AChR

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.

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.

beta-Amyrone (β-Amyron) has antifungal activity against Chikungunya virus replication with an EC50 of 86 uM. beta-Amyrone has anti-inflammatory activity through inhibiting the expression of COX-2. beta-Amyrone exhibits anti-α-glucosidase inhibitory activity and moderate AChE activity. β-Amyrone can be used in the research of disease like inflammation, infection, and obesity.

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

Anisodine is an inhibitor of muscarinic acetylcholine receptors (mAChR) with neuroprotective activity, used in research on multiple myeloma and metastatic breast cancer.

Tematropium (CDDD3602) possesses anticholinergic effects and can be used in neurological studies.

AF-710B is a specific variant of M1 muscarinic and Sigma-1 receptor agonist used in the study of neurological disorders such as Alzheimer's disease dementia and schizophrenia.

Sulfoxaflor (GF 2032) is an agonist of nAChR1 and nAChR2 subtypes and a systemic insecticide that acts on the insect central nervous system. Sulfoxaflor was found to have some effects on peripheral blood lymphocytes and is used to control sap-feeding insects such as brown planthopper, whitefly, peach aphid, and cotton aphid.

Xanomeline (LY-246708) is a functionally selective M1 M4 activator used in the study of neurological disorders such as schizophrenia and has shown promising treatment in preclinical trials. Xanomeline is well absorbed orally, crosses the blood-brain barrier and undergoes extensive liver metabolism with at least six metabolites.

Physostigmine, a parasympathomimetic alkaloid, is a reversible cholinesterase inhibitor. It extracts from the Calabar bean.

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.

PF-4348235 HCl (β2AR M-receptor agonist-2 HCl) is a muscarinic M3 receptor antagonist (Ki: 0.73 nM) and β2 adrenergic receptor agonist (MABA, EC50: 3.7 nM). PF-4348235 HCl is also a bronchial BM213 acetate is a bronchodilator used to study cardiovascular and respiratory diseases such as chronic obstructive pulmonary disease (COPD).

Ethoxysanguinarine (6-Ethoxydihydrosanguinarine) shows human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity, with IC50 values of 0.83 + - 0.04 microM and 4.20 + - 0.19 microM, respectively.

3-Bromocytisine ((-)-3-Bromocytisine) is an effective agonist of nAChR (IC50s: 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7).

ICL-CCIC-0019, an inhibitor of choline kinase alpha (ChoKα), induces G1 arrest, endoplasmic reticulum stress, and apoptosis in cancer cell lines.

Fesoterodine ((R) Fesoterodine) is an orally active, competitive mAChR antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. It is used for the overactive bladder (OAB).

Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.

α-Conotoxin GI acetate is a competitive antagonist of the muscle-type nicotinic acetylcholine receptors (nAChR).

V-11-0711 HCl is a selective and highly effective choline kinase α (ChoKα) inhibitor that inhibits the catalytic activity of Chk.

Darifenacin (UK-88525) is a muscarinic receptor M3 antagonist with anticonvulsant activity and can be used to study urinary incontinence and overactive bladder.

Desformylflustrabromine hydrochloride (dFBr hydrochloride) is a selective agonist of nicotinic acetylcholine receptor (nAChR) in α4β2 neurons, with pEC50 of 6.48.

Methyllycaconitine citrate (MLA) is an α7 neuronal nicotinic acetylcholine receptor (α7nAChR) antagonist that crosses the blood-brain barrier.

VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (M4 mAChR).

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.

Emraclidine (CVL-231) is a novel, highly selective allosteric modulator of the muscarinic M4 receptor positive receptor for the study of neurological diseases.

PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).

Monepantel (AAD1566) is an organic anthelmintic and nicotinic acetylcholine receptor antagonist from roundworms and esophagostomies that is widely used for de-worming in agriculture and livestock.

SCH-900271 is a potent nicotinic acid receptor for the treatment of dyslipidaemia and is commonly used in the study of mixed hyperlipidaemia and primary hypercholesterolaemia.

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

Vinblastine sulfate (Vincaleukoblastine sulfate salt) can inhibit the formation of microtubule, it also inhibits nAChR(IC50=8.9 uM).

Simpinicline (OC-02) (OC-02) is a highly selective nicotinic acetylcholine receptor (nAChR) agonist that activates the trigeminal parasympathetic pathway and can be used to treat dry eye.

Gnetol competitivity inhibits butyrylcholinesterase (IC50: 1.3 uM). Gnetol has a strong inhibitory effect on murine tyrosinase activity. Gnetol significantly suppresses melanin biosynthesis in murine B16 melanoma cells. It is active in the inhibition of a

Afacifenacin (SMP-986) fumarate is an M3 muscarinic receptor-selective antagonist used in the study of ischemic heart disease, urinary incontinence and cystitis and other disorders.

Asoxime dichloride (Tert-Butyl2-(2-hydroxyethyl)-1-pyrrolidinecarboxylate) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system. Asoxime dichloride involves in modulating immunity response.

Epiberberine chloride, a natural pro-berberine from Coptis chinensis Franch. is an AChE, BChE, and BACE1 inhibitor with IC50 values of 1.07, 6.03, and 8.55 μM, respectively.Epiberberine chloride has antioxidant effects and inhibits the effects of Ca9-22 and Fa2R. Epiberberine chloride has antioxidant effects, inhibits the motility of Ca9-22 and FaDu cell lines, and can be used to study hyperlipidemia, Alzheimer's disease and diabetes.

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

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.

9-Cyclopentyladenine (NSC-19486) is an adenylate cyclase inhibitor that blocks cellular morphological differentiation and phosphorylation of specific signaling molecules.

Acetylcholine Chloride is the chloride salt form of acetylcholine, a synthetic, quaternary amino alcohol with cholinergic properties. Acetylcholine chloride (Pilofrin) mimics the parasympathomimetic effect of the endogenous compound acetylcholine. Administered as an ophthalmic solution, this drug stimulates the cholinoceptors in the sphincter muscle of the iris, causing the pupil to constrict.

(Rac)-ABT-202 dihydrochloride is a racemate of ABT-202, a nicotinic acetylcholine receptor (nAChRs) agonist used as an analgesic.

Cotinine (NIH-10498) is an alkaloid found in tobacco and is also the predominant metabolite of nicotine.

Cytisinicline (Sophorine), an alkaloid, is found naturally in several plants.

GTS-21 dihydrochloride (DMBX-anabaseine) is a nAChRs agonist. nAChRs are neuron receptor proteins that activated by the binding of the neurotransmitter ACh.

nAChR agonist 1 (DUN71755) is a brain-permeable and orally efficacious positive allosteric α7 nicotinic acetylcholine receptor (α7 nAChR)modulator.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Anabasine ((S)-Anabasine) is an alkaloid extracted from tobacco, acting as a full agonist of nicotinic acetylcholine receptors (nAChRs) with insecticidal activity. It depolarizes TE671 cells that endogenously express human myotypic nAChRs.

TAK-071 is a potent, novel and highly selective modulator of muscarinic acetylcholine receptor 1 (M1R) positive allosteric(EC50 : 520 nM).

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.