2026-03-12T16:28:35Z 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 1027054 Chen, Jiahui 1027055 Katsushi, Kumata 1027056 Xiao, Zhiwei 1027057 Rong, Jiang 1027058 Haider, Ahmed 1027059 Shao, Tuo 1027060 Lu, Wang 1027061 Xu, Hao 1027062 Zhang, Ming-Rong 1027063 Liang, Huan 1027064 Katsushi, Kumata 1027065 Lu, Wang 1027066 Zhang, Ming-Rong 1027067 Liang, Huan 1027068 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. journal article ELSEVIER 2021-03 Tetrahedron Letters 70 153007 0040-4039 https://repo.qst.go.jp/records/82773 eng 10.1016/j.tetlet.2021.153007 https://www.sciencedirect.com/science/article/abs/pii/S0040403921002033 metadata only access