PET imaging of dopamine transporters with [(18)F]FE-PE2I: Effects of anti-Parkinsonian drugs

Abstract

Purpose: This study aimed to assess the striatal [(18)F]FE-PE2I binding and the immunohistochemical stain of tyrosine hydroxylase (TH) in the striatum, and to evaluate the effects of therapeutic drugs on [(18)F]FE-PE2I binding.

Methods: Dynamic PET/CT of [(18)F]FE-PE2I was performed in Parkinson's disease (PD) rat models, induced by the unilateral injection of 6-OHDA into the striatum. A simplified reference tissue model method was used to calculate the striatal binding potential (striatal BPND). Each of the four normal rats was pretreated with pramipexole, amantadine, and escitalopram 30 min before [(18)F]FE-PE2I injection. The effect of L-DOPA combined with benserazide was assessed in the normal and PD rats.

Results: The BPND was significantly lower in the lesioned striatum than in the striatum of the normal rats. After the pretreatment with pramipexole, amantadine, and escitalopram, the values of the striatal BPND did not differ from those of the controls. The pretreatment with L-DOPA/benserazide, however, significantly reduced the striatal BPND. The striatal BPND of the PD rats with L-DOPA/benserazide pretreatment was not different from that of the same PD rats with placebo treatment.

Conclusion: [(18)F]FE-PE2I may be used as a radioligand for the in-vivo imaging of the DAT. In the normal rats, [(18)F]FE-PE2I binding is unaffected by pramipexole, amantadine, and escitalopram. L-DOPA/benserazide does not affect the striatal [(18)F]FE-PE2I binding in PD rats.

Keywords: (E)-N-(3-iodoprop-2-enyl)-2beta-carbofluoroethoxy-3beta-(4′-methyl-phenyl) nortropane; Dopamine transporter (DAT); Levodopa; Parkinson’s disease (PD); Positron emission tomography (PET).