ASP-2905 是一种有效且选择性的钾通道Kv12.2抑制剂。ASP2905 可以穿越血脑屏障并具有抗精神病活性。

ASP-2905 is a potent and selective inhibitor of potassium channel Kv12.2 encoded by the Kcnh3/BEC1 gene. It can cross the blood-brain barrier and has antipsychotic activities

ASP2905 (0.1 M, 1 M) decreased the frequency of spontaneous inhibitory postsynaptic currents in cultured rat hippocampal neurons.?In mice, ASP2905 reversed the disruption of spontaneous alternation behavior induced by MK-801 and scopolamine (minimum effective dose of ASP2905: 0.0625mg/kg, po).?ASP2905 ameliorated the cognitive deficits of aged rats in step-through passive avoidance (0.0313 and 0.0625mg/kg, po) and Morris water-maze tasks (0.01mg/kg, po) and effectively penetrated the brain.?The mean plasma and brain concentrations of ASP2905 reached their maxima (Cmax = 0.399ng/ml and 1.77ng/g, respectively) 1h after a single oral administration and then decreased (t1/2 = 1.5-1.6h) (brain plasma ratio = 2.7-4.9).?ASP2905 is a selective, orally administered inhibitor of KCNH3, which can enhance cognitive performance[1].

ASP2905 on channel activity in vitro and its neuropharmacological properties in young and aged rats as well as in mice.?ASP2905 potently inhibited potassium currents in CHO cells expressing KCNH3 (IC50 = 9.0nM).?In contrast, ASP2905 ( 10μM) minimally bound with low affinities to 55 transmembrane proteins.[1]

792184-90-8

C20H17FN8

388.41

ASP-2905;ASP2905

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years