Tingyu Yang, Wei Zheng, Xuebo Cheng, Hualong Chen, Zeng Jiang, Ziyue Yu, Lu Zhang, Yi Xie, Lianjie Du, Xuan Ge, Jiahuai Zhang, Leilei Yuan, Yajing Liu, Zehui Wu
By modifying the structures of targeted A2A R antagonists and tracers, novel compounds 3 , 7a , 9 , 12c , and BIBD-399 were designed and synthesized. In vitro inhibition experiments demonstrated that 3 , 12c , and BIBD-399 have high affinity for A2A R. [ 18 F]3 and [18 F]BIBD-399 were successfully synthesized. In terms of biological distribution, the brain uptake of [18 F]MNI-444 exhibits greater than that of [ 18 F]3 and [18 F]BIBD-399. PET imaging shows that [ 18 F]3 is off-target in the brain, while [18 F]BIBD-399 and [18 F]MNI-444 can be specifically imaged in regions with high A2A R expression...
March 8, 2024: ACS Chemical Neuroscience