Radiosynthesis and Radiotracer Properties of a 7-(2-[18F]Fluoroethoxy)-6-methoxypyrrolidinylquinazoline for Imaging of Phosphodiesterase 10A with PET 英文参考文献.docVIP

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Radiosynthesis and Radiotracer Properties of a 7-(2-[18F]Fluoroethoxy)-6-methoxypyrrolidinylquinazoline for Imaging of Phosphodiesterase 10A with PET 英文参考文献.doc

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Radiosynthesis and Radiotracer Properties of a 7-(2-[18F]Fluoroethoxy)-6-methoxypyrrolidinylquinazoline for Imaging of Phosphodiesterase 10A with PET 英文参考文献

Pharmaceuticals 2012, 5, 169-188; doi:10.3390/ph5020169 OPEN ACCESS Pharmaceuticals ISSN 1424-8247 /journal/pharmaceuticals Article Radiosynthesis and Radiotracer Properties of a 7-(2-[18F]Fluoroethoxy)-6-methoxypyrrolidinylquinazoline for Imaging of Phosphodiesterase 10A with PET Uta Funke 1,*, Winnie Deuther-Conrad 1, Gregor Schwan 2, Aurélie Maisonial 1, Matthias Scheunemann 1, Steffen Fischer 1, Achim Hiller 1, Detlef Briel 2 and Peter Brust 1 1 Institute of Radiopharmacy, Research Site Leipzig, Helmholtz-Zentrum Dresden-Rossendorf, Permoserstra?e 15, Leipzig 04318, Germany; E-Mails: w.deuther-conrad@hzdr.de (W.D.-C.); aurelie.maisonial@inserm.fr (A.M.); m.scheunemann@hzdr.de (M.S.); s.fischer@hzdr.de (S.F.); a.hiller@hzdr.de (A.H.); p.brust@hzdr.de (P.B.) 2 Institute of Pharmacy, Universit?t Leipzig, Brüderstra?e 34, Leipzig 04103, Germany; E-Mails: gschwan@uni-leipzig.de (G.S.); briel@rz.uni-leipzig.de (D.B.) * Author to whom correspondence should be addressed; E-Mail: u.funke@hzdr.de; Tel.: +49-341-235-3695; Fax: +49-341-235-2731. Received: 24 November 2011; in revised form: 18 January 2012 / Accepted: 19 January 2012 / Published: 6 February 2012 Abstract: Phosphodiesterase 10A (PDE10A) is a key enzyme of intracellular signal transduction which is involved in the regulation of neurotransmission. The molecular imaging of PDE10A by PET is expected to allow a better understanding of physiological and pathological processes related to PDE10A expression and function in the brain. The aim of this study was to develop a new 18F-labeled PDE10A ligand based on a 6,7-dimethoxy- 4-pyrrolidinylquinazoline and to evaluate its properties in biodistribution studies. Nucleophilic substitution of the 7-tosyloxy-analogue led to the 7-[18F]fluoroethoxy-derivative [18F]IV with radiochemical yields of 25% ± 9% (n = 9), high radiochemical purity of ≥99% and specific activities of 110–1,100 GBq/μmol. [18F]IV showed moderate