Cholinesterase (ChE) Inhibitor

Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO^- scavenging effect (IC₅₀, 16.83 μM), and may protect against Alzheimer disease. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberine has the potential effect in the research of diabetic disease.

Rivastigmine tartrate (ENA 713; SDZ-ENA 713) 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 tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate 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.

Pyridostigmine bromide is an orally active cholinesterase (ChE) inhibitor that can be used in cardiovascular disease research.

Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC₅₀ of 74.6 μM.

(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC₅₀ of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.

Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.

Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers.

Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.

Nodakenin is a major coumarin glucoside in the root of Angelica decusiva. Nodakenin inhibits acetylcholinesterase (AChE) activity with an IC₅₀ of 84.7 μM.

Tacrine hydrochloride is a potent brain-penetrant inhibitor of both AChE and BChE, with IC₅₀s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC₅₀ of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease.

Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC₅₀ of 226 μM. Corydaline is a μ-opioid receptor (K_i of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC₅₀ of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities.

Ethopropazine (Isothazine) hydrochloride is a potent and selective BChE inhibitor, a poor AChE inhibitor and a non-selective mAChR and NMDA antagonist. Ethopropazine hydrochloride has anticholinergic, antihistamine, antiadrenergic actions and properties. Ethopropazine hydrochloride alleviates thermal hyperalgesia in a dose dependent manner. Ethopropazine hydrochloride can be used for the research of Parkinson’s disease.

(-)-Carvone is an insect neurotoxin and a irreversible acetylcholinesterase (AChE) inhibitor. (-)-Carvone can be used as a bird repellent, inhibits larval growth, decreases pupatation rate, and increases mortality of larvae.

Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning.

Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC₅₀ = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease.

Coumaran (2,3-Dihydrobenzofuran) is an AChE inhibitor with antileishmanial activity. Coumaran may acquire antiparasitic capabilities through activation of macrophages and exert immunomodulatory activity. Coumaran can be used as a biopesticide..

Protriptyline hydrochloride is a potent tricyclic antidepressant (TCA). Protriptyline hydrochloride inhibits AChE activity with an IC₅₀ value of 0.06 mM and inhibits Aβ self-assembly. Protriptyline hydrochloride can be used for the study of depression and Alzheimers disease.

Cyanidin-3-O-galactoside chloride (Ideain chloride) is a component from extract peel of hawthorn fruit (EPHF) with the value of 179.4 mg/g. EPHF exhibits strong AChE inhibitory activity.

Protopine (Corydinine), an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity.