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Synthesis of fluorine-18-labeled ciprofloxacin for PET studies in humans.

Abstract：

:Ciprofloxacin (1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid), a widely-prescribed antibiotic, was labeled with fluorine-18 with the aim to perform positron emission tomography studies in humans for pharmacokinetic measurements. Due to a lack of chemical activation of ciprofloxacin for a direct nucleophilic exchange reaction a novel two-step synthetic approach, which employed an activated 6-fluoro-7-chloro substituted precursor molecule, was developed. The radiosynthesis yielded, starting from 52.5 +/- 11.3 GBq of [(18)F]fluoride, 1.3 +/- 0.6 GBq (n = 13) [(18)F]ciprofloxacin ready for intravenous administration in about 130 min synthesis time. A series of analytical tests was performed in order to prove the identity of the radiolabeled compound and its suitability for human applications.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Langer O,Mitterhauser M,Brunner M,Zeitlinger M,Wadsak W,Mayer BX,Kletter K,Müller M

doi

10.1016/s0969-8051(02)00444-4

keywords:

subject

Has Abstract

pub_date

2003-04-01 00:00:00

pages

285-91

issue

3

eissn

0969-8051

issn

1872-9614

pii

S0969805102004444

journal_volume

30

pub_type

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