Synthesis and Resolution of ATPO, a Potent and Selective Ampa Receptor Antagonist

Abstract

The excitatory amino acid (EAA) receptors mediate one of the major signaling systems in the central nervous system, and they are thought to be implicated in some neurodege-nerative disorders, e.g. Alzheimer's disease and stroke. It is of key importance to design selective ligands for every group of EAA receptors. The AMPA receptors are one such group of EAA receptors. (RS)-ATPO is a potent antagonist at the AMPA receptors, but it has hitherto been pharmacologically characterized only as the racemate.[1, 2]