α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy[1].
Echothiopate iodide is a potent hBChE (human butyrylcholinesterase) inhibitor. Echothiopate iodide is a long-acting anticholinesterase agent. Echothiopate iodide can be used for glaucoma research[1][2].
Ladostigil (TV-3326) is a dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with an IC50 of 37.1 and 31.8 μM for MAO-B and AChE, reapectively. Ladostigil could increase cholinergic transmission, prevent the formation of ROS or their actions and be used for the research of depression and Alzheimer's disease[1][2].
hCAI/II-IN-5 (compound MZ8) is a potent hCA I and hCA II (human carbonic anhydrase isoenzymes I and II) inhibitor, with IC50 values of 37.88 and 45.23 nM, respectively. hCAI/II-IN-5 also shows inhibition profile against α-Glycosidase and AChE, with IC50 values of 48.98 and 420.14 nM, respectively. hCAI/II-IN-5 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy[1].
AChE-IN-20 (compound M26) is a potent AChE inhibitor with IC50 value of 397.32 nM and with Ki value of 335.76 nM. AChE-IN-20 shows inhibition potency against hCA I , hCA II and α-GLY with IC50 values of 84.14, 69.24 and 52.08 nM and with Ki values of 97.86, 76.23 and 57.93 nM, respectively[1].
3β-Hydroxy-lup-20(29)-en-16-one (compound 9) is a dual inhibitor of AChE and BChE, with selectivity for BChE (IC50: 28.9 μM)[1].
BChE-IN-10 (compound 6) is a potent butyrylcholinesterase (BChE) mixed-type inhibitor with an IC50 value of 6.4 μM. BChE-IN-10 can be isolated from Bletilla striata. BChE-IN-10 can be used for the research of Alzheimer's disease (AD)[1].
(Rac)-Rivastigmine-d6 ((Rac)-Rivastigmine-d6) is a labelled racemic Rivastigmine. Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
Coumarinic acid is a brain-penetrating inhibitor of AChE and β-amyloid. Coumarinic acid can be used in study anti-Alzheimer drug[1].
Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.
Dihydro Donepezil (Dihydro E2020) is a metabolite of Donepezil. Donepezil is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bAChE and hAChE, respectively[1].
Lucidadiol is a natural compound isolated from Ganoderma lucidum. Lucidadiol exhibits acetylcholinesterase-inhibitory activity, with IC50 values of 31 μM. Lucidadiol shows antiviral activity against influenza virus type A and HSV type 1[1][2].
hBChE-IN-1 (compound 4), a quinolizidinyl derivative, is a potent hBChE inhibitor (IC50=7 nM) and highly selective over hAChE. hBChE-IN-1 shows inhibitory activity against tau and Aβ40 protein aggregation, with IC50 values of 20 and 4.3 μM, respectively. hBChE-IN-1 can be used for Alzheimer's disease research[1].
Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside), a flavonol, possesses enzyme inhibition property towards α-amylase, α-glucosidase and Acetylcholinesterase. Kaempferol-3,7-di-O-β-glucoside protects differentiating neuronal cells, SH-SY5Y from Amyloid β peptide-induced injury. Kaempferol-3,7-di-O-β-glucoside has the potential for Alzheimer's research[1].
(±)-Marmesin is a good precursor of the linear furanocoumarins. (±)-Marmesin derivatives have high degree of acetylcholinesterase inhibitory property[1][2].
Protriptyline is a tricyclic antidepressant (TCA), specifically a secondary amine, for the treatment of depression and ADHD. Unique among the TCAs, protriptyline tends to be energizing instead of sedating, used for narcolepsy to achieve a wakefulness-promoting effect.
BChE-IN-11 (compound 10) is a potent, selective and non-competitive BChE (butyrylcholinesterase) inhibitor, with an IC50 of 2.1 μM. BChE-IN-11 can be used for Alzheimer's disease (AD) research[1].
Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively[1].
TAE-1 is a potent inhibitor of AChE and BuChE. TAE-1 also inhibits Aβ fibril formation and aggregation. TAE-1 can be used for the researches of Alzheimer's disease[1].
Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
Rivastigmine, an cholinesterase inhibitor(IC50= 5.5 uM), inhibits both butyrylcholinesterase and acetylcholinesteraseIC50 value: 5.5 uMTarget: AChERivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease. The drug can be administered orally or via a transdermal patch; the latter form reduces the prevalence of side effects, which typically include nausea and vomiting. The drug is eliminated through the urine, and appears to have relatively few drug-drug interactions. Rivastigmine, a cholinesterase inhibitor, inhibits both butyrylcholinesterase and acetylcholinesterase. It is thought to work by inhibiting these cholinesterase enzymes, which would otherwise break down the brain chemical acetylcholine.
Hydrangenol 8-O-glucoside (Hydrangenol 8-O-β-D-glucopyranoside) can be isolated from Hydrangea macrophyllu. Hydrangenol 8-O-glucoside is an AChE inhibitor (IC50: 22.66 μM). Hydrangenol 8-O-glucoside inhibits passive cutaneous anaphylaxis (PCA) reaction[1][2].
Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and elevate acetylcholine levels in the brain. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3].
BuChE-IN-4 (Compound C6) is a potent inhibitor of BuChE with an IC50 of 7.7 nM. BuChE-IN-4 exhibits mild antioxidant capacity, nontoxicity, lipophilicity and neuroprotective activity[1].
AChE-IN-15 (Compound 3d) is a reversible human acetylcholinesterase (huAChE) (IC50=6.8 μM) and human butyrylcholinesterase (huBChE) (IC50=16.1 μM) inhibitor. AChE-IN-15 shows significant antioxidant potency, AChE-IN-15 can be used for the research of Alzheimer’s disease[1].
Esculentoside B (Phytolaccoside B) is a natural product from the roots of Phytolacca acinosa Roxb. Esculentoside B is neurotoxic to zebrafish larvae, and impairs their central nervous system development. Esculentoside B inhibits inflammatory response and has antifungal activity[1][2][3].
Velnacrine maleate (HP 029) is an orally active cholinesterase inhibitor that can be used for the research of Alzheimer's disease[1].
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM[1]. Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL[2]. Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM[3].
Pitofenone hydrochloride, a spasmolytic compound, inhibits the acetylcholinesterase (AChE) activity from bovine erythrocytes and from electric eel with Kis of 36 and 45 μM, respectively.
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory[1][2][3].