Cholinesterase (ChE) Inhibitor

α-Amylase-IN-3 (Compound 4) is the inhibitor for α-Amylase, AChE and AChE with IC₅₀s of 18.04 μM, 21.04 μM and 22.2 μM, respectively. α-Amylase-IN-3 exhibits antioxidant activity. α-Amylase-IN-3 can be used in research of diabetes and oxidative stress associated disease.

Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine is a potent and orally active inhibitor of AChE (IC₅₀=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.

Kuwanon U is a potent cholinesterase inhibitor with IC₅₀s of 19.69, 10.11 µM and K_is of 6.48, 9.59 µM for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively. Kuwanon U has the potential for the research of Alzheimer’s disease (AD).

P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC₅₀ of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease.

Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC₅₀ of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes.

O-Desmethyl Galanthamine (Sanguinine) is galanthamine-type alkaloid. O-Desmethyl Galanthamine is an acetylcholinesterase (AChE) inhibitor, with an IC₅₀ 1.83 μM.

Pitofenone hydrochloride, a spasmolytic compound, inhibits the acetylcholinesterase (AChE) activity from bovine erythrocytes and from electric eel with K_is of 36 and 45 μM, respectively.

Minaprine is a brain-penetrant monoamine oxidase inhibitor. Minaprine also weakly inhibits acetylcholinesterase (AChE) activity. Minaprine reduces intraneuronal dopamine metabolism, lowers striatal homovanillic acid and dihydroxyphenylacetic acid levels, and raises striatal 3-methoxytyramine and 5-hydroxytryptamine levels. Minaprine exhibits convulsant, antidepressant properties.

Epiberberine 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 has antioxidant activity, with peroxynitrite ONOO^- scavenging effect (IC₅₀, 16.83 μM), and can be used for the research of Alzheimer disease. Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberinecan be used for the research of diabetic disease.

Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC₅₀s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease. Ladostigil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Norneostigmine is a potent inhibitor of AChE that can penetrate the blood-brain barrier. Norneostigmine can achieve a 50% inhibition rate of mouse brain AChE after 10 min treatment, which is close to the inhibitory effect of tetrahydroaminoacridine (57% at 10 min). Norneostigmine can be used to study memory disorders related to Alzheimer's disease and other memory disorders.

Benactyzine hydrochloride is a competitive BChE inhibitor with a K_i of 0.01 mM. Benactyzine hydrochloride is an anticholinergic drug. Benactyzine hydrochloride has the potential for organophosphate poisoning research.

Dihydrogalanthamine hydrobromide is the hydrobromide form of 1,2-dihydrogalanthamine, which exhibits acetylcholinesterase (acetylcholinesterase, AChE) inhibitory activity. Dihydrogalanthamine hydrobromide can be used in the research of nervous system-related diseases.

Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABA_Areceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .

(R)-Donepezil is a R-enantiomer of Donepezil (HY-14566). Donepezil is a specific and potent AChE inhibitor.

Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K_i values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD).

Broussonin A is a potent BChE inhibitor, with an IC₅₀ of 4.16 µM. Broussonin A is a diarylpropane natural product that can be isolated from the bark of Broussonetia papyrifera after solid fermentation.

Osmanthuside B can be isolated from Pseuderanthemum carruthersii (Seem.) Guill. var. atropurpureum (Bull.) Fosb and has weak acetylcholinesterase inhibitory activity.

(S)-Donepezil is a S-enantiomer of Donepezil (HY-14566). Donepezil is a specific and potent AChE inhibitor.

Kokusaginine is a furoquinoline alkaloids, which exhibits inhibitory efficacy for acetylcholinesterase (AChE) with an IC₅₀ of 28.2 μM. Kokusaginine exhibits anti-proliferative and apoptotic inducing effects in MCF-7/ADR cells.