Next Article in Journal
Undersampling in Orthogonal Frequency Division Multiplexing Telecommunication Systems
Next Article in Special Issue
CERN-MEDICIS (Medical Isotopes Collected from ISOLDE): A New Facility
Previous Article in Journal
Diffraction Focal Position and Vector Diffraction Theory for Micro Holographic Storage Systems
Previous Article in Special Issue
Dry Distillation of Radioiodine from TeO2 Targets
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

1
, 1
, 1
, 1
, 1
, 1
, 1
, 2
 and 1,*
Received: 30 April 2013; in revised form: 7 February 2014 / Accepted: 27 February 2014 / Published: 17 March 2014
(This article belongs to the Special Issue Radioisotope Production and Applications)
View Full-Text   |   Download PDF [535 KB, uploaded 17 March 2014]   |   Browse Figures
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.

Export to BibTeX |
EndNote


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.

AMA Style

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.


Appl. Sci. EISSN 2076-3417 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert