Design, synthesis and evaluation of (18)F-labeled bradykinin B1 receptor-targeting small molecules for PET imaging
作者： Zhengxing Zhang , Hsiou-Ting Kuo , Joseph Lau , Silvia Jenni , Chengcheng Zhang
DOI: 10.1016/J.BMCL.2016.06.066
关键词:
摘要: Two fluorine-18 ((18)F) labeled bradykinin B1 receptor (B1R)-targeting small molecules, (18)F-Z02035 and (18)F-Z02165, were synthesized evaluated for imaging with positron emission tomography (PET). Z02035 Z02165 derived from potent antagonists, showed high binding affinity (0.93±0.44 2.80±0.50nM, respectively) to B1R. (18)F-Z02165 prepared by coupling 2-[(18)F]fluoroethyl tosylate their respective precursors, obtained in 10±5 (n=4) 22±14% (n=3), respectively, decay-corrected radiochemical yield >99% purity. exhibited moderate lipophilicity (LogD7.4=1.10 0.59, respectively), stable mouse plasma. PET biodistribution studies mice that both tracers enabled visualization of the B1R-positive HEK293T::hB1R tumor xenografts better contrast than control B1R-negative HEK293T tumors. Our data indicate molecule antagonists can be used as pharmacophores design B1R-targeting tracers.
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