Figure 6.
Design of GlyT1 Ligands. Structures of glycine 1 (co-agonist of the NMDA receptor), sarcosine 2 (a weak GlyT1 inhibitor) and NFPS 3 (ALX-5047), the prototypical sarcosine-derived GlyT1 inhibitor, competitive, non-sarcosine-derived GlyT1 inhibitor lead 4, optimized GlyT1 inhibitor 5 (ACPPB), and the radiolabelded congener [35S]ACPPB, 6. See text for details.