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Automated radiosynthesis of [18F]SPA-RQ for imaging human brain NK1 receptors with PET

✍ Scribed by Frederick T. Chin; Cheryl L. Morse; H. Umesha Shetty; Victor W. Pike


Publisher
John Wiley and Sons
Year
2006
Tongue
French
Weight
316 KB
Volume
49
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

[^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.


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