Browsing by Subject "[11C]GSK1482160"

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    Development, validation and implementation of radio-HPLC methods for the P2X7-receptor-targeted [11C]GSK1482160 radiopharmaceutical
    (Elsevier, 2018-12) Wissman, Carmen L.; Wang, Min; Gao, Mingzhang; Zheng, Qi-Huang; Green, Mark A.; Radiology and Imaging Sciences, School of Medicine
    A radio-analytical RP-HPLC method was developed and validated to support production of the P2X7-receptor-targeted [11C]GSK1482160 radiopharmaceutical. Method validation included characterization of retention times, peak shapes, linearity, accuracy, precision, selectivity, limits of detection and quantitation (UV signal), radiochemical stability, as well as analytical method range and robustness. The validated radio-HPLC method is suitable for the definition of [11C]GSK1482160 radiochemical identity, radiochemical purity, as well as molar activity, and is being employed in support of human studies with [11C]GSK1482160.
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    Synthesis of [11C]GSK1482160 as a new PET agent for targeting P2X7 receptor
    (Elsevier, 2015-05) Gao, Mingzhang; Wang, Min; Green, Mark A.; Hutchins, Gary D.; Zheng, Qi-Huang; Department of Radiology and Imaging Sciences, School of Medicine
    The authentic standards GSK1482160 and its isomer, as well as the radiolabeling precursors desmethyl-GSK1482160 and Boc-protected desmethyl-GSK1482160 were synthesized from l-pyroglutamic acid, methyl l-pyroglutamate and 2-chloro-3-(trifluoromethyl)benzylamine with overall chemical yield 27–28% in 3 steps, 58% in 4 steps, 76% in 1 step and 33% in 2 steps, respectively. [11C]GSK1482160 was prepared from either desmethyl-GSK1482160 or Boc-protected desmethyl-GSK1482160 with [11C]CH3OTf through N-[11C]methylation and isolated by HPLC combined with SPE in 40–50% and 30–40% radiochemical yield, respectively, based on [11C]CO2 and decay corrected to end of bombardment (EOB). The radiochemical purity was >99%, and the specific activity at EOB was 370–1110 GBq/μmol with a total synthesis time of ∼40-min from EOB.