Catalog No.: PC-24091Not For Human Use, Lab Use Only.
SSR504734 is a potent, selective and reversible inhibitor of glycine transporter-1 (GlyT1) with 8, 15, and 38 nM for human, rat, and mouse GlyT1 respectively.
SSR504734 is a potent, selective and reversible inhibitor of glycine transporter-1 (GlyT1) with 8, 15, and 38 nM for human, rat, and mouse GlyT1 respectively. SSR504734 has no effect (IC50>1 μM) on human GlyT2 and D-serine transporters, and on murine proline, glutamate, and GABA transporters. SSR504734 blocks reversibly the ex vivo uptake of glycine (mouse cortical homogenates: ID50: 5 mg/kg i.p.), rapidly and for a long duration. SSR504734 increases extracellular levels of glycine in the rat prefrontal cortex (PFC), potentiates NMDA-mediated excitatory postsynaptic currents (EPSCs) in rat hippocampal slices (MEC=0.5 uM) and intrastriatal glycine-induced rotations in mice (MED: 1 mg/kg i.p.). SSR504734 prevented ketamine-induced metabolic activation in mice limbic areas and reversed MK-801-induced hyperactivity and increase in EEG spectral energy in mice and rats, respectively (MED: 10-30 mg/kg i.p.). SSR504734 shows activity in schizophrenia, anxiety and depression models.
