Synthesis and ex vivo evaluation of carbon-11 labelled N-(4-methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea ([11C]AR-A014418): A radiolabelled glycogen synthase kinase-3β specific inhibitor for PET studies
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Acknowledgments
The Faculty of Medicine at the University of Toronto is acknowledged for financial support for this work from the Dean’s Fund (N.V.). The authors thank Doug Hussey, Patrick McCormick, and Hermia Cheung for their expertise with the ex vivo evaluations.
References and notes (28)
- et al.
Prog. Neurobiol.
(2001) - et al.
Trends Pharmacol. Sci.
(2004) - et al.
J. Biol. Chem.
(2003) - et al.
Nucl. Med. Biol.
(2000) - et al.
Nucl. Med. Biol.
(1996) - et al.
J. Chem. Neuroanat.
(1999) - et al.
Life Sci.
(2001) - et al.
Mol. Imaging Biol.
(2003) - et al.
Appl. Radiat. Isot.
(2001) Mol. Imaging Biol.
(2003)
EMBO J.
J. Clin. Psychiatry
Nat. Rev. Drug Disc.
Med. Res. Rev.
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