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

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

doi:10.1002/jlcr.1776

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 journal › Article › peer-review

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 language	English
Pages (from-to)	412-414
Number of pages	3
Journal	Journal of Labelled Compounds and Radiopharmaceuticals
Volume	53
Issue number	5-6
DOIs	https://doi.org/10.1002/jlcr.1776
Publication status	Published - May 1 2010
Externally published	Yes

Keywords

[F]FMZ
Flumazenil
GABA receptor antagonist

ASJC Scopus subject areas

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

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10.1002/jlcr.1776

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title = "The autosynthetic and solid extraction method developed on [F-18]flumazenil radiosynthesis",

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.",

keywords = "[F]FMZ, Flumazenil, GABA receptor antagonist",

author = "Chen, {Jenn Tzong} and Chang, {Kang Wei} and Tu, {Yean Hung} and Lin, {Wuu Jyh}",

year = "2010",

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doi = "10.1002/jlcr.1776",

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T1 - The autosynthetic and solid extraction method developed on [F-18]flumazenil radiosynthesis

AU - Chen, Jenn Tzong

AU - Chang, Kang Wei

AU - Tu, Yean Hung

AU - Lin, Wuu Jyh

PY - 2010/5/1

Y1 - 2010/5/1

N2 - 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.

AB - 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.

KW - [F]FMZ

KW - Flumazenil

KW - GABA receptor antagonist

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IS - 5-6

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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