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SSR103800 is a potent and selective inhibitor of glycine transporter-1 (GlyT1). By blocking GlyT1, SSR103800 increases synaptic glycine levels, enhancing the function of the N-methyl-D-aspartate (NMDA) receptor—a mechanism thought to counteract hypoglutamatergic states implicated in schizophrenia. Preclinical studies have demonstrated antipsychotic-like and antidepressant-like activity, including the ability to reduce MK-801-induced hyperactivity, increase prepulse inhibition, and reduce despair-related behaviors. It has a reduced side-effect profile compared to classical antipsychotics and does not induce catalepsy. SSR103800 was developed for the management of core symptoms of schizophrenia and comorbid depression states. Development has primarily been preclinical, with evidence of phase 1 testing, but no later clinical stages are reported[1][2][3][5][8].
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