The autosynthetic and solid extraction method developed on [F-18]flumazenil radiosynthesis

Jenn Tzong Chen, Kang Wei Chang, Yean Hung Tu, Wuu Jyh Lin

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

This study represents the newly developed autosynthetic and purification method for radiofluorinated flumazenil [18F]FMZ as the brain GABA/BZR receptor antagonist imaging agent. It represents a fast and convenient way to produce [18F]FMZ and is much easier to meet GMP compliance than preparative HPLC process. The process takes 45 minutes, decay corrected yield is 20-30%, and the radiochemical purity of the product is higher than 95%. The lipophilicity is a little higher partition coefficient with 1.49±0.12 which represents the high capability of penetrating the blood-brain barrier (BBB). An ex vivo study of this product bound to brain whole-hemisphere sections demonstrated complete inhibition of a BZR agonist which proved the capability of the newly developed solid extraction purification method can be applied in non-carrier added 18F-flumazenil preparation for further animal and clinical studies.

Original languageEnglish
Pages (from-to)412-414
Number of pages3
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume53
Issue number5-6
DOIs
Publication statusPublished - May 1 2010
Externally publishedYes

Fingerprint

Flumazenil
Purification
Brain
GABA Antagonists
Blood-Brain Barrier
Compliance
Animals
High Pressure Liquid Chromatography
Imaging techniques
Clinical Studies

Keywords

  • [F]FMZ
  • Flumazenil
  • GABA receptor antagonist

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

Cite this

The autosynthetic and solid extraction method developed on [F-18]flumazenil radiosynthesis. / Chen, Jenn Tzong; Chang, Kang Wei; Tu, Yean Hung; Lin, Wuu Jyh.

In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 53, No. 5-6, 01.05.2010, p. 412-414.

Research output: Contribution to journalArticle

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