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 activities
In Vitro
SSR504734 (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 Vivo
SSR504734 (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.
