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147340-43-0

中文名称 147340-43-0
英文名称 MHP 133
CAS 147340-43-0
分子式 C17H20ClN5O3
分子量 377.83
MOL 文件 147340-43-0.mol
147340-43-0 结构式 147340-43-0 结构式

基本信息

中文别名
化合物 T13772
英文别名
MHP 133

物理化学性质

储存条件-20°C储存
溶解度溶于二甲基亚砜

常见问题列表

生物活性
MHP 133 是一种多靶点抑制剂,可以抑制 AChE 的活性,KKi 值为 69 μM;同时抑制毒蕈碱 M1 和 M2 受体,5HT4 受体 和咪唑 I2 受体。
靶点

AChE

69 μM (Ki)

muscarinic M1 receptor

muscarinic M2 receptor

5-HT 4 Receptor

体外研究

MHP-133 is be active (>50% displacement or activity) against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors. MHP-133 exhibits this nicotinic-like activity in the cell line. Although the ED 50 for inducing TrkA expression is only about 1 μM, it does predicts the cytoprotective action of MHP-133 in differentiated PC-12 cells deprived of growth factor for 24 h. MHP-133 (10-100 μM) significantly increases the levels of sAPP from cultured astrocytes by 40-60%. MHP-133 produces a bi-phasic effect on slice survival, particularly in the dentate gyrus and the CA1 regions.

体内研究

In rats, MHP-133 (50, 100, or 200 μg/kg, i.p.) enhances acquisition of the task and increases task accuracy. MHP-133 elicits significant improvements in task accuracies during sessions initiated 10 min after dosing.

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