AChR
Isoform-specific Inhibitors
AChR Products
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S2462 |
Donepezil HClDonepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively. |
![]() ![]() Donepezil-mediated eACh activity in vitro. After being cultured in serum-free EBM-2, HUVECs were treated with donepezil at a concentration of 10 umol/L for 24 hours. E and F: Representative images (x 400 magnification) of anti-ChAT and -VAChT immunofluorescence. Scale bar: 50 um. ChAT indicates choline acetyltransferase; eACh, endothelium-derived acetylcholine; EBM-2, endothelial basal medium 2; HUVECs, human umbilical vein endothelial cells; PCR, polymerase chain reaction; VAChT, vesicular acetylcholine transporter.
|
|
S2251 |
(-)-Huperzine A (HupA)(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4. |
||
S3311New |
MyosmineMyosmine 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. |
||
S3245New |
NodakenetinNodakenetin (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. |
||
S3246New |
Picfeltarraenin IBPicfeltarraenin 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. |
||
S0766New |
RHC 80267RHC 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). |
||
S2452 |
Amfebutamone (Bupropion) HClAmfebutamone (Bupropion) HCl is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively. |
||
S1339 |
Galanthamine HBrGalanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. |
||
S4031 |
Aclidinium BromideAclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively. |
||
S1397 |
Rocuronium BromideRocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia. |
||
S3047 |
Otilonium BromideOtilonium bromide is an antimuscarinic. |
||
S2471 |
Gallamine TriethiodideGallamine Triethiodide is a cholinergic receptor blocker with an IC50 of 68.0 ± 8.4 μM. |
||
S1608 |
Pyridostigmine BromidePyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor. |
![]() ![]() Acetylcholine (ACh)-related protein expression in vivo. Choline acetyltransferase (ChAT) in the ischemic area were determined among 3 experimental groups. Data of Western blotting are represented as fold of control. |
|
S2087 |
Rivastigmine TartrateRivastigmine Tartrate (ENA 713) is a cholinesterase inhibitor with IC50 of 5.5 μM, and used as a parasympathomimetic or cholinergic agent for the treatment of mild to moderate Alzheimer disease. |
||
S1929 |
IrsogladineIrsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. |
||
S2490 |
Neostigmine BromideNeostigmine Bromide is a reversible acetylcholinesterase inhibitor. |
||
S3202 |
CatharanthineCatharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM. |
||
S5073 |
DonepezilDonepezil (Aricept, Donepezilo) is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type. |
||
S4014 |
HyoscyamineHyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM. |
||
S9219 |
Huperzine BHuperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects. |
||
S5886 |
HodostinHodostin (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. |
||
S5385 |
ImidafenacinImidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3). |
||
S4023 |
Procaine HClProcaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM. |
![]() ![]() Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. *p<0.05, **p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
|
|
S3820 |
Dehydroevodiamine hydrochlorideDehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production. |
||
S5900 |
Edrophonium chlorideEdrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase. |
||
S9252 |
CorydalineCorydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers. |
||
S1832 |
Atracurium BesylateAtracurium Besylate (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg. |
||
S9260 |
NodakeninNodakenin ((+)-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. |
||
S3835 |
LoganinLoganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively. |
||
S4619 |
Itopride hydrochlorideItopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM. |
||
S4162 |
Benzethonium ChlorideBenzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively. |
||
S3639 |
Tacrine hydrochloride hydrateTacrine (Tetrahydroaminacrine, Tetrahydroaminoacridine) is a centerally active cholinesterase inhibitor that has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. It also acts as a histamine N-methyltransferase inhibitor. |
||
S3662 |
Pirenzepine dihydrochloridePirenzepine is an antimuscarinic agent which inhibits gastric acid secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular and urinary functions. |
||
S3769 |
PalmatinePalmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities. |
||
S9069 |
Jatrorrhizine chlorideJatrorrhizine 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. |
||
S3788 |
CarvacrolCarvacrol (Cymophenol), monoterpenic phenol isomeric with thymol, has diverse activities such as antimicrobial, antitumor, an-timutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet, AChE inhibitory, antielastase, insecticidal, antihepatotoxic and hepatoprotective activities. |
||
S9087 |
TenuifolinTenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
||
S3884 |
JatrorrhizineJatrorrhizine (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. |
||
S4505 |
Vinblastine sulfateVinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis. |
||
S5075 |
AcotiamideAcotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties. |
||
S4357 |
Tacrine HClTacrine is a centrally acting anticholinesterase and indirect cholinergic agonist. Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively. |
||
S4687 |
RivastigmineRivastigmine (SDZ-ENA 713, Exelon) is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM). |
||
S4776 |
HarmalineHarmaline, a natural occurrence β-carboline alkaloid, is a central nervous system stimulant and an acetylcholinesterase (AChR) inhibitor; also inhibits histamine N-methyltransferase. |
||
S3903 |
LycorineLycorine (Galanthidine, Amarylline, Narcissine, Licorine, Belamarine) is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis. |
||
S3904 |
IsoimperatorinIsoimperatorin, 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 IAPicfeltarraenin 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. |
||
S4542 |
Trihexyphenidyl hydrochlorideTrihexyphenidyl hydrochloride (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class. |
||
S5511 |
Ethyl (triphenylphosphoranylidene) acetateEthyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE. |
||
S2082 |
Adiphenine HClAdiphenine HCl is a nicotinic receptor inhibitor, used as an antispasmodic drug. |
||
S5424 |
CarbarylCarbaryl (1-naphthyl methylcarbamate) is a carbamate insecticide and parasiticide and also a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. |
||
S0016 |
SN-6SN-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. |
||
S9154 |
ChelidonineChelidonine (Stylophorin, Helidonine), a major bioactive, isoquinoline alkaloid ingredient in Chelidonium majus, exhibits anti-inflammatory properties and acetylcholinesterase and butyrylcholinesterase inhibitory activity. |
||
S3866 |
GalanthamineGalantamine (Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders. |
||
S9560 |
Anisodamine HydrobromideAnisodamine (6-Hydroxyhyoscyamine) is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs). |
||
S4838 |
Acotiamide hydrochlorideAcotiamide Hydrochloride (YM-443, Z-338) is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. It is a new orally active selective acetylcholinesterase inhibitor. |
||
S9179 |
Catharanthine hemitartrateCatharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine. |
||
S5493 |
Atropine sulfateAtropine Sulfate (Sulfatropinol, Atropette, Tropintran) is the sulfate salt of atropine, which is a natural alkaloid anticholinergic agent and has potent antimuscarinic effects. |
||
S4389New |
Bephenium HydroxynaphthoateBephenium is an activator of B-type Acetylcholine receptor (AChR). Bephenium selectively activates the Hco-L-AChR1 subtype made of Hco-UNC-29.1, Hco-UNC-38, Hco-UNC-63, Hco-ACR-8 subunits. Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis. |
||
S4575 |
Pralidoxime chloridePralidoxime chloride (2-PAM) is an antidote to organophosphate pesticides and chemicals; An acetylcholinesterase (AChE) reactivator. |
||
S5100 |
Pralidoxime IodidePralidoxime Iodide (2-PAM) is an antidote approved for reactivation of inhibited acetylcholinesterase (AChE) in organophosphate poisoning. |
||
S2547 |
Tiotropium Bromide hydrateTiotropium Bromide hydrate (BA 679BR) is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist. |
||
S2497 |
Pancuronium dibromidePancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant. |
||
S4713New |
AtropineAtropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. |
||
S3298New |
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. |
||
S2550 |
Tolterodine tartrateTolterodine tartrate (PNU-200583E) is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist. |
||
S2240 |
Fesoterodine FumarateFesoterodine Fumarate (SPM 907) is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome. |
||
S1754 |
OxybutyninOxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties. |
||
S3048 |
Solifenacin succinateSolifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class. |
||
S1683 |
Ipratropium BromideIpratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD). |
||
S2549 |
Trospium chlorideTrospium chloride is a competitive muscarinic cholinergic receptor antagonist. |
||
S2130 |
Atropine sulfate monohydrateAtropine sulfate monohydrate is a competitive antagonist for the muscarinic acetylcholine receptor, used to decrease the production of saliva and secretions of the airway prior to surgery. |
||
S1978 |
MethscopolamineMethscopolamine is a muscarinic acetylcholine receptor blocker. |
||
S2508 |
Scopolamine HBrScopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
||
S2659 |
5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM. |
||
S3144 |
Darifenacin HBrDarifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. |
||
S5873 |
Scopolamine HBr trihydrateScopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
||
S4931 |
Propiverine hydrochloridePropiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence. Propiverine is a muscarinic receptor antagonist possessing additional properties, i.e., block of L-type Ca2+ channels. |
||
S0032 |
BatefenterolBatefenterol (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. |
||
S5480 |
Clidinium BromideClidinium Bromide is an anticholinergic drug. |
||
S4024 |
Homatropine MethylbromideHomatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively. |
||
S4025 |
Homatropine BromideHomatropine Bromide is an muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively. |
||
S4027 |
Flavoxate HClFlavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM. |
||
S5238 |
Solifenacin (YM905)Solifenacin (YM905) is a competitive muscarinic receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle. |
||
S5258 |
RevefenacinRevefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease. |
||
S2054 |
Orphenadrine CitrateOrphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects. |
||
S4034 |
Diphemanil MethylsulfateDiphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR). |
||
S4143 |
Pentoxyverine CitratePentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold. |
||
S3701 |
Benactyzine hydrochlorideBenactyzine hydrochloride is a centrally acting muscarinic antagonist. It is used as an antidepressant in the treatment of depression and associated anxiety. |
||
S5699 |
Scopolamine N-Oxide HydrobroMide MonohydrateScopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors. |
||
S4623 |
Methylbenactyzine BromideMethylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity. |
||
S4069 |
Hexamethonium DibromideHexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia. |
||
S4660 |
GlycopyrrolateGlycopyrrolate (Glycopyrronium, Robinul, Gastrodyn) is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics. |
||
S3735 |
Umeclidinium bromideUmeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). |
||
S5538 |
TropisetronTropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. |
||
S3117 |
Oxybutynin hydrochlorideOxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties. |
||
S4834 |
Propantheline bromidePropantheline bromide (Pro-Banthine, Neometantyl, Neopepulsan) is a muscarinic antagonist used to treat gastrointestinal conditions associated with intestinal spasm and to decrease secretions during anesthesia. |
||
S4992 |
NanofinNanofin (2,6-Dimethylpiperidine, Lupetidine, Naniopinum) is a ganglion blocker alkaloid having nicotinic acetylcholine receptor antagonist action. It has antihypertensive effect used for mild to moderate hypertension. |
||
S6469 |
ThonzylamineThonzylamine (Neohetramine) is an antihistamine and anticholinergic drug. |
||
S5921 |
Cyclopentolate HydrochlorideCyclopentolate is an antagonist of muscarinic acetylcholine receptors with Ki values of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively. |
||
S4292 |
Diphenidol HClDiphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo. |
||
S1913 |
TropicamideTropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM. |
||
S1356 |
LevetiracetamLevetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy. Levetiracetam (UCB-L059, SIB-S1) is an agonist of muscarinic acetylcholine receptors (mAChR). Levetiracetam modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel. |
![]() ![]() Levetiracetam reduces DNA, synaptic, and neurite damage caused by Dox. (A) An example of cortical cultures pre-treated with 5 μ M Lev and then Dox (0.01 μ M, overnight), fixed and stained with antibodies against MAP2c. Scale bar is 20 μ m. (B) Cortical neurons at 28–32 DIV were pre-treated with 5 μ M Lev, and then a vehicle or with Dox (0.01 μ M for 3 days, or 0.1 μ M, overnight) was added. Neurons were fixed, and stained for MAP2c, synapsin, and with the Hoechst dye, and imaged. Note that red MAP2c staining also includes Dox's red fluorescence. (C) Synaptically developed primary cortical cultures at 28−32 DIV were pretreated with 5 mM Lev, and then a vehicle or with Dox (0.01 μM for 3 days, or 0.1 μM, overnight) was added. Neurons were then fixed, and stained with antibodies against γH2A.X and MAP2c, and with the Hoechst dye. Blue staining was used by the algorithm to identify and analyze γH2A.X.
|
|
S6887New |
Clozapine N-oxideClozapine 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. |
||
S0457New |
DREADD agonist 21DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM. |
||
S6795 |
VU0357017 HydrochlorideVU0357017 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. |
||
S1440 |
Varenicline TartrateVarenicline Tartrate (CP 526555-18) is a nicotinic AChR partial agonist, used to treat nicotine addiction. |
||
S2455 |
Bethanechol chlorideBethanechol chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors. |
||
S2614 |
Arecoline HBrArecoline is a muscarinic acetylcholine receptor agonist. |
![]() ![]() Arecoline affects expression of epithelial-mesenchymal transition-related genes in a dose-dependent manner. Expression of epithelial-mesenchymal transition-related genes (CK19, E-cadherin, N-cadherin and vimentin) in HaCaT cells was determined by western blotting and the results were quantified. Data shown are means ± SD, *P<0.05, **P<0.01, ***P<0.001. CK19, cytokeratin 19.
|
|
S4231 |
Pilocarpine HClPilocarpine HCl (NSC 5746) is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy. |
||
S4121 |
Succinylcholine Chloride DihydrateSuccinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker. |
||
S4422 |
NitenpyramNitenpyram is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets. |
||
S7366 |
LY2119620LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors. |
||
S2287 |
CytisineCytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist. |
||
S4171 |
Choline ChlorideCholine chloride is a quaternary ammonium salt used as an additive for animal feed. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism. |
||
S4072 |
Decamethonium BromideDecamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent. |
||
S6432 |
CevimelineCevimeline (AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3. |
||
S3684 |
Methacholine chlorideMethacholine (Mecholyl, Acetyl-β-methylcholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system but has little effects on the nicotinic receptors. |
||
S5930 |
PNU 282987 HClPNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor. |
||
S1805 |
Acetylcholine ChlorideThe chemical compound Acetylcholine Chloride is a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans. |
||
S4718 |
Acetylcholine iodideAcetylcholine iodide (Acetylcolina) is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system. |
||
S0782New |
VU0238441VU0238441 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. |
||
S0783New |
VU0119498VU0119498 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. |
||
S0552New |
BNC210BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR). |
||
S2646New |
VU0238429VU0238429 (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. |
||
S1351 |
IvermectinIvermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
||
S2629 |
PNU-120596PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM. |
![]() ![]() C) A summary: MCAO-induced infarct volumes were significantly smaller in treated vs. untreated animals: p=0.0147 (n=10; two-tailed, the Mann–Whitney U-test). The results are presented as mean+S.E.M. |
|
S3972 |
Lobeline hydrochlorideLobeline hydrochloride is an alkaloid that acts on nicotinic cholinergic receptors but is less potent than nicotine. It is also a VMAT2 ligand and an antagonist of μ-opioid receptors. |
||
S5931 |
BQCABQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR). |
||
S5844 |
Lobelin sulphateLobelin 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. |
||
S5747 |
Morantel tartrateMorantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs). |
||
S1405 |
Vecuronium BromideVecuronium Bromide (ORG NC45) is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery. |
||
S4804 |
1-Naphthyl acetate1-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. |
||
S4703 |
Choline bitartrateCholine bitartrate (2-hydroxyethyl(trimethyl)azanium, 2,3,4-trihydroxy-4-oxobutanoate) is a form of the nutrient choline which is found in foods. Choline is necessary for normal liver and kidney function and a component of the neurotransmitter acetylcholine, a chemical that facilitates communication between the nerves and muscles. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S2462 |
Donepezil HClDonepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively. |
![]() ![]() Donepezil-mediated eACh activity in vitro. After being cultured in serum-free EBM-2, HUVECs were treated with donepezil at a concentration of 10 umol/L for 24 hours. E and F: Representative images (x 400 magnification) of anti-ChAT and -VAChT immunofluorescence. Scale bar: 50 um. ChAT indicates choline acetyltransferase; eACh, endothelium-derived acetylcholine; EBM-2, endothelial basal medium 2; HUVECs, human umbilical vein endothelial cells; PCR, polymerase chain reaction; VAChT, vesicular acetylcholine transporter.
|
|
S2251 |
(-)-Huperzine A (HupA)(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4. |
||
S3311New |
MyosmineMyosmine 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. |
||
S3245New |
NodakenetinNodakenetin (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. |
||
S3246New |
Picfeltarraenin IBPicfeltarraenin 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. |
||
S0766New |
RHC 80267RHC 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). |
||
S2452 |
Amfebutamone (Bupropion) HClAmfebutamone (Bupropion) HCl is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively. |
||
S1339 |
Galanthamine HBrGalanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. |
||
S4031 |
Aclidinium BromideAclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively. |
||
S1397 |
Rocuronium BromideRocuronium Bromide (ORG 9426) is a competitive AchR antagonist, used in modern anaesthesia. |
||
S3047 |
Otilonium BromideOtilonium bromide is an antimuscarinic. |
||
S2471 |
Gallamine TriethiodideGallamine Triethiodide is a cholinergic receptor blocker with an IC50 of 68.0 ± 8.4 μM. |
||
S1608 |
Pyridostigmine BromidePyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor. |
![]() ![]() Acetylcholine (ACh)-related protein expression in vivo. Choline acetyltransferase (ChAT) in the ischemic area were determined among 3 experimental groups. Data of Western blotting are represented as fold of control. |
|
S2087 |
Rivastigmine TartrateRivastigmine Tartrate (ENA 713) is a cholinesterase inhibitor with IC50 of 5.5 μM, and used as a parasympathomimetic or cholinergic agent for the treatment of mild to moderate Alzheimer disease. |
||
S1929 |
IrsogladineIrsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. |
||
S2490 |
Neostigmine BromideNeostigmine Bromide is a reversible acetylcholinesterase inhibitor. |
||
S3202 |
CatharanthineCatharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM. |
||
S5073 |
DonepezilDonepezil (Aricept, Donepezilo) is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type. |
||
S4014 |
HyoscyamineHyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM. |
||
S9219 |
Huperzine BHuperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects. |
||
S5886 |
HodostinHodostin (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. |
||
S5385 |
ImidafenacinImidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3). |
||
S4023 |
Procaine HClProcaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM. |
![]() ![]() Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. *p<0.05, **p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
|
|
S3820 |
Dehydroevodiamine hydrochlorideDehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production. |
||
S5900 |
Edrophonium chlorideEdrophonium chloride is the chloride salt of edrophonium, which is a rapid-onset, short-acting, readily reversible inhibitor of acetylcholinesterase. |
||
S9252 |
CorydalineCorydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers. |
||
S1832 |
Atracurium BesylateAtracurium Besylate (BW 33A, 51W89) is a neuromuscular blocking agent with ED95 of 0.2 mg/kg. |
||
S9260 |
NodakeninNodakenin ((+)-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. |
||
S3835 |
LoganinLoganin (Loganoside) is an iridoid glycoside first isolated from the seeds of Strychnos nux-vomica, a member of the Loganiaceae family. It is a non-competitive inhibitor of BACE1 with IC50 of 47.97 μM an also inhibits AChE and BChE with IC50 values of 3.95 μM and 33.02 μM, respectively. |
||
S4619 |
Itopride hydrochlorideItopride hydrochloride (Ganaton, HSR803) is an AChE inhibitor. The IC50 of itopride with AChE is 2.04 +/- 0.27 μM. |
||
S4162 |
Benzethonium ChlorideBenzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively. |
||
S3639 |
Tacrine hydrochloride hydrateTacrine (Tetrahydroaminacrine, Tetrahydroaminoacridine) is a centerally active cholinesterase inhibitor that has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. It also acts as a histamine N-methyltransferase inhibitor. |
||
S3662 |
Pirenzepine dihydrochloridePirenzepine is an antimuscarinic agent which inhibits gastric acid secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular and urinary functions. |
||
S3769 |
PalmatinePalmatine (Berbericinine, Burasaine), an isoquinoline alkaloid, has sedative, antidepressant, antioxidative, anti-ulcerative, antacid, anticancer, and anti-metastatic activities. |
||
S9069 |
Jatrorrhizine chlorideJatrorrhizine 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. |
||
S3788 |
CarvacrolCarvacrol (Cymophenol), monoterpenic phenol isomeric with thymol, has diverse activities such as antimicrobial, antitumor, an-timutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet, AChE inhibitory, antielastase, insecticidal, antihepatotoxic and hepatoprotective activities. |
||
S9087 |
TenuifolinTenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
||
S3884 |
JatrorrhizineJatrorrhizine (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. |
||
S4505 |
Vinblastine sulfateVinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis. |
||
S5075 |
AcotiamideAcotiamide (Acofide, Z388) is a novel acetylcholinesterase inhibitor with fundus-relaxing and gastroprokinetic properties. |
||
S4357 |
Tacrine HClTacrine is a centrally acting anticholinesterase and indirect cholinergic agonist. Tacrine hydrochloride hydrate is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively. |
||
S4687 |
RivastigmineRivastigmine (SDZ-ENA 713, Exelon) is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM). |
||
S4776 |
HarmalineHarmaline, a natural occurrence β-carboline alkaloid, is a central nervous system stimulant and an acetylcholinesterase (AChR) inhibitor; also inhibits histamine N-methyltransferase. |
||
S3903 |
LycorineLycorine (Galanthidine, Amarylline, Narcissine, Licorine, Belamarine) is a toxic crystalline alkaloid found in various Amaryllidaceae species that weakly inhibits acetylcholinesterase (AChE) and ascorbic acid biosynthesis. |
||
S3904 |
IsoimperatorinIsoimperatorin, 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 IAPicfeltarraenin 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. |
||
S4542 |
Trihexyphenidyl hydrochlorideTrihexyphenidyl hydrochloride (Benzhexol, Artane) is an antiparkinsonian agent of the antimuscarinic class. |
||
S5511 |
Ethyl (triphenylphosphoranylidene) acetateEthyl (triphenylphosphoranylidene) acetate (Triphenylcarbethoxymethylenephosphorane, (Carbethoxymethylene)triphenylphosphorane) may act as an inhibitor of cholinesterase that inhibits AChE and BChE. |
||
S2082 |
Adiphenine HClAdiphenine HCl is a nicotinic receptor inhibitor, used as an antispasmodic drug. |
||
S5424 |
CarbarylCarbaryl (1-naphthyl methylcarbamate) is a carbamate insecticide and parasiticide and also a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. |
||
S0016 |
SN-6SN-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. |
||
S9154 |
ChelidonineChelidonine (Stylophorin, Helidonine), a major bioactive, isoquinoline alkaloid ingredient in Chelidonium majus, exhibits anti-inflammatory properties and acetylcholinesterase and butyrylcholinesterase inhibitory activity. |
||
S3866 |
GalanthamineGalantamine (Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders. |
||
S9560 |
Anisodamine HydrobromideAnisodamine (6-Hydroxyhyoscyamine) is a naturally occurring atropine derivative and exhibits anti-inflammatory activity. It also inhibits α1-adrenergic receptors and muscarinic acetylcholine receptors (mAChRs). |
||
S4838 |
Acotiamide hydrochlorideAcotiamide Hydrochloride (YM-443, Z-338) is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. It is a new orally active selective acetylcholinesterase inhibitor. |
||
S9179 |
Catharanthine hemitartrateCatharanthine hemitartrate is the starting material for the synthesis of the antitumor drugs vinblastine and vincristine. |
||
S5493 |
Atropine sulfateAtropine Sulfate (Sulfatropinol, Atropette, Tropintran) is the sulfate salt of atropine, which is a natural alkaloid anticholinergic agent and has potent antimuscarinic effects. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S4389New |
Bephenium HydroxynaphthoateBephenium is an activator of B-type Acetylcholine receptor (AChR). Bephenium selectively activates the Hco-L-AChR1 subtype made of Hco-UNC-29.1, Hco-UNC-38, Hco-UNC-63, Hco-ACR-8 subunits. Bephenium hydroxynaphthoate is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis. |
||
S4575 |
Pralidoxime chloridePralidoxime chloride (2-PAM) is an antidote to organophosphate pesticides and chemicals; An acetylcholinesterase (AChE) reactivator. |
||
S5100 |
Pralidoxime IodidePralidoxime Iodide (2-PAM) is an antidote approved for reactivation of inhibited acetylcholinesterase (AChE) in organophosphate poisoning. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S2547 |
Tiotropium Bromide hydrateTiotropium Bromide hydrate (BA 679BR) is a monohydrate of tiotropium bromide (Spiriva; Tiova; BA 679BR; tiopropium) that is an anticholinergic and bronchodilator and a muscarinic receptor antagonist. |
||
S2497 |
Pancuronium dibromidePancuronium dibromide is a competitive nicotinic acetylcholine receptor antagonist, used as a muscle relaxant. |
||
S4713New |
AtropineAtropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. |
||
S3298New |
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. |
||
S2550 |
Tolterodine tartrateTolterodine tartrate (PNU-200583E) is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist. |
||
S2240 |
Fesoterodine FumarateFesoterodine Fumarate (SPM 907) is a prodrug of 5-hydroxymethyl tolterodine that is a muscarinic AChR receptor antagonist, used to treat overactive bladder syndrome. |
||
S1754 |
OxybutyninOxybutynin is a competitive antagonist of the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor, used to relieve urinary and bladder difficulties. |
||
S3048 |
Solifenacin succinateSolifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class. |
||
S1683 |
Ipratropium BromideIpratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD). |
||
S2549 |
Trospium chlorideTrospium chloride is a competitive muscarinic cholinergic receptor antagonist. |
||
S2130 |
Atropine sulfate monohydrateAtropine sulfate monohydrate is a competitive antagonist for the muscarinic acetylcholine receptor, used to decrease the production of saliva and secretions of the airway prior to surgery. |
||
S1978 |
MethscopolamineMethscopolamine is a muscarinic acetylcholine receptor blocker. |
||
S2508 |
Scopolamine HBrScopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
||
S2659 |
5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM. |
||
S3144 |
Darifenacin HBrDarifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. |
||
S5873 |
Scopolamine HBr trihydrateScopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM. |
||
S4931 |
Propiverine hydrochloridePropiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence. Propiverine is a muscarinic receptor antagonist possessing additional properties, i.e., block of L-type Ca2+ channels. |
||
S0032 |
BatefenterolBatefenterol (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. |
||
S5480 |
Clidinium BromideClidinium Bromide is an anticholinergic drug. |
||
S4024 |
Homatropine MethylbromideHomatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively. |
||
S4025 |
Homatropine BromideHomatropine Bromide is an muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively. |
||
S4027 |
Flavoxate HClFlavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM. |
||
S5238 |
Solifenacin (YM905)Solifenacin (YM905) is a competitive muscarinic receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle. |
||
S5258 |
RevefenacinRevefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease. |
||
S2054 |
Orphenadrine CitrateOrphenadrine Citrate is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects. |
||
S4034 |
Diphemanil MethylsulfateDiphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR). |
||
S4143 |
Pentoxyverine CitratePentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold. |
||
S3701 |
Benactyzine hydrochlorideBenactyzine hydrochloride is a centrally acting muscarinic antagonist. It is used as an antidepressant in the treatment of depression and associated anxiety. |
||
S5699 |
Scopolamine N-Oxide HydrobroMide MonohydrateScopolamine N-Oxide (Hyoscine N-oxide, Genoscopolamine) is a muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors. |
||
S4623 |
Methylbenactyzine BromideMethylbenactyzine Bromide (Gastrimade, Noinarin, Paragone, Semulgin) is a kind of muscarinic cholinergic receptor antagonist with antispasmodic activity. |
||
S4069 |
Hexamethonium DibromideHexamethonium Dibromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia. |
||
S4660 |
GlycopyrrolateGlycopyrrolate (Glycopyrronium, Robinul, Gastrodyn) is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics. |
||
S3735 |
Umeclidinium bromideUmeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). |
||
S5538 |
TropisetronTropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. |
||
S3117 |
Oxybutynin hydrochlorideOxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties. |
||
S4834 |
Propantheline bromidePropantheline bromide (Pro-Banthine, Neometantyl, Neopepulsan) is a muscarinic antagonist used to treat gastrointestinal conditions associated with intestinal spasm and to decrease secretions during anesthesia. |
||
S4992 |
NanofinNanofin (2,6-Dimethylpiperidine, Lupetidine, Naniopinum) is a ganglion blocker alkaloid having nicotinic acetylcholine receptor antagonist action. It has antihypertensive effect used for mild to moderate hypertension. |
||
S6469 |
ThonzylamineThonzylamine (Neohetramine) is an antihistamine and anticholinergic drug. |
||
S5921 |
Cyclopentolate HydrochlorideCyclopentolate is an antagonist of muscarinic acetylcholine receptors with Ki values of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively. |
||
S4292 |
Diphenidol HClDiphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo. |
||
S1913 |
TropicamideTropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S1356 |
LevetiracetamLevetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy. Levetiracetam (UCB-L059, SIB-S1) is an agonist of muscarinic acetylcholine receptors (mAChR). Levetiracetam modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel. |
![]() ![]() Levetiracetam reduces DNA, synaptic, and neurite damage caused by Dox. (A) An example of cortical cultures pre-treated with 5 μ M Lev and then Dox (0.01 μ M, overnight), fixed and stained with antibodies against MAP2c. Scale bar is 20 μ m. (B) Cortical neurons at 28–32 DIV were pre-treated with 5 μ M Lev, and then a vehicle or with Dox (0.01 μ M for 3 days, or 0.1 μ M, overnight) was added. Neurons were fixed, and stained for MAP2c, synapsin, and with the Hoechst dye, and imaged. Note that red MAP2c staining also includes Dox's red fluorescence. (C) Synaptically developed primary cortical cultures at 28−32 DIV were pretreated with 5 mM Lev, and then a vehicle or with Dox (0.01 μM for 3 days, or 0.1 μM, overnight) was added. Neurons were then fixed, and stained with antibodies against γH2A.X and MAP2c, and with the Hoechst dye. Blue staining was used by the algorithm to identify and analyze γH2A.X.
|
|
S6887New |
Clozapine N-oxideClozapine 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. |
||
S0457New |
DREADD agonist 21DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM. |
||
S6795 |
VU0357017 HydrochlorideVU0357017 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. |
||
S1440 |
Varenicline TartrateVarenicline Tartrate (CP 526555-18) is a nicotinic AChR partial agonist, used to treat nicotine addiction. |
||
S2455 |
Bethanechol chlorideBethanechol chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors. |
||
S2614 |
Arecoline HBrArecoline is a muscarinic acetylcholine receptor agonist. |
![]() ![]() Arecoline affects expression of epithelial-mesenchymal transition-related genes in a dose-dependent manner. Expression of epithelial-mesenchymal transition-related genes (CK19, E-cadherin, N-cadherin and vimentin) in HaCaT cells was determined by western blotting and the results were quantified. Data shown are means ± SD, *P<0.05, **P<0.01, ***P<0.001. CK19, cytokeratin 19.
|
|
S4231 |
Pilocarpine HClPilocarpine HCl (NSC 5746) is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy. |
||
S4121 |
Succinylcholine Chloride DihydrateSuccinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker. |
||
S4422 |
NitenpyramNitenpyram is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets. |
||
S7366 |
LY2119620LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors. |
||
S2287 |
CytisineCytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist. |
||
S4171 |
Choline ChlorideCholine chloride is a quaternary ammonium salt used as an additive for animal feed. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism. |
||
S4072 |
Decamethonium BromideDecamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent. |
||
S6432 |
CevimelineCevimeline (AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3. |
||
S3684 |
Methacholine chlorideMethacholine (Mecholyl, Acetyl-β-methylcholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system but has little effects on the nicotinic receptors. |
||
S5930 |
PNU 282987 HClPNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor. |
||
S1805 |
Acetylcholine ChlorideThe chemical compound Acetylcholine Chloride is a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans. |
||
S4718 |
Acetylcholine iodideAcetylcholine iodide (Acetylcolina) is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S0782New |
VU0238441VU0238441 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. |
||
S0783New |
VU0119498VU0119498 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. |
||
S0552New |
BNC210BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR). |
||
S2646New |
VU0238429VU0238429 (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. |
||
S1351 |
IvermectinIvermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
||
S2629 |
PNU-120596PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM. |
![]() ![]() C) A summary: MCAO-induced infarct volumes were significantly smaller in treated vs. untreated animals: p=0.0147 (n=10; two-tailed, the Mann–Whitney U-test). The results are presented as mean+S.E.M. |
|
S3972 |
Lobeline hydrochlorideLobeline hydrochloride is an alkaloid that acts on nicotinic cholinergic receptors but is less potent than nicotine. It is also a VMAT2 ligand and an antagonist of μ-opioid receptors. |
||
S5931 |
BQCABQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR). |
||
S5844 |
Lobelin sulphateLobelin 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. |
||
S5747 |
Morantel tartrateMorantel (CP-12009-18, UK 296418) is a positive allosteric modulator of neuronal nicotinic acetylcholine receptors (nAChRs). |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S1405 |
Vecuronium BromideVecuronium Bromide (ORG NC45) is a non-depolarizing neuromuscular blocking agent, used for skeletal muscle relaxation during surgery. |
||
S4804 |
1-Naphthyl acetate1-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. |
||
S4703 |
Choline bitartrateCholine bitartrate (2-hydroxyethyl(trimethyl)azanium, 2,3,4-trihydroxy-4-oxobutanoate) is a form of the nutrient choline which is found in foods. Choline is necessary for normal liver and kidney function and a component of the neurotransmitter acetylcholine, a chemical that facilitates communication between the nerves and muscles. |