AS057278 是一种有效、具有选择性、口服活性和血脑屏障渗透性的 D-氨基酸氧化酶 (DAAO) 非肽抑制剂，IC50 为 0.91 μM，EC50 为 2.2-3.95 μM。AS057278 可使苯环已哌啶 (PCP) 诱导的小鼠前脉冲抑制恢复正常。AS057278 可用于精神分裂症的研究。
货号:ajcx38536
CAS:402-61-9
分子式:C5H6N2O2
分子量：126.11
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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) C_{0 (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.