| Description | 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 |
| In vitro | 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]. |
| In vivo | 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] |
| Synonyms | ASP-2905 |
| molecular weight | 388.4 |
| Molecular formula | C20H17FN8 |
| CAS | 792184-90-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 27.5 mg/mL (70.8 mM) |
| References | 1. Shinji Takahashi, et al. Neurochemical and neuropharmacological characterization of ASP2905, a novel potent selective inhibitor of the potassium channel KCNH3. Eur J Pharmacol. 2017 Sep 5;810:26-35. 2. Shinji Takahashi, et al. ASP2905, a specific inhibitor of the potassium channel Kv12.2 encoded by the Kcnh3 gene, is psychoactive in mice. Behav Brain Res. 2020 Jan 27;378:112315. |