AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia[1].
AS057278 (PO; 20 mg/kg b.i.d for 28 days; 80 mg/kg single dosage) normalizes phencyclidine (PCP)-induced prepulse inhibition[1].AS057278 (10 mg/kg; PO and IV; single dosage) exhibits good pharmacokinetic effects[1].Pharmacokinetic Parameters of AS057278 in male Sprague-Dawley rats[1]. IV (10 mg/kg) PO (10 mg/kg) C0 (ng/mL)100,557.3Cmax (ng/mL)73,559.88088.8tmax (h)0.0831CZ (ng/mL)26.840.5tZ (h)2424AUCZ (ng/mL.h)45,596.218,254.4 ΛZ (h^-1)0.1240.096AUC (ng/mL.h)45,810.918,649.9VZ (L/kg)1.76VSS (L/kg)0.24CL (L/kg/h)0.22MRT (h)1.087F0.407
[1]. Adage T, et al. In vitro and in vivo pharmacological profile of AS057278, a selective d-amino acid oxidase inhibitor with potential anti-psychotic properties. Eur Neuropsychopharmacol. 2008;18(3):200-214.