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SSR504734 is a potent, selective, reversible, and orally active small molecule inhibitor of glycine transporter 1 (GlyT1). By inhibiting GlyT1, SSR504734 elevates glycine availability in the vicinity of N-methyl-D-aspartate receptor (NMDAR)-containing glutamatergic synapses, enhancing NMDAR function. This mechanism is of interest for neuropsychiatric disorders such as schizophrenia and cognitive impairment, as it may balance excitation and inhibition in key brain regions. SSR504734 has demonstrated pro-cognitive and antipsychotic-like activity in animal models, but clinical development has been discontinued[1][2][3][4][5].
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