2026-03-12T16:30:13Z https://repo.qst.go.jp/oai

oai:repo.qst.go.jp:00082773 2023-05-15T17:56:52Z 1

Imaging the trace amine-associated receptor 1 by positron emission tomography Sun, Jiyun Chen, Jiahui Katsushi, Kumata Xiao, Zhiwei Rong, Jiang Haider, Ahmed Shao, Tuo Lu, Wang Xu, Hao Zhang, Ming-Rong Liang, Huan Katsushi, Kumata Lu, Wang Zhang, Ming-Rong Liang, Huan metadata only access Trace amine-associated receptor 1 (TAAR1) has been implicated in drug addiction, schizophrenia, depression and Parkinson’s disease (PD). To date, there are no reports on TAAR1-targeted probes for non-invasive quantification of receptor density in vivo. Herein, we report the synthesis of a 11C-labeled TAAR1 high-affinity antagonist N-(3-methoxyphenyl)-6-(pyrrolidin-1-yl)-5-(trifluoromethyl)nicotinamide [11C]4 (also named [11C]TAAR1-1911), as well as its physicochemical and preclinical evaluations for positron emission tomography (PET) imaging. This PET ligand was afforded using [11C]CH3I with the base NaOH in good radiochemical yield (non-decay corrected 14% relative to starting [11C]CO2), excellent radiochemical purities (> 99%) and high molar activities (> 37 GBq/µmol). Despite promising in vitro performance characteristics, [11C]4 did not exhibit in vivo specificity, potentially owing to fast metabolic degradation. Further studies are warranted to identify a suitable TAAR1 PET tracer, which would ultimately aid the development of TAAR1-directed therapeutic agents. ELSEVIER 2021-03 eng journal article https://repo.qst.go.jp/records/82773 10.1016/j.tetlet.2021.153007 https://www.sciencedirect.com/science/article/abs/pii/S0040403921002033 0040-4039 Tetrahedron Letters 70 153007