Radiosynthesis and in vivo evaluation of [11 C] MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain

Z Tu, J Fan, S Li, LA Jones, J Cui, PK Padakanti…

文献索引：Tu, Zhude; Fan, Jinda; Li, Shihong; Jones, Lynne A.; Cui, Jinquan; Padakanti, Prashanth K.; Xu, Jinbin; Zeng, Dexing; Shoghi, Kooresh I.; Perlmutter, Joel S.; MacH, Robert H. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 5 p. 1666 - 1673

全文：HTML全文

被引用次数: 43

摘要

2-((4-(1-[11C] Methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl) phenoxy) methyl)-quinoline (MP-10), a specific PDE10A inhibitor (IC50= 0.18 nM with 100-fold selectivity over other PDEs), was radiosynthesized by alkylation of the desmethyl precursor with [11C] CH3I,∼ 45% yield,> 92% radiochemical purity,> 370GBq/μmol specific activity at end of bombardment (EOB). Evaluation in Sprague–Dawley rats revealed that [11C] MP-10 had highest brain ...