A-582941 dihydrochloride 是选择性和可透过血脑屏障的 α7 nAChR的部分激动剂,在大鼠脑膜和人额叶皮层的Ki值分别为 10.8 和 16.7 nM。它与人5-HT3受体结合,Ki值为 150 nM,具有与各种神经退行性疾病和精神疾病相关的认知缺陷的研究潜力。
产品描述
A 582941 is a Selective agonist of α7 nAChR partial
体内活性
A-582941 was found to exhibit high-affinity binding and partial agonism at alpha7 nAChRs.?In vitro and in vivo studies indicated that A-582941 activates signaling pathways known to be involved in cognitive function such as ERK1/2 and CREB phosphorylation.?A-582941 enhanced cognitive performance in behavioral models that capture domains of working memory, short-term recognition memory, memory consolidation, and sensory gating deficit.?A-582941 exhibited a benign secondary pharmacodynamic and tolerability profile as assessed in a battery of assays of cardiovascular, gastrointestinal, and CNS function.
Cas No.
848591-90-2
分子式
C17H20N4
分子量
280.375
别名
A 582941;A-582941 dihydrochloride
储存和溶解度
DMSO:55 mg/ml (196.17 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years