SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 ( IC 50 =18, 15, and 38 nM, respectively). SSR504734 exhibits activity in schizophrenia, anxiety and depression models [1].

GlyT1 (human):18 nM, GlyT1 (rat):15 nM

SSR504734 (15 nM-86 μM; 10 min) inhibits the ex vivo uptake of glycine in human SK-N-MC and rat C6 cells [1]. Cell Viability Assay [1] Cell 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.

SSR504734 (i.p. and p.o.; 1-100 mg/kg; once) treatment demonstrates good oral bioavailability [1]. SSR504734 (i.p.; 30 mg/kg; once) induces a rapid and significant decrease of specific glycine uptake [1]. SSR504734 (i.p.; 10 mg/kg; once) increases extracellular levels of Glycine in the prefrontal cortex (PFC) of freely moving rats [1]. Animal Model: Male Sprague-Dawley rats [1] 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 [1] 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 [1] Dosage: 10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg; once Result: Produced a rapid and sustained increase in PFC extracellular levels of glycine.