Radiosynthesis and evaluation of a radiotracer for investigating Ca2+-permeable AMPA receptor (CP-AMPAR) for neurological disease

Conclusions: We have successfully synthesized compound TZ7911 by using the commercially available Fmoc-​3-​iodo-​L-​tyrosine involving seven steps. It is further screened for ex vivo electrophysiology assay in rodents and TZ7911 displayed as a very potent CP-AMPARs inhibitor. The radiosynthesis of [125I]TZ7911 was achieved successfully. Further evaluation of [125I]TZ7911 to investigate the CP-AMPAR regulate functions for the brain disorders is in the progress within our institution. Research Support: USA NIH/NINDS #NS103988, NS075527, and NS103957. References: 1. Neuron 2018, 99, 956-968. 2. J. Med. Chem. 2002, 45, 5745-5754. 3. J. Med. Chem. 1991, 34, 2389-2394. 4. Science 2015, 347, 659-664.

Source: Journal of Nuclear Medicine - May 14, 2020 Category: Nuclear Medicine Authors: Tangadanchu, V. K. R., Creed, M. C., Liang, Q., Gu, J., Luo, Z., Shoghi, K., Moron-Concepcion, J., Tu, Z. Tags: Preclinical Probes for Neuroimaging (Poster Session) Source Type: research