title: PET imaging of dopamine transporters with [(18)F]FE-PE2I: Effects of anti-Parkinsonian drugs.
abstract: OBJECTIVE
  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.
  
  
  CONCLUSIONS
  [(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.
authors.affiliation: Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul National University Bundang Hospital, 300 Gumi-dong, Bundang-gu, Seongnam 463-707, Republic of Korea.
authors.forename: Ji-In
authors.initials: JI
authors.lastname: Bang
authors.affiliation: Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul National University Bundang Hospital, 300 Gumi-dong, Bundang-gu, Seongnam 463-707, Republic of Korea.
authors.forename: In Soon
authors.initials: IS
authors.lastname: Jung
authors.affiliation: Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul National University Bundang Hospital, 300 Gumi-dong, Bundang-gu, Seongnam 463-707, Republic of Korea.
authors.forename: Yoo Sung
authors.initials: YS
authors.lastname: Song
authors.affiliation: Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul National University Bundang Hospital, 300 Gumi-dong, Bundang-gu, Seongnam 463-707, Republic of Korea; Department of Transdisciplinary Studies, Graduate School of Convergence Science and Technology, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
authors.forename: Hyun Soo
authors.initials: HS
authors.lastname: Park
authors.affiliation: Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul National University Bundang Hospital, 300 Gumi-dong, Bundang-gu, Seongnam 463-707, Republic of Korea.
authors.forename: Byung Seok
authors.initials: BS
authors.lastname: Moon
authors.affiliation: Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul National University Bundang Hospital, 300 Gumi-dong, Bundang-gu, Seongnam 463-707, Republic of Korea; Center for Nanomolecular Imaging and Innovative Drug Development, Advanced Institutes of Convergence Technology, 864-1, Iui-dong, Yeongtong-gu, Suwon 443-270, Republic of Korea.
authors.forename: Byung Chul
authors.initials: BC
authors.lastname: Lee
authors.affiliation: Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul National University Bundang Hospital, 300 Gumi-dong, Bundang-gu, Seongnam 463-707, Republic of Korea; Department of Transdisciplinary Studies, Graduate School of Convergence Science and Technology, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea; Center for Nanomolecular Imaging and Innovative Drug Development, Advanced Institutes of Convergence Technology, 864-1, Iui-dong, Yeongtong-gu, Suwon 443-270, Republic of Korea. Electronic address: kse@snu.ac.kr.
authors.forename: Sang Eun
authors.initials: SE
authors.lastname: Kim
mesh_terms: D000818:Animals; D001545:Benserazide / Q000494:pharmacology* / Q000627:therapeutic use; D001692:Biological Transport / Q000187:drug effects; D050483:Dopamine Plasma Membrane Transport Proteins / Q000378:metabolism*; D007980:Levodopa / Q000494:pharmacology* / Q000627:therapeutic use; D008297:Male; D017072:Neostriatum / Q000000981:diagnostic imaging / Q000187:drug effects* / Q000378:metabolism; D009662:Nortropanes / Q000378:metabolism*; D010300:Parkinson Disease / Q000000981:diagnostic imaging / Q000188:drug therapy / Q000378:metabolism*; D049268:Positron-Emission Tomography; D051381:Rats; D017207:Rats, Sprague-Dawley; D014057:Tomography, X-Ray Computed; D014446:Tyrosine 3-Monooxygenase / Q000378:metabolism
chemical_list: C543996:(E)-N-(3-iodoprop-2-enyl)-2beta-carbofluoroethoxy-3beta-(4'-methyl-phenyl) nortropane; D050483:Dopamine Plasma Membrane Transport Proteins; D009662:Nortropanes; D007980:Levodopa; D001545:Benserazide; D014446:Tyrosine 3-Monooxygenase
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)