SSR504734 is an orally active, selective, and reversible inhibitor of human, rat, and mouse GlyT1 (IC50 = 18, 15, and 38 nM, respectively). SSR504734 exhibits activity in schizophrenia, anxiety, and depression models [1].

SSR504734 (15 nM-86 μM; 10 min) inhibits the ex vivo uptake of glycine in human SK-N-MC and rat C6 cells, with IC50 values of 18 nM and 15 nM, respectively [1].

SSR504734 (i.p. and p.o.; 1-100 mg/kg; once) demonstrates good oral bioavailability with ID50 values of 5.0 and 4.6 mg/kg for i.p. and p.o. treatments, respectively [1]. At 30 mg/kg (i.p.; once), it maintains approximately 80% inhibition of specific glycine uptake from 1 to 7 hours post-administration [1]. At 10 mg/kg (i.p.; once), it rapidly and significantly increases extracellular glycine levels in the prefrontal cortex of freely moving male Sprague-Dawley rats [1].