Description
SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 ( IC 50 =18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activitiesIn VitroSSR504734 (15 nM-86 µM; 10 min) inhibits glycine uptake in human SK-N-MC and rat C6 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human neuroblastoma (SK-N-MC) and rat astrocytoma (C6) cells Concentration: 15 nM-86 µM Incubation Time: 10 min Result: Showed IC 50 values of 18 and 15 nM for human SK-N-MC and rat C6 cells, respectively.In VivoSSR504734 (i.p. and p.o.; 1-100 mg/kg; once) treatment shows good oral bioavailability. SSR504734 (i.p.; 30 mg/kg; once) induces a rapid and significant decrease of specific glycine uptake. SSR504734 (i.p.; 10 mg/kg; once) increases extracellular levels of Glycine in the prefrontal cortex (PFC) of freely moving rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats Dosage: 1-100 mg/kg Administration: Intraperitoneal injection and oral gavage.; 1-100 mg/kg; once Result: Showed ID 50 values of 5.0 and 4.6 mg/kg for i.p. and p.o. treatments, respectively. Animal Model: Male Sprague-Dawley rats Dosage: 30 mg/kg Administration: Intraperitoneal injection; 30 mg/kg; once Result: Maintained at about 80% inhibition from 1 to 7 h after administration. Animal Model: Male Sprague-Dawley rats Dosage: 10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg; once Result: Produced a rapid and sustained increase in PFC extracellular levels of glycine.Form:SolidIC50& Target:hGlyT1 18 nM (IC 50 ) rGlyT1 15 nM (IC 50 )