AChE/BChE-IN-3

AChE BChE-IN-3 (BMC-1) 是AChE 和BChE 的双重抑制剂，对电鳗 AChE (elAChE) 的IC50值为 6.08 μM ，对马血清 BChE (eqBChE) 的IC50值为 0.383 μM。

AChE BChE-IN-3 (BMC-1) hydrochloride 是 AChE 和 BChE 的双重抑制剂。AChE BChE-IN-3 对马血清 BChE (eqBChE) 和电鳗 AChE (elAChE) 的 IC50值分别为 0.383 μM 和 6.08 μM。

hBChE-IN-3（compound 30）兼具碳酸酐酶（CA）激活和胆碱酯酶（ChE）抑制功能，其对AchE和BchE的IC50值分别是7.4 nM和1.9 nM。该化合物适用于神经退行性与精神疾病的研究领域。

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value of 11.3 nM. Oral administration of donecopride (1 mg/kg) reduces brain soluble and insoluble amyloid-β (1-42) levels and increases the time spent exploring the novel object in the novel object recognition (NOR) test in the 5XFAD transgenic mouse model of Alzheimer's disease. Donecopride (3 mg/kg, p.o.) prevents a reduction in spontaneous alternation behavior induced by intracerebroventricular administration of soluble Aβ42 (sAβ42) in the Y-maze in mice.2 1.Lecoutey, C., Hedou, D., Freret, T., et al.Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatmentProc. Natl. Acad. Sci. USA111(36)E3825-E3830(2014) 2.Rochais, C., Lecoutey, C., Hamidouche, K., et al.Donecopride, a Swiss army knife with potential against Alzheimer's diseaseBr. J. Pharmacol.177(9)1988-2005(2020)

Rivastigmine carbamate impurity (3-Nitrophenyl ethyl(methyl)carbamate) is a byproduct found in Rivastigmine, which is recognized as a powerful and orally active inhibitor of cholinesterase (ChE). Specifically, Rivastigmine effectively inhibits both butyrylcholinesterase (BChE) and acetylcholinesterase (AChE), with IC50 values of 0.037 μM and 4.15 μM, respectively.

AChE BChE-IN-4 (BMC-3) 是 AChE 和 BChE 的双重抑制剂，可透过血脑屏障。AChE BChE-IN-4 对人 AChE (hAChE) 和 BChE (hBChE) 的 IC50值分别为 792 nM 和 2.2 nM。

BChE-IN-3 是一种选择性的、选择性的、时间依赖性的、假不可逆的 BChE 丁酰胆碱酯酶抑制剂 (IC50: 56.9 nM)。BChE-IN-3 对 AChE 乙酰胆碱酯酶表现出边缘可逆 (不依赖于时间) 的抑制作用。

AChE BChE MAO-B-IN-3 是一种 1-茚满酮衍生物，是一种有效的MAO-B 抑制剂，对人MAO-B 的IC50为 0.0359 μM。AChE BChE MAO-B-IN-3 是一种有效的AChE 和BChE 酶抑制剂，对人AChE 和BChE 酶的IC50值分别为 0.0473 μM 和 0.0782 μM。AChE BChE MAO-B-IN-3 显示出显着的抗氧化活性，并具有用于阿尔茨海默病 (AD) 研究的潜力。