In silico study and biological evaluation of 99mTc-tricabonyl oxiracetam as a selective imaging probe for AMPA receptors

Abstract

The non-invasive quantification of AMPA receptors (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) could become a prognostic marker for brain disorders. 99mTc-tricarbonyl oxiracetam complex was prepared as a novel probe for AMPA receptor targeting with radiolabeling yield >98% and showed stability of 12 h. Molecular modeling and docking studies of 99mTc-tricarbonyl oxiracetam were performed. The results suggested that the complex act as very good positive allosteric modulators for AMPA receptor. The biodistribution studies revealed high brain uptake (7.5 ± 0.11% %ID/g) at 5 min post-I.V. injection that make 99mTc-tricarbonyl oxiracetam as a novel brain perfusion imaging radiotracer.