ASP2905 is a potent and selective potassium channel Kv12.2 inhibitor encoded by the Kcnh3/BEC1 gene. ASP2905 can cross the blood-brain barrier and has antipsychotic activities.
体外研究
ASP2905 potently inhibits potassium currents in CHO cells expressing KCNH3 (IC50 of 9.0 nM). ASP2905 (≤10 μM) minimally bound with low affinities to 55 transmembrane proteins. ASP2905 (0.1 µM, 1 µM) decreases the frequency of spontaneous inhibitory postsynaptic currents in cultured rat hippocampal neurons.
体内研究
ASP2905 treatment inhibits hyperlocomotion induced by Phencyclidine. And significantly ameliorates Phencyclidine-induced prolongation of immobility time in mice subjected to the forced swimming test.
Animal Model:
Male ddY mice (aged 4-5 weeks) injected with Phencyclidine hydrochloride (PCP)
Dosage:
0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg
Administration:
Oral administration; once
Result:
Inhibited hyperlocomotion induced by Phencyclidine.
分子式
C20H17FN8
分子量
388.40
CAS号
792184-90-8
运输条件
Room temperature in continental US; may vary elsewhere.