GlyT-1 inhibitor-1

GlyT-1 inhibitor-1 is a potent and selective small molecule inhibitor of the glycine transporter-1 (GlyT1), with a reported IC50 of 38 nM for the rat GlyT1 transporter. Developed by researchers at Vanda Pharmaceuticals and described in a 2018 study, the compound is designed to increase extracellular glycine concentrations in the brain. Glycine acts as an obligatory co-agonist at the N-methyl-D-aspartate (NMDA) receptor; by preventing its reuptake through GlyT1 inhibition, the compound enhances NMDA receptor-mediated neurotransmission. This mechanism is hypothesized to address the NMDA receptor hypofunction associated with the pathophysiology of schizophrenia. Preclinical evaluations have demonstrated that GlyT-1 inhibitor-1 possesses both antipsychotic activity and memory-enhancing properties, suggesting potential utility in treating schizophrenia and cognitive impairment. It is currently utilized as a research tool and has not been approved for clinical use.

Other names

CAS 1820934-93-7CAS1820934-93-7CAS-1820934-93-7Compound 1Compound1Compound-1