta2 subtype imaging, and 11C-2-methylamino-benzoic acid 1-aza-bicyclo[2.2.2]oct-3-yl ester (11C-MeQAA) for alpha7 subtype imaging.

摘要

正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）对于脑受体的无创研究很有用。通过这些成像技术，可以长期追踪慢性药物治疗和疾病进展过程中脑受体密度和分布的变化。PET和SPECT分子成像需要合适的放射性标记成像剂。烟碱型乙酰胆碱受体（nAChRs）在脑功能中起重要作用。α4β2和α7是脑中主要的nAChR亚型。迄今为止，已经报道了几种针对nAChR的亚型选择性放射性标记配体。对于α4β2亚型，一些试剂已应用于人体研究，但针对α7亚型开发的试剂很少。在此，我们概述了用于α4β2亚型成像的[(125/123)I]5-碘-3-(2(S)-氮杂环丁烷甲氧基)吡啶和5-[11C]甲基-3-(2-(S)-氮杂环丁烷甲氧基)吡啶([11C]5MA)，以及用于α7亚型成像的11C-2-甲氨基苯甲酸1-氮杂双环[2.2.2]辛-3-基酯(11C-MeQAA)的研究结果。