SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities[1].
SSR504734 (15 nM-86 μM; 10 min) inhibits glycine uptake 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 IC50 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 shows 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 ID50 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. |
[1]. Ronan DepoortÈre, et al. Neurochemical, electrophysiological and pharmacological profiles of the selective inhibitor of the glycine transporter-1 SSR504734, a potential new type of antipsychotic. Neuropsychopharmacology. 2005 Nov;30(11):1963-85.