butyrylcholinesterase

Lucidadiol exhibits butyrylcholinesterase-inhibitory activity at concentrations up to 200 uM, it also possesses inhibitory activity against acetylcholinesterase (AChE) with the percentage inhibition at 100 uM. Lucidadiol shows antiviral activity against i

Rivastigmine (Exelon) 是具有口服活性的、有效的、可透过血脑屏障的胆碱酯酶抑制剂，可抑制丁酰胆碱酯酶和乙酰胆碱酯酶，IC50分别为 0.037 μM 和 4.15 μM。它是一种拟副交感神经剂或胆碱能剂，用于研究轻度至中度阿尔茨海默氏型痴呆和帕金森氏病引起的痴呆。

Rivastigmine tartrate (SDZ-ENA 713) 是一种具有口服活性的、可透过血脑屏障的胆碱酯酶抑制剂，能够抑制丁酰胆碱酯酶和乙酰胆碱酯酶。它是一种拟副交感神经剂或胆碱能剂，用于研究轻度至中度阿尔茨海默氏型痴呆和帕金森氏病引起的痴呆。

RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue. RX 67668 is an effective cholinesterase inhibitor (IC50: 5 μM for both acetylcholinesterase and butyrylcholinesterase). RX 67668 can reverse the neuromuscular blockade induced by D-tub

N-Methylcoclaurine shows binding affinities for the ĸ opioid receptor with the equilibrium dissociation constant (Ki) value of 0.9 ± 0.1 uM. N-methylcoclaurine also shows promising butyrylcholinesterase inhibition activities, with the IC50 value of 1

H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor antagonist. It exhibits inhibitory effects on acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B) with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. With a Ki of 170 nM for hH3R, H3R antagonist 2 demonstrates favorable anti-neuropathic pain and memory-enhancing effects. Additionally, it can cross the blood-brain barrier (BBB) [1].

hBChE-IN-2 是一种丁酰胆碱酯酶 (BChE) 抑制剂和大麻素受体 2 BChE) 抑制剂，具有神经保护活性，可用于研究阿尔茨海默症类的神经系统疾病。

Kuwanon G (Moracenin B) 是一种从桑树中得到的黄酮类蛙皮素受体拮抗剂，具有杀菌作用。

Ethoxysanguinarine (6-Ethoxydihydrosanguinarine) 是存在于龙葵中的一种苯并菲啶生物碱天然产物，通过抑制蛋白磷酸酶 2A，可抑制结直肠癌细胞活力，诱导细胞凋亡。

BuChE-IN-TM-10 (TM-10) 是一种有效的丁基胆碱酯酶 (BuChE) 抑制剂，其IC50 值为8.9 nM。BuChE inhibitor 1能够抑制和分解自诱导的Aβ聚合, 表现出强大的抗氧化活性和良好的血脑屏障 (BBB) 渗透性。可用于阿尔兹海默症的研究。

Garcinol 是一种从印度藤黄提取的聚异戊二烯基二苯甲酮，对乙酰胆碱酯酶和丁酰胆碱酯酶具有抗胆碱酯酶的特性，IC50分别为 0.66 µM 和 7.39 µM。它还抑制组蛋白乙酰转移酶和 p300 CPB 相关因子，具有抗炎和抗癌活性。

CL-13, 作为一种丁基胆碱酯酶 (BChE) 抑制剂，其IC50值达到1.15 μM，并具有针对乙酰胆碱酯酶的高选择性，选择性指数(SI)为9.2。在SH-SY5Y细胞中，CL-13展现了显著的抗氧化活性（DPPHEC50= 47.01 μM），能够螯合参与Aβ聚集及 或氧化应激的金属，且在50 μM浓度下不表现出神经毒性。此外，CL-13能有效逆转由东莨菪碱引发的认知障碍，同时不影响小鼠的运动能力。

AChE BChE-IN-23（Compound 6e）作为一种AChE BChE抑制剂，对AChE、eqBChE 和 hBChE具备较强的抑制效应，其IC50分别为0.91 μM、1.19 μM 和1.01 μM。该化合物不仅显示出优异的抗氧化活性，而且能够有效抑制Aβ1-42 和Tau蛋白的聚集。此外，AChE BChE-IN-23通过抑制活性氧的释放和减少线粒体损伤，进而抑制小胶质细胞的激活，并降低人小胶质细胞中NLRP3炎症小体的表达。它还能逆转东莨菪碱诱导的小鼠记忆损伤。

4-Methoxyphenyl isothiocyanate (4-Methylphenyl ITC) 是一种具抗氧化特性的化合物，表现出IC50为1.25 mM的DPPH自由基清除能力，并在ORAC测试中显示抗氧化性能为11.7 mM TE（此值相当于11.7 mmol Trolox的抗氧化效力）。在Briggs–Rauscher反应中，它能延长氧化过程约9180秒。此外，4-Methoxyphenyl isothiocyanate 对胆碱酯酶有一定的抑制活性，抑制乙酰胆碱酯酶(AChE)的率为30.4%，抑制丁酰胆碱酯酶(BChE)的率为17.9%。因此，该化合物有望在抗氧化和神经系统疾病研究领域中发挥作用。

BChE-IN-39 (Compound 7c) 是丁酰胆碱酯酶（BChE）的选择性抑制剂，IC50为0.08 μM [抑制AChE的IC50=3.98 μM]。它能下调GSK-3β的表达，并抑制tau蛋白的过度磷酸化。

Bisnorcymserine is a reversible inhibitor of butyrylcholinesterase. The leaving group, bisnoreseroline, interacts in a non-covalent way with Ser(200) and His(440), disrupting the existing interactions within the catalytic triad, and it stacks with Trp(84)

CHF 2819 is a novel orally active acetylcholinesterase inhibitor (AChE) developed for the treatment of Alzheimer's disease (AD). CHF 2819 is a selective inhibitor of AChE, it is 115 times more potent against this enzyme than against butyrylcholinesterase (BuChE).

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)

Ursolic acid acetate (Acetylursolic acid) 分离于 Ficus microcarpa 的气根中，对 KB 细胞显示细胞毒性(IC50:8.4 μM)。

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.

Multitarget AD inhibitor-1 is a reversible and selective inhibitor of butyrylcholinesterase (BuChE) with IC50 values of 7.22 μM and 1.55 μM for human BuChE (hBuChE) and equine serum BuChE (eqBuChE), respectively. Additionally, it exhibits inhibitory activity towards β-secretase (IC50 value of 41.60 μM), amyloid β aggregation (IC50 value of 3.09 μM), and tau aggregation. As a diphenylpropylamine derivative, Multitarget AD inhibitor-1 holds promise for research pertaining to the multifunctional, disease-modifying treatment of Alzheimer's disease.

ACG548B (compound 24) is a highly effective inhibitor of acetyl- and butyrylcholinesterase (AChE and BChE) with IC50 values of 1.78 and 0.496 μM, respectively. It exhibits a greater affinity for AChE and demonstrates selectivity over BChE and ChoK (choline kinase).

1,3,5-Trihydroxy-4-prenylxanthone is a relatively potent inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 3.0 μM; it shows in vitro inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 valu

BChE-IN-14 (compound 19c) 可以在体内恢复认知障碍，可用于研究阿尔茨海默症。BChE-IN-14 具有原代细胞安全性和良好的血脑屏障通透性。BChE-IN-14 是丁酰胆碱酯酶(BChE) 的选择性抑制剂，其对 人BChE 和马血清BChE 的IC50值分别为 0.011 μM 和0.23μM。