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.

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

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

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.

Harmalol (Harmidol) is a bioactive beta-carboline and a member of the harmala alkaloids

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.

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.

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

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).

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

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

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.

Mivacurium dichloride (Mivacurium chloride) is a non-depolarising, rapid neuromuscular blocker of short duration, used therefore as anesthetic, to provide skeletal muscle relaxation in minor surgical operations, in emergency surgical procedures of short to intermediate duration and during intubation of the trachea.

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.

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.

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.

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.

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.

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.

α-Conotoxin Vc1.1 TFA is a peptide isolated from Conus victoriae and a selective nAChR antagonist that inhibits α3α5β2, α3β2 and α3β4, reversing mechanical allodynia in neuropathic pain models and can be used to study neuropathic chronic pain. α-Conotoxin Vc1.1 TFA inhibits human dorsal root ganglion nerve excitability and mouse colon nociception via GABA(B) receptors.

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.

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

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

Ispronicline (TC-1734) An orally active, selective, and potent α4β2 nAChR partial agonist with antidepressant, neuroprotective, and long-lasting cognitive effects.Ispronicline has a high affinity for the α4β2 nAChR with a Ki= 11 nM.

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.

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.

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).

α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.

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.

Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300 CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity. Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 μM and 7.39 μM, respectively.

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.

Thonzylamine hydrochloride (Resistab) is an anticholinergic and antihistamine used as an antipruritic.

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

Anisodamine (6-beta-Hydroxyhyoscyamine) is an antagonist of muscarinic and nicotinic cholinoceptor with similar affinities at the muscarinic receptor as scopolamine and atropine. Anisodamine improve the microcirculation in states of shock and can be used in studies about organophosphate poisoning.

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

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

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

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

1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf MEK1 ERK1 2 and AMPKα Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.

Adenine (6-Aminopurine), a purine derivative, is a nucleobase essential in biochemistry, participating in cellular respiration through ATP, NAD, and FAD, and in protein synthesis as a component of DNA and RNA.

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.

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

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.

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

Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.

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.