MHP133是一种多靶点抑制剂，可以抑制AChE的活性，KKi值为69μM;同时抑制毒蕈碱M1和M2受体，5HT4受体和咪唑I2受体。
CAS：147340-43-0
分子式：C17H20ClN5O3
分子量：377.83
纯度：98%
存储：Store at -20°C

Background:

a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.

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 ED50 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[1].

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[1].

参考文献：

[1]. Buccafusco JJ, et al. MHP-133, a drug with multiple CNS targets: potential for neuroprotection and enhanced cognition. Neurochem Res. 2007 Jul;32(7):1224-37. Epub 2007 Apr 3.