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Radiosynthesis and in Vivo Evaluation of Two PET Radioligands for Imaging α-Synuclein
AbstractTwo α-synuclein ligands, 3-methoxy-7-nitro-10H-phenothiazine (2a, Ki = 32.1 ± 1.3 nM) and 3-(2-fluoroethoxy)-7-nitro-10H-phenothiazine (2b, Ki = 49.0 ± 4.9 nM), were radiolabeled as potential PET imaging agents by respectively introducing 11C and 18F. The syntheses of [11C]2a and [18F]2b were accomplished in a good yield with high specific activity. Ex vivo biodistribution studies in rats revealed that both [11C]2a and [18F]2b crossed the blood-brain barrier (BBB) and demonstrated good brain uptake 5 min post-injection. MicroPET imaging of [11C]2a in a non-human primate (NHP) confirmed that the tracer was able to cross the BBB with rapid washout kinetics from brain regions of a healthy macaque. The initial studies suggested that further structural optimization of [11C]2a and [18F]2b is necessary in order to identify a highly specific positron emission tomography (PET) radioligand for in vivo imaging of α-synuclein aggregation in the central nervous system (CNS).
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Zhang, X.; Jin, H.; Padakanti, P.K.; Li, J.; Yang, H.; Fan, J.; Mach, R.H.; Kotzbauer, P.; Tu, Z. Radiosynthesis and in Vivo Evaluation of Two PET Radioligands for Imaging α-Synuclein. Appl. Sci. 2014, 4, 66-78.View more citation formats
Zhang X, Jin H, Padakanti PK, Li J, Yang H, Fan J, Mach RH, Kotzbauer P, Tu Z. Radiosynthesis and in Vivo Evaluation of Two PET Radioligands for Imaging α-Synuclein. Applied Sciences. 2014; 4(1):66-78.Chicago/Turabian Style
Zhang, Xiang; Jin, Hongjun; Padakanti, Prashanth K.; Li, Junfeng; Yang, Hao; Fan, Jinda; Mach, Robert H.; Kotzbauer, Paul; Tu, Zhude. 2014. "Radiosynthesis and in Vivo Evaluation of Two PET Radioligands for Imaging α-Synuclein." Appl. Sci. 4, no. 1: 66-78.