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

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

Department of Radiology, Washington University School of Medicine, 510 S. Kingshighway Boulevard, St. Louis, MO 63110, USA
Department of Neurology, Washington University School of Medicine, 660 S. Euclid Ave, St. Louis, MO 63110, USA
Author to whom correspondence should be addressed.
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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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 (CC BY 3.0).

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MDPI and ACS Style

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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