Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation[1][2].
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease[1].
AChE-IN-30 is an AChE inhibitor with an IC50 value of 4.4 μM. AChE-IN-30 has neuroprotective activity, and inhibits H2O2-induced apoptosis by suppressing intracellular ROS accumulation. AChE-IN-30 can be used for research of Alzheimer's disease[1].
Methyl tridecanoate-d25 is the deuterium labeled Methyl tridecanoate. Methyl tridecanoate moderately inhibits β-amyloid aggregation. Methyl tridecanoate weakly inhibits acetylcholinesterase (AChE)[1].
Isorosmanol is an abietane-type diterpene isolated from the leaves of sage, with antioxidant, neuroprotective and neurotrophic effects. Isorosmanol inhibits AChE activity and melanin synthesis[1][2][3].
7β-Hydroxybufalin is a bufadienolide that isolated from the venom of Bufo bufo gargarizans. 7β-Hydroxybufalin inhibits α-glucosidase and acetylcholinesterase[1].
Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM.
Scopoletin is an inhibitor of acetylcholinesterase (AChE).
Aposcopolamine is an alkaloid that can be isolated from Datura ferox. Aposcopolamin can closely binds with ACHE, ADRA2A and CHRM2. Aposcopolamine can be used for the research of Alzheimer's disease[1].
AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with Ki values of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 can cross the BBB and has low cytotoxicity[1].
Picfeltarraenin IV, a triterpenoid obtained from Picriafel-terrae Lour (P.fel-terrae), is an acetylcholinesterase (AChE) inhibitor. Picfeltarraenin IV can be used for the treatment of herpes infections, cancer and inflammation[1].
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.
Isonaringin shows anti-Alzheimer’s activity by inhibiting AChE[1].
Penconazole-d7 is the deuterium labeled Penconazole[1]. Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats[2][3].
Glycyl-L-glutamic acid is a neurotrophic factor (NF) in vivo, and exerts function of maintenance of AChE content and activity. Glycyl-L-glutamic acid doesn’t act directly on AChE synthesis, and may prevent preganglionic neuronal degeneration[1][2].
Xanthohumol I, a chalkone, is a derivative of Xanthohumol (HY-N1067). Xanthohumol is a Cholinesterase (ChE) inhibitor, which inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) wih IC50s of 71.34 μM and 32.67 μM, respectively. The hydroxy compound of Xanthohumol (3-hydroxy-xanthohumol), also shoes inhibitory effect on AChE and BChE with IC50s of 51.25 μM and 63.07 μM[1].
Trimyristin--d15 is the deuterium labeled Trimyristin. 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].
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity[1][2].
Hexafluorenium dibromide (Mylaxen) is a potent cholinesterase (ChE) inhibitor with pI50 value of 6.96 and Ki value of 2.4 nM for human plasma cholinesterase (ChE)[1].
Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory[1][2][3].
Fosthiazate is a broad-spectrum nematicide against various plant parasitic nematodes, including Meloidogyne spp., Globodera spp., and Pratylenchus spp., through inhibiting the synthesis of acetylcholinesterase[1].
Dehydronuciferine is isolated from the leaves of Nelumbo nucifera Gaertn, a acetylcholinesterase (AChE) inhibitor with an IC50 of 25 μg/mL[1].
COX-2-IN-22 (Compound 4h) is a COX-2 inhibitor with an IC50 of 8.6 µM. COX-2-IN-22 also inhibits AChE, BChE, β-Secretase, LOX-5 and DPPH with IC50 values of 2.8, 6.3, 15.3, 13.9 and 6.8 µM, respectively. COX-2-IN-22 can cross BBB[1].
Coumaran (2,3-Dihydrobenzofuran) is an acetylcholinesterase (AChE) inhibitor isolated from leaves of L. camara. Coumaran can be used as a biopesticide[1].
Methyl tridecanoate moderately inhibits β-amyloid aggregation. Methyl tridecanoate weakly inhibits acetylcholinesterase (AChE)[1].
(R)-Rivastigmine D6 (tartrate) is the deuterium labeled (R)-Rivastigmine, which is an cholinesterase inhibitor.
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD)[1][2].
Nodakenin is a major coumarin glucoside in the root of Peucedanum decursivum Maxim. Nodakenin inhibits acetylcholinesterase (AChE) activity with an IC50 of 84.7 μM[1][2].
Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease[1][2][3][4].