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Automated radiosynthesis of [ 18 F]SPA‐RQ for imaging human brain NK 1 receptors with PET
Author(s) -
Chin Frederick T.,
Morse Cheryl L.,
Shetty H. Umesha,
Pike Victor W.
Publication year - 2006
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1016
Subject(s) - radiosynthesis , chemistry , radiochemistry , radioligand , positron emission tomography , pet imaging , nuclear chemistry , yield (engineering) , nuclear medicine , receptor , physics , biochemistry , medicine , thermodynamics
[ 18 F]SPA‐RQ is an effective radioligand for imaging brain neurokinin type‐1 (NK 1 ) receptors in clinical research and drug discovery with positron emission tomography. For the automated regular production of [ 18 F]SPA‐RQ for clinical use in the USA under an IND we chose to use a modified commercial synthesis module (TRACERlab FX F‐N ; GE Medical Systems) with an auxiliary custom‐made robotic cooling–heating reactor, after evaluating several alternative radiosynthesis conditions. The automated radiosynthesis and its quality control are described here. [ 18 F]SPA‐RQ was regularly obtained within 150 min from the start of radiosynthesis in high radiochemical purity (>99%) and chemical purity and with an overall decay‐corrected radiochemical yield of 15±2% (mean±S.D.; n =10) from cyclotron‐produced [ 18 F]fluoride ion. The specific radioactivity of [ 18 F]SPA‐RQ at the end of synthesis ranged from 644 to 2140 mCi/µmol (23.8–79.2 GBq/µmol). Copyright © 2005 John Wiley & Sons, Ltd.