AChR

Inhibitory Selectivity

Isoform-specific Inhibitors

AChR Products

New AChR Products
Catalog No. Information Product Use Citations Product Validations
S3245

Nodakenetin

Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.

S9219

Huperzine B

Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects.

S5886

Hodostin

Hodostin (Neostigmine methyl sulfate, Syntostigmin, Neostigmeth) is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis.

S3913New

Pimethixene maleate

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.

S5022New

Varenicline Hydrochloride

Varenicline (CP 526555) Hydrochloride is a potent and selective inhibitor of nicotine acetylcholine receptor (nAChR) with Ki of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively.

S3311New

Myosmine

Myosmine is not only one of the minor tobacco alkaloids but is also present in various foods. Myosmine has low affinity against a4b2 nicotinic acetylcholinergic receptors (nAChR) with Ki of 3300 nM.

S3246

Picfeltarraenin IB

Picfeltarraenin IB, a cucurbitacin glycoside isolated from Picriafel-terrae, is an inhibitor of acetylcholinesterase (AChE). Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation.

S3820

Dehydroevodiamine hydrochloride

Dehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production.

S9252

Corydaline

Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers.

S0766

RHC 80267

RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC).

S9260

Nodakenin

Nodakenin ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM.

S9069

Jatrorrhizine chloride

Jatrorrhizine chloride (Neprotine, Yatrorhizine) is the hydrochloride salt form of jatrorrhizine, which is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.

S3884

Jatrorrhizine

Jatrorrhizine (Neprotin, Yatrorizine), one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.

S3904

Isoimperatorin

Isoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. 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.

S9138

Picfeltarraenin IA

Picfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system.

S0016

SN-6

SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.

S0032

Batefenterol 

Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively.

S6985New

Varenicline

Varenicline is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors.

S5777New

Ipratropium bromide monohydrate

Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively.

S4713New

Atropine

Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.

S3298

Caulophylline (N-Methylcytisine)

Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.

S0717

Varenicline (CP 526555) dihydrochloride

Varenicline (CP 526555, Chantix, Champix) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.

S9789New

JHU37152

JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

S9790New

JHU37160

JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

S7366

LY2119620

LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.

S6887

Clozapine N-oxide

Clozapine N-oxide (CNO) is a metabolite of Clozapine (GLXC-06516) and an agonist of human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs). Clozapine is a potent dopamine (DA) antagonist and a selective muscarinic M4 receptor agonist.

S0457

DREADD agonist 21

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM.

S6795

VU0357017 Hydrochloride

VU0357017 hydrochloride (CID-25010775) is a potent, highly selective and CNS-penetrant agonist of M1 which is a subtype of muscarinic acetylcholine receptors (mAChRs). VU0357017 hydrochloride appears to act at an allosteric site to activate the receptor with EC50 of 477 nM and Ki of 9.91 μM.

S0552

BNC210

BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR).

S0782

VU0238441

VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively.

S0783

VU0119498

VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively.

S5931

BQCA

BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).

S5844

Lobelin sulphate

Lobelin sulphate (Lobeline sulfate, Bantron) is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, and smoking cessation.

S2646

VU0238429

VU0238429 (M5 PAM) is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4.

S4804

1-Naphthyl acetate

1-Naphthyl acetate is usually used in a rapid staining method for identification of macrophages. 1-Naphthyl acetate is a potent chromogenic substrate for the detection of erythrocyte acetylcholinesterase (AChE) activity.

Catalog No. Information Product Use Citations Product Validations
S3245

Nodakenetin

Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.

S9219

Huperzine B

Huperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects.

S5886

Hodostin

Hodostin (Neostigmine methyl sulfate, Syntostigmin, Neostigmeth) is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis.

S3913New

Pimethixene maleate

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.

S5022New

Varenicline Hydrochloride

Varenicline (CP 526555) Hydrochloride is a potent and selective inhibitor of nicotine acetylcholine receptor (nAChR) with Ki of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively.

S3311New

Myosmine

Myosmine is not only one of the minor tobacco alkaloids but is also present in various foods. Myosmine has low affinity against a4b2 nicotinic acetylcholinergic receptors (nAChR) with Ki of 3300 nM.

S3246

Picfeltarraenin IB

Picfeltarraenin IB, a cucurbitacin glycoside isolated from Picriafel-terrae, is an inhibitor of acetylcholinesterase (AChE). Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation.

S3820

Dehydroevodiamine hydrochloride

Dehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production.

S9252

Corydaline

Corydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers.

S0766

RHC 80267

RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC).

S9260

Nodakenin

Nodakenin ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM.

S9069

Jatrorrhizine chloride

Jatrorrhizine chloride (Neprotine, Yatrorhizine) is the hydrochloride salt form of jatrorrhizine, which is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.

S3884

Jatrorrhizine

Jatrorrhizine (Neprotin, Yatrorizine), one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE.

S3904

Isoimperatorin

Isoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. 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.

S9138

Picfeltarraenin IA

Picfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system.

S0016

SN-6

SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.

Catalog No. Information Product Use Citations Product Validations
S0032

Batefenterol 

Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively.

S6985New

Varenicline

Varenicline is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors.

S5777New

Ipratropium bromide monohydrate

Ipratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively.

S4713New

Atropine

Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.

S3298

Caulophylline (N-Methylcytisine)

Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.

Catalog No. Information Product Use Citations Product Validations
S0717

Varenicline (CP 526555) dihydrochloride

Varenicline (CP 526555, Chantix, Champix) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.

S9789New

JHU37152

JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

S9790New

JHU37160

JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

S7366

LY2119620

LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.

S6887

Clozapine N-oxide

Clozapine N-oxide (CNO) is a metabolite of Clozapine (GLXC-06516) and an agonist of human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs). Clozapine is a potent dopamine (DA) antagonist and a selective muscarinic M4 receptor agonist.

S0457

DREADD agonist 21

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM.

S6795

VU0357017 Hydrochloride

VU0357017 hydrochloride (CID-25010775) is a potent, highly selective and CNS-penetrant agonist of M1 which is a subtype of muscarinic acetylcholine receptors (mAChRs). VU0357017 hydrochloride appears to act at an allosteric site to activate the receptor with EC50 of 477 nM and Ki of 9.91 μM.

Catalog No. Information Product Use Citations Product Validations
S0552

BNC210

BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR).

S0782

VU0238441

VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively.

S0783

VU0119498

VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively.

S5931

BQCA

BQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).

S5844

Lobelin sulphate

Lobelin sulphate (Lobeline sulfate, Bantron) is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, and smoking cessation.

S2646

VU0238429

VU0238429 (M5 PAM) is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4.

Catalog No. Information Product Use Citations Product Validations
S4804

1-Naphthyl acetate

1-Naphthyl acetate is usually used in a rapid staining method for identification of macrophages. 1-Naphthyl acetate is a potent chromogenic substrate for the detection of erythrocyte acetylcholinesterase (AChE) activity.