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AChR Agonists

Cat.No. Product Name Information Product Use Citations Product Validations
S6887 Clozapine N-oxide (CNO chemical) CNO (Clozapine N-oxide) 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.Solutions are unstable and should be fresh-prepared.
Theranostics, 2025, 15(5):1822-1841
STAR Protoc, 2025, 6(1):103542
Theranostics, 2024, 14(7):2881-2896
S4231 Pilocarpine HCl Pilocarpine HCl (NSC 5746) is a selective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.
Viruses, 2024, 16(10)1559
Heliyon, 2024, 10(1):e23945
Theranostics, 2021, 11(12):5986-6005
S2614 Arecoline HBr Arecoline(NSC-31750) is a muscarinic acetylcholine receptor agonist.
Antioxidants (Basel), 2024, 13(4)430
Int J Oral Sci, 2024, 16(1):17
Oncogene, 2020, 39(11):2437-2449
Verified customer review of Arecoline HBr
S1805 Acetylcholine Chloride The chemical compound Acetylcholine Chloride(ACh chloride) is a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans.
Cell Mol Life Sci, 2024, 81(1):88
iScience, 2023, 26(3):106241
Cell, 2022, 185-21:3950-3965.e25
S2455 Bethanechol chloride Bethanechol chloride(Myocholine,Urecholine) is a selective muscarinic receptor agonist without any effect on nicotinic receptors.
Environ Toxicol Chem, 2021, 10.1002/etc.5018
Exp Physiol, 2020, 10.1113/EP088900
Lung, 2018, 196(2):219-229
S4171 Choline Chloride Choline chloride(Hepacholine) 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.
Nat Commun, 2023, 14(1):5034
S4718 Acetylcholine iodide Acetylcholine 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.
Food Sci Nutr, 2022, 10(8):2773-2785
Biotechnol Lett, 2020, 42(7):1219-1227
S1440 Varenicline Tartrate (CP 526555-18) Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction.
Neuropharmacology, 2023, S0028-3908(23)00262-9
S4121 Succinylcholine Chloride Dihydrate Succinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.
Cell Rep Methods, 2023, 3(10):100599
S4422 Nitenpyram Nitenpyram(Bestguard,Capstar) is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets.
Proc Natl Acad Sci U S A, 2020, 117(21):11321-11327
S2287 Cytisine Cytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist.
Transl Oncol, 2023, 35:101712
E1265 Deschloroclozapine Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs (muscarinic Designer Receptors Exclusively Activated by Designer Drugs) agonist, and binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively.
Curr Biol, 2025, 35(12):2916-2926.e3
S6432 Cevimeline HCl hemihydrate Cevimeline HCl hemihydrate(AF 102B, SNI 2011, SNK 508) is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3.
Front Pharmacol, 2022, 13:914153
S3684 Methacholine chloride Methacholine (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.
Phytomedicine, 2025, 148:157306
S5930 PNU 282987 HCl PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor.
Biol Pharm Bull, 2025, 48(5):728-732
E7001 Pilocarpine Pilocarpine is a non-selective agonist of muscarinic acetylcholine receptor (mAChR), commonly used to treat xerostomia and glaucoma. It modulates the electrical properties of heart cells, likely by activating a potassium (K+) current mediated by M3 receptors.
Front Mol Biosci, 2024, 11:1423351
S0717 Varenicline (CP 526555) dihydrochloride Varenicline (CP 526555, Chantix, Champix,CP 526555 dihydrochloride) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.
S0720 PNU-282987 PNU-282987 is a novel selective agonist of the alpha7 nAChR with Ki of 26 nM for rat alpha7 nAChR. This compound shows no activity at all tested monoamine, muscarine, glutamate, and GABA receptors, except 5-HT3 receptors with Ki of 930 nM.
S0521 PNU-282987 S enantiomer free base PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base, which is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.
S5022 Varenicline Hydrochloride Varenicline (CP 526555) Hydrochloride is a partial agonist of α4β2 nicotine acetylcholine receptor (nAChR) and α6β2 nicotine acetylcholine receptor (nAChR), with a Ki value of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively, in the striatum of rats.
E1876 GTS-21 dihydrochloride GTS-21 dihydrochloride (DMXB-A, DMBX-anabaseine) is a selective agonist of alpha7 nicotinic acetylcholine receptor (α7-nAChR) and exhibits anti‑inflammatory and cognition‑enhancing activities. This compound is also an antagonist of α4β2 with a Ki value of 20 nM for humanα4β2 and 5-HT3A receptor with an IC50 value of 3.1 μM.
S7366 LY2119620 LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
E0755 Guvacoline hydrochloride Norarecoline hydrochloride (Guvacoline hydrochloride) is a pyridine alkaloid found in Areca triandra, which can act as a full agonist at both atrial and ileal muscarinic receptors.
E4714 Xanomeline Xanomeline(LY-246708) is a selective agonist of muscarinic type 1(M(1) receptor and muscarinic type 4 receptor(M(4). It increases neuronal excitability and inhibits behaviors induced by D-amphetamine and (-)-apomorphine.
S4072 Decamethonium Bromide Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
S9789 JHU37152 JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.
S9790 JHU37160 JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.
S2957 Encenicline (EVP-6124) hydrochloride Encenicline (EVP-6124) hydrochloride is a selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors.
E0176 Dinotefuran

Dinotefuran (MTI-446), a neonicotinoid, is an effective nAChRs agonist with EC50 of 7.8 μM and shows high insecticidal activity on Da2b2 hybrid nAChRs.
S0457 DREADD agonist 21 DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM.
S6795 VU0357017 Hydrochloride VU0357017 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.
E5819New Clozapine N-oxide dihydrochloride Clozapine N-oxide dihydrochloride is a primary metabolite of clozapine. It acts as an agonist for human muscarinic designer receptors DREADD, with a pEC50 of 8.31 for the M1 DREADD.
S1356 Levetiracetam (UCB-L059) Levetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy and an agonist of muscarinic acetylcholine receptors (mAChR). This compound also modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel.
Front Neurosci, 2023, 17:1336026
bioRxiv, 2023, 2023.11.10.566574
Alzheimers Dement (N Y), 2022, 8(1):e12329
Verified customer review of Levetiracetam (UCB-L059)