Synthesis and Biodistribution of Flumazenil Derivative F-18(3-(2-Fluoro) flumazenil for Imaging Benzodiazepine Receptor / 대한핵의학회잡지
Korean Journal of Nuclear Medicine
;
: 527-536, 1999.
Article
in Korean
| WPRIM
| ID: wpr-40162
ABSTRACT
PURPOSE:
Radiotracers that bind to the central benzodiazepine receptor are useful for the investigation of various neurological and psychiatric diseases. [C-11]Flumazenil, a benzodiazepine antagonist, is the most widely used radioligand for central benzodiazepine receptor imaging by PET. We synthesized 3-(2-[F- 18]fluoro)flumazenil, a new fluorine-18 (t1/2=110 min) labeled analogue of benzodiazepine receptor imaging agent, and evaluated in vivo for biodistribution in mice. MATERIALS ANDMETHODS:
Flumazenil (Ro 15-1788) was synthesized by a modification of the reported method. Precursor of 3-(2-[F-18]fluoro)flumazenil, the tosylated flumazenil derivative was prepared by the tosylation of the ethyl ester by ditosylethane. [F-18] labeling of tosyl substitued flumazenil precursor was performed by adding F-18 ion at 85 degree C in the hot cell for 20 min. The reaction mixture was trapped by C18 cartridge, washed with 10% ethanol, and eluted by 40% ethanol. Bidistribution in mice was determined after intravenous injection.RESULTS:
The total chemical yield of tosylated flumazenil derivative was ~40%. The efficiency of labeling 3-(2-[F-18]fluoro)flumazenil was 66% with a total synthesis time of 50 min. Brain uptakes of 3-(2-[F-18]fluoro)flumazenil at 10, 30, 60 min after injection, were 2.5+/-0.37, 2.2+/-0.26, 2.1+/-0.11 and blood activities were 3.7+/-0.43, 3.3+/-0.07, 3.3+/-0.09%ID/g, respectively.CONCLUSION:
We synthesized a tosylated flumazenil derivative which was successfully labeled with no-carrier-added F-18 by nucleophilic substitution.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Benzodiazepines
/
Brain
/
Flumazenil
/
Receptors, GABA-A
/
Ethanol
/
Injections, Intravenous
Limits:
Animals
Language:
Korean
Journal:
Korean Journal of Nuclear Medicine
Year:
1999
Type:
Article
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