The first synthesis of [11C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3)
✍ Scribed by Min Wang; Mingzhang Gao; Kathy D. Miller; George W. Sledge; Gary D. Hutchins; Qi-Huang Zheng
- Publisher
- Elsevier Science
- Year
- 2011
- Tongue
- English
- Weight
- 464 KB
- Volume
- 21
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
synthase kinase-3 (GSK-3) Radiosynthesis Positron emission tomography (PET) Cancer Alzheimer's disease a b s t r a c t SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC 50 value of 34 nM.
, a new potential PET agent for imaging of GSK-3, was first designed and synthesized in 20-30% decay corrected radiochemical yield and 370-555 GBq/lmol specific activity at end of bombardment (EOB). The synthetic strategy was to prepare a carbon-11-labeled maleic anhydride intermediate followed by the conversion to maleimide.