Radiosynthesis and in vivo evaluation of two PET radioligands for imaging α-synuclein

Xiang Zhang, Hongjun Jin, Prashanth K. Padakanti, Junfeng Li, Hao Yang, Jinda Fan, Robert H. Mach, Paul Kotzbauer, Zhude Tu

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49 Scopus citations


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).

Original languageEnglish
Pages (from-to)66-78
Number of pages13
JournalApplied Sciences (Switzerland)
Issue number1
StatePublished - Mar 1 2014


  • Lewy bodies
  • PET
  • Parkinson's disease
  • Phenothiazine
  • Radiosynthesis
  • α-synuclein


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