A large excess of 100X non-radiolabeled apelin ligand enabled a highly significant 65.2 ± 11.7% reduction of [ 68 Ga]Ga-AP747 binding to T84 cells compared to non-blocked conditions (cell-to-background [ 68 Ga]Ga-AP747 autoradiography signal ratios: 0.50 ± 0.23 and 1.40 ± 0.38, respectively, *** P = 0.0006, n = 6; Shapiro–Wilk normality tests: [ 68 Ga]Ga-AP747 group: P = 0.2110; [ 68 Ga]Ga-AP747 “blocking” group: P = 0.3476).
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Design and preclinical evaluation of a novel apelin-based PET radiotracer targeting APJ receptor for molecular imaging of angiogenesis.
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