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Synthesis of [18F]3-[1-(3-fluoropropyl)-(S)-pyrrolidin-2-ylmethoxy]pyridine ([18F]NicFP): a potential α4β2 nicotinic acetylcholine receptor radioligand for PET

✍ Scribed by Filip Dumont; Abida Sultana; Andrew Balter; Rikki N. Waterhouse

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
102 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Nicotinic acetylcholine receptors are widely distributed throughout the human brain and are believed to play a role in several neurological and psychiatric disorders. In order to identify an effective PET radioligand for in vivo assessment of the a4b2 subtype of nicotinic receptor, we synthesized [ 18 F]3-[1-(3-fluoropropyl)-(S)-pyrrolidin-2-ylmethoxy]pyridine (NicFP). The in vitro K D of NicFP was determined to be 1.1 nM, and the log P value obtained by HPLC analysis of the unlabelled standard was found to be 2.2. The radiosynthesis of [ 18 F]NicFP was carried out by a nucleophilic substitution reaction of anhydrous [ 18 F]fluoride and the corresponding mesylate precursor. After purification by HPLC, the radiochemical yield was determined to be 11.3 AE 2.1% and the specific activity was 0.47 AE 0.18 Ci/mmol (EOS, n = 3). The time of synthesis and purification was 99 AE 2 min. The final product was prepared as a sterile saline solution suitable for in vivo use.

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