AChR

(+)-Sparteine (Pachycarpine) is a natural product extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent

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.

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.

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.

Pilocarpine Hydrochloride (NSC 5746 HCl) , a nonselective muscarinic acetylcholine receptor agonist, is utilized to produce an experimental model of epilepsy.

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.

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.

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.

Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.

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.

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.

Anisodamine Hydrobromide (6-Hydroxyhyoscyamine) is an anticholinergic and α1-adrenergic receptor antagonist used in the treatment of acute circulatory shock.

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.

Irsogladine (Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.

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.

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.

Adiphenine hydrochloride (Patrovina), a nicotinic receptor inhibitor, can be used as an antispasmodic drug.

Arecoline hydrobromide (Arecoline HBr) is a muscarinic acetylcholine receptor agonist.

8-Aminoadenine (7H-purine-6,8-diamine) is a ligand for Adenine Receptor with Ki of 0.0341 μM.

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.

Catharanthine inhibits nicotinic receptor-mediated diaphragm contractions.

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).

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.

Cyclodrine (Cyclopent) is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.

(-)-OPC-51803 is an antidiuretic hormone V2 receptor agonist used in the treatment of nocturia and urinary incontinence.

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.

Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.

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.

Darenzepine is a muscarinic receptor inhibitor.

Blarcamesine (AVex-73) is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease.

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.

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.

(-)-Coclaurine hydrochloride is an antagonist of nAChRs isolated from Sarcopetalum harveyanum.

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.

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.

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.

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).

S16961 (S169611) is an agonist of nicotinic receptor.

SSR 180 is a potent and subtype-selective α7 agonist with applications in the study of Alzheimer;s disease and schizophrenia.

(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.

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.

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.

A-582941 is a alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties

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.

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.

Oxyphencyclimine Hydrochloride (Ulcociclinina) is a synthetic tertiary amine and antimuscarinic agent with antispasmodic and antisecretory activities.

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.

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.

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.

JNJ-39393406 is an α7 nicotinic acetylcholine receptor positive allosteric modulator for the study of tobacco dependence and Alzheimer's disease.