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AChR

An acetylcholine receptor (abbreviated AChR) is an integral membrane protein that responds to the binding of acetylcholine, a neurotransmitter.

  • (+)-Sparteine
    T7853492-08-0
    (+)-Sparteine (Pachycarpine) is a natural product extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent
    • $42
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  • Forskolin
    T293966575-29-9
    Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.
    • $36
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  • Polygalacic acid
    T376722338-71-2
    Polygalacic acid (Virgaureagenin G)(PA) significantly improves cholinergic system reactivity, as indicated by decreased acetylcholinesterase (AChE) activity, increases choline acetyltransferase (ChAT) activity, and elevates levels of acetylcholine (ACh) in the hippocampus and frontal cortex, PA also significantly ameliorates neuroinflammation and oxidative stress in mice; suggest that PA might exert a significant neuroprotective effect on cognitive impairment, driven in part by the modulation of cholinergic activity and neuroinflammation. Polygalacic acid shows significant postingestive effects on Spodoptera littoralis larvae.
    • $91
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  • CLOZAPINE N-OXIDE
    T449434233-69-7
    Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.
    • $30
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  • Pilocarpine Hydrochloride
    T080454-71-7
    Pilocarpine Hydrochloride (NSC 5746 HCl) , a nonselective muscarinic acetylcholine receptor agonist, is utilized to produce an experimental model of epilepsy.
    • $54
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  • Procainamide hydrochloride
    T0018614-39-1
    Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.
    • $41
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  • Propoxur
    T0976114-26-1
    Propoxur (Propoxure) is an insecticide used to control cockroaches, flies, mosquitoes, and lawn and turf insects. Acute (short-term) exposure of humans to propoxur by ingestion leads to cholinesterase inhibition of red blood cells, with mild cholinergic symptoms including blurred vision, nausea, vomiting, sweating, and tachycardia; however, the effects are transient. Chronic (long-term) inhalation exposure has resulted in depressed cholinesterase levels, headaches, vomiting, and nausea in humans. Chronic ingestion studies in animals have reported depressed cholinesterase levels, depressed body weight, effects to the liver and bladder, and a slight increase in neuropathy. No information is available on the reproductive, developmental, or carcinogenic effects of propoxur in humans. Mixed results are available from cancer studies of propoxur in animals. EPA has not classified propoxur for carcinogenicity.
    • $51
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  • Sulindac sulfide
    T1303749627-27-2In house
    Sulindac sulfide (cis-Sulindac sulfide) is a non-steroidal anti-inflammatory compound that has a high affinity for COX-1 and acts as an inhibitor in Ras activation of Raf-1. Sulindac sulfide is a non-competitive inhibitor of gamma-secretase with an IC50 value of 20.2 μM. It is an active metabolite of sulinic acid.
    • $31
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  • Ribavirin
    T068436791-04-5
    Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.
    • $39
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  • Methacholine Chloride
    T168262-51-1
    Methacholine Chloride (Acetyl-β-methylcholine chloride) is a quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma.
    • $59
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  • L-Hyoscyamine sulfate
    T4S1619620-61-1
    L-Hyoscyamine sulfate (Levsin Sulfate) is the sulfate salt of a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. Hyoscyamine functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.
    • $41
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  • Anisodamine Hydrobromide
    T830455449-49-5
    Anisodamine Hydrobromide (6-Hydroxyhyoscyamine) is an anticholinergic and α1-adrenergic receptor antagonist used in the treatment of acute circulatory shock.
    • $66
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  • Pilocarpine nitrate
    T1231148-72-1
    Pilocarpine nitrate (Pilagan) is a slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
    • $41
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  • Irsogladine
    T654857381-26-7
    Irsogladine (Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
    • $29
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  • Choline chloride
    T103967-48-1
    Choline chloride (Biocoline) is a basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.
    • $33
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  • Cholesterol myristate
    T80401989-52-2
    Cholesterol Myristate (Cholesteryl Myristate) is a natural steroid found in traditional Chinese medicine that interacts with various ion channels, including the GABAA receptor, nicotinic acetylcholine receptor, and the inward-rectifier potassium ion channel.
    • $30
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  • Adiphenine hydrochloride
    T007250-42-0
    Adiphenine hydrochloride (Patrovina), a nicotinic receptor inhibitor, can be used as an antispasmodic drug.
    • $39
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  • Arecoline hydrobromide
    T2198300-08-3
    Arecoline hydrobromide (Arecoline HBr) is a muscarinic acetylcholine receptor agonist.
    • $50
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  • Blarcamesine
    T7780195615-83-9
    Blarcamesine (AVex-73) is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease.
    • $40
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  • 8-Aminoadenine
    T2201328128-33-8
    8-Aminoadenine (7H-purine-6,8-diamine) is a ligand for Adenine Receptor with Ki of 0.0341 μM.
    • $37
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  • ICL-CCIC-0019
    T27579936498-64-5In house
    ICL-CCIC-0019 is an inhibitor of choline kinase alpha (ChoKα). ICL-CCIC-0019 induces G1 arrest, endoplasmic reticulum stress, and apoptosis of cancer cell lines.
    • $195
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  • Catharanthine sulfate
    T302370674-90-7
    Catharanthine inhibits nicotinic receptor-mediated diaphragm contractions.
    • $50
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  • Pimethixene
    T12489314-03-4
    Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).
    • $35
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  • Terodiline
    T6053615793-40-5In house
    Terodiline is a seconal amine with anticholinergic and calcium antagonistic properties that blocks the hERG current (IC50: 375 nM).Terodiline is cardiotoxic and has been used in the study of disorders caused by urethral muscle instability.
    • $293 TargetMol
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  • Darenzepine
    T1096184629-61-8In house
    Darenzepine is a muscarinic receptor inhibitor.
    • $226
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  • TZ3O
    T776782218754-19-7
    TZ3O is an anticholinergic compound with neuroprotective activity.TZ3O ameliorates memory impairment and cognitive decay in Scopolamine-induced Alzheimer's type model in rats, and can be used in the study of Alzheimer's disease.
    • $195
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  • Cyclodrine
    T10914L52109-93-0In house
    Cyclodrine (Cyclopent) is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.
    • $117
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  • (-)-OPC-51803
    T28257L192514-57-1In house
    (-)-OPC-51803 is an antidiuretic hormone V2 receptor agonist used in the treatment of nocturia and urinary incontinence.
    • $195
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  • DMAB-anabaseine dihydrochloride
    T22735154149-38-9
    DMAB-anabaseine dihydrochloride (N,N-dimethyl-4-[(E)-(6-pyridin-3-yl-3,4-dihydro-2H-pyridin-5-ylidene)methyl]aniline;dihydrochloride) is an α7-containing neuronal nicotinic receptor partial agonist and an antagonist at α4β2 and other nicotinic receptors.
    • $94
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  • Dimethindene
    T314885636-83-9In house
    Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.
    • $117
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  • YM-58790
    T72038168830-70-4In house
    YM-58790 free base is a potent mAChR antagonist.YM-58790 free base inhibited M1 mAChR, M2 mAChR, and M3 mAChR with Ki values of 28 nM, 260 nM, and 15 nM, respectively.YM-58790 free base inhibits reflex rhythmic bladder contraction in rats by inhibiting bladder pressurization. YM-58790 free base inhibits reflex rhythmic bladder contractions in rats by inhibiting bladder pressurization.
    • $147
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  • SCH 57790
    T28722221660-80-6In house
    SCH 57790 is a novel and selective muscarinic M(2) receptor antagonist that releases acetylcholine and enhances cognition in experimental animals for the treatment of Alzheimer's disease.
    • $258
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  • (-)-Coclaurine hydrochloride
    TN1519L3422-42-2
    (-)-Coclaurine hydrochloride is an antagonist of nAChRs isolated from Sarcopetalum harveyanum.
    • $195
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  • α-Conotoxin MII acetate
    TP2063L
    α-Conotoxin MII acetate is a 16-amino acid peptide from the venom of the marine snail Conus magus. α-Conotoxin MII acetate potently blocks nicotinic acetylcholine receptors composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII acetate potently blocks β3-containing neuronal nicotinic acetylcholine receptors.
    • $148
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  • Lobelanidine
    T32832552-72-7
    Lobelanidine (8,10-Diphenyllobelidiol), which can be extracted from the above-ground parts of Lobelia chinensis Lour and Lobelia tupa, is an analogue of lobeline and shows a moderate affinity for nAChR.
    • $350
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  • Glutathione arsenoxide hydrochloride
    T27417L In house
    Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) is a potentially active anti-cancer molecule and inhibitor of tumour metabolism. glutathione arsenoxide hydrochloride targets the mitochondrial inner membrane adenine nucleotidyl transferase (ANT), which inhibits cell proliferation and promotes apoptosis. Glutathione arsenoxide hydrochloride can be used to recognize cell surface proteins such as protein disulfide isomerases.
    • $350
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  • PF-03635659
    T33941931409-24-4In house
    PF-03635659 is a potent and long dissociative half-life muscarinic M3 antagonist (Ki: 0.2 nM) that shows potential for the treatment of chronic obstructive pulmonary disease (COPD).
    • $240
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  • S16961
    T12820153874-14-7In house
    S16961 (S169611) is an agonist of nicotinic receptor.
    • $43
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  • SSR 180
    T84293298198-52-4In house
    SSR 180 is a potent and subtype-selective α7 agonist with applications in the study of Alzheimer;s disease and schizophrenia.
    • $195 TargetMol
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  • (Rac)-VU 6008667
    T126792092917-63-8
    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) with IC50 of 1.8 μM and pIC50 of 5.75, has high CNS penetration.
    • $54
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  • SIB 1553A
    T16881L191611-76-4In house
    SIB 1553A is an orally available and selective agonist of nicotinic acetylcholine receptors (nAChRs), which are subtype-selective ligands for nicotinic acetylcholine receptors.SIB-1553A is a cognitive enhancer that may be used in the study of neurodegenerative-related diseases such as Alzheimer's disease.
    • $195
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  • GSK233705
    T31207850607-58-8In house
    GSK233705 (Darotropium bromide) is a muscarinic receptor antagonist used in conjunction with the prevention and treatment of chronic obstructive pulmonary disease (COPD) and asthma in humans.
    • $130
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  • A 582941 HCl (848591-90-2(free base))
    T8725
    A-582941 is a alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties
    • $133
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  • Orphenadrine
    T6859983-98-7In house
    Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.
    • $52
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  • LY2033298
    T27931886047-13-8
    LY2033298, a positive allosteric modulator of muscarine M4 receptor, enhances the inhibitory effect of oximoline on light-induced phase shift in circadian activity in hamsters and can be used in neurosystem-related diseases.
    • $89
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  • Oxyphencyclimine Hydrochloride
    T2138125-52-0
    Oxyphencyclimine Hydrochloride (Ulcociclinina) is a synthetic tertiary amine and antimuscarinic agent with antispasmodic and antisecretory activities.
    • $48
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  • GAT107
    T274041476807-74-5In house
    GAT107 is a novel and potent α7 nicotinic cholinergic receptor modifier agonist and modulator with anti-inflammatory activity that reverses injury perception in a mouse model of neuropathic pain.
    • $258
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  • ASM-024
    T266661609534-88-4In house
    ASM-024, a potent nicotinic receptor agonist, is a small molecule synthetic piperazine compound that promotes different targets and signaling pathways of β2-adrenergic receptors mediating smooth muscle relaxation, and is a potential compound for the treatment of asthma and chronic obstructive bronchitis with anti-inflammatory activity.
    • $258
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  • CP-810123
    T31079439608-12-5In house
    CP-810123 is a new alpha 7 nAChR agonist for the treatment of cognitive impairment associated with psychiatric or neurological disorders such as schizophrenia and Alzheimer's disease.
    • $293 TargetMol
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  • JNJ-39393406
    T27679953428-73-4In house
    JNJ-39393406 is an α7 nicotinic acetylcholine receptor positive allosteric modulator for the study of tobacco dependence and Alzheimer's disease.
    • $146
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