规格: | 98% |
分子量: | 388.4 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Background:
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[1][2].
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[1].
ASP2905 treatment inhibits hyperlocomotion induced by Phencyclidine. And significantly ameliorates Phencyclidine-induced prolongation of immobility time in mice subjected to the forced swimming test[2].
参考文献:
[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.