Z218484536 is a selective phosphoserine phosphatase (PSPH) inhibitor that can penetrate the blood-brain barrier. It binds to PSPH with an affinity (Kd) of approximately 0.23 μM. By doing so, Z218484536 reduces levels of L-serine and D-serine in astrocytes. It also inhibits spontaneous seizures without causing significant side effects and demonstrates effective antiepileptic properties in the temporal lobe epilepsy (TLE) model.

Z218484536 inhibits the release of L-serine in cultured astrocytes with an IC50 of 0.4 μM and reduces intracellular L-serine levels with an IC50 of 0.38 μM when used in concentrations ranging from 40 to 2,000 nM for 24 hours. Additionally, Z218484536 shows no cytotoxic effects on the proliferation of HepG2 cells when used at concentrations between 0.078 and 40 μM for 48 hours.

Z218484536, when administered via intraperitoneal injection at doses of 0.5-20 mg/kg once daily for 3 days, can delay acute seizures and reduce their severity while exhibiting anticonvulsant effects in the pentylenetetrazol (PTZ) induced acute seizure model. In a TLE mouse model induced by (red algae acid) KA, Z218484536 at 2 mg/kg and 4 mg/kg intraperitoneally once daily for 3 days, reduces hippocampal L-serine and D-serine levels. Spontaneous seizures in TLE mice are inhibited by Z218484536 at a dose of 2 mg/kg or 4 mg/kg once daily over a 7-week period. Administering 4 mg/kg of Z218484536 intraperitoneally for 7 days does not affect emotional state or motor ability in mice. Additionally, Z218484536 at doses of 1 mg/kg or 2 mg/kg given intraperitoneally once daily for 2 weeks over a period of 3.5 months decreases seizure activity in a cynomolgus monkey TLE model.