Tilapertin is an oral inhibitor of glycine transporter type-1 (GlyT1).
in vivo
Tilapertin is a nanomolar potent, orally bioavailable and selective GlyT1 inhibitor. Oral administration of Tilapertin dose-dependently increases cerebrospinal fluid (CSF) glycine concentration in rats[1].
IC 50
GlyT1
References
[1] Dunayevich E, et al. Efficacy and safety of the glycine transporter type-1 inhibitor AMG 747 for the treatment of negative symptoms associated with schizophrenia. Schizophr Res. 2017 Apr;182:90-97. DOI:10.1016/j.schres.2016.10.027
