Ex vivo evaluation of N-(3-[18F]fluoropropyl)-2 beta-carbomethoxy-3 beta-(4-fluorophenyl)nortropane in rats

Teija Koivula, Päivi Marjamäki, Merja Haaparanta, Veronica Fagerholm, Tove Grönroos, Tiina Lipponen, Outi Perhola, Jouko Vepsäläinen, Olof Solin

Research output: Contribution to journalArticleScientificpeer-review

10 Citations (Scopus)


INTRODUCTION: The dopamine transporter (DAT) ligand N-(3-fluoropropyl)-2 beta-carbomethoxy-3beta-(4-fluorophenyl)nortropane (beta-CFT-FP) was labeled with fluorine-18, and its biodistribution was evaluated in rats ex vivo.

METHODS: The distribution of 18F radioactivity in the brain and peripheral organs and tissues was determined at several time points 5-120 min after intravenous injection of [18F]beta-CFT-FP.

RESULTS: The highest brain uptake of [18F]beta-CFT-FP was localized in the striatum; limbic structures also exhibited high uptake. Low uptake was found in the cerebellum. The highest ratio of striatum-to-cerebellum uptake, already reached within 5 min, was 3.1. Pretreatment with the selective DAT inhibitor GBR12909 significantly decreased [18F]beta-CFT-FP uptake in the striatum. In most peripheral tissues, the highest uptake was found at 5 min, indicating fast washout of the radioligand. Some accumulation of (18)F radioactivity was seen in bone as a function of time, reflecting defluorination of the radioligand.

CONCLUSION: The results indicate that [18F]beta-CFT-FP is a potential radioligand for studying DAT in vivo with positron emission tomography.

Original languageEnglish
Pages (from-to)177-83
Number of pages7
JournalNuclear Medicine and Biology
Issue number2
Publication statusPublished - Feb 2008
MoE publication typeA1 Journal article-refereed


  • Animals
  • Binding, Competitive
  • Bone and Bones/diagnostic imaging
  • Cerebellum/diagnostic imaging
  • Cocaine/analogs & derivatives
  • Corpus Striatum/diagnostic imaging
  • Dopamine Plasma Membrane Transport Proteins/antagonists & inhibitors
  • Dopamine Uptake Inhibitors/pharmacology
  • Fluorine Radioisotopes/pharmacokinetics
  • Limbic System/diagnostic imaging
  • Male
  • Nortropanes/pharmacokinetics
  • Piperazines/pharmacology
  • Radioligand Assay/methods
  • Radionuclide Imaging
  • Radiopharmaceuticals/pharmacokinetics
  • Rats
  • Rats, Sprague-Dawley
  • Tissue Distribution


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