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Appl. Sci. 2014, 4(1), 66-78; doi:10.3390/app4010066
Article

Radiosynthesis and in Vivo Evaluation of Two PET Radioligands for Imaging α-Synuclein

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Received: 30 April 2013 / Revised: 7 February 2014 / Accepted: 27 February 2014 / Published: 17 March 2014
(This article belongs to the Special Issue Radioisotope Production and Applications)
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Abstract

Two 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).
Keywords: Lewy bodies; Parkinson’s disease; PET; phenothiazine; radiosynthesis; α-synuclein Lewy bodies; Parkinson’s disease; PET; phenothiazine; radiosynthesis; α-synuclein
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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