AZD4282

AZD4282 is a small molecule inhibitor of the glycine transporter 1 (GlyT1), originally developed by AstraZeneca for the treatment of neuropathic pain. GlyT1 is a membrane-bound protein responsible for the reuptake of glycine from the synaptic cleft, thereby regulating glycine concentrations at N-methyl-D-aspartate (NMDA) receptors. By inhibiting GlyT1, AZD4282 increases extracellular glycine levels, which enhances NMDA receptor-mediated neurotransmission. While GlyT1 inhibitors have been extensively studied for their potential to treat the negative and cognitive symptoms of schizophrenia, AZD4282 was specifically investigated in Phase II clinical trials for its analgesic efficacy in patients with posttraumatic neuralgia. Despite reaching Phase II development, the program was ultimately discontinued by AstraZeneca.