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

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• 作者：Ji-In Bang^a ; In Soon Jung^a ; Yoo Sung Song^a ; Hyun Soo Park^a ; ^b ; Byung Seok Moon^a ; Byung Chul Lee^a ; ^c ; Sang Eun Kim^a ; ^b ; ^c ; ^{kse@snu.ac.kr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Parkinson&rsquo ; s disease (PD) ; Dopamine transporter (DAT) ; (E)-N-(3-iodoprop-2-enyl)-2beta-carbofluoroethoxy-3beta-(4&prime ; -methyl-phenyl) nortropane ; Levodopa ; Positron emission tomography (PET)
• 刊名：Nuclear Medicine and Biology
• 出版年：2016
• 出版时间：February 2016
• 年：2016
• 卷：43
• 期：2
• 页码：158-164
• 全文大小：646 K

文摘

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

Methods

Dynamic PET/CT of [¹⁸F]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 BP_ND). Each of the four normal rats was pretreated with pramipexole, amantadine, and escitalopram 30 min before [¹⁸F]FE-PE2I injection. The effect of l-DOPA combined with benserazide was assessed in the normal and PD rats.

Results

The BP_ND 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 BP_ND did not differ from those of the controls. The pretreatment with l-DOPA/benserazide, however, significantly reduced the striatal BP_ND. The striatal BP_ND of the PD rats with l-DOPA/benserazide pretreatment was not different from that of the same PD rats with placebo treatment.

Conclusion

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