ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease.
体外研究
ASP2535 potently inhibits rat GlyT1 (IC50=92 nM) with 50-fold selectivity over rat glycine transporter-2 (GlyT2) in vitro.
体内研究
ASP2535 (0.3-3 mg/kg; p.o) attenuates working memory deficit in MK-801-treated mice and visual learning deficit in neonatally phencyclidine (PCP)-treated mice.
ASP2535 (1-3 mg/kg, p.o.) also improves the PCP-induced deficit in prepulse inhibition in rats.
Animal Model:
5-week-old male ddY mice
Dosage:
0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration:
Oral administration
Result:
Significantly attenuated the MK-801-induced decrease in alternation rate.
分子式
C22H18N6O
分子量
382.42
CAS号
374886-51-8
运输条件
Room temperature in continental US; may vary elsewhere.