2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. nAChR

nAChR

Nicotinic acetylcholine receptors

nAChR

Related Products

PDF 2.11 MB

nAChRs (nicotinic acetylcholine receptors) are neuron receptor proteins that signal for muscular contraction upon a chemical stimulus. They are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the presynaptic and postsynaptic sides of theneuromuscular junction. Nicotinic acetylcholine receptors are the best-studied of the ionotropic receptors. Like the other type of acetylcholine receptor-the muscarinic acetylcholine receptor (mAChR)-the nAChR is triggered by the binding of the neurotransmitter acetylcholine (ACh). Just as muscarinic receptors are named such because they are also activated by muscarine, nicotinic receptors can be opened not only by acetylcholine but also by nicotine —hence the name "nicotinic".

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-59201A
    A-582941 dihydrochloride
    		Agonist 99.78%
    A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia.
    A-582941 dihydrochloride
  • HY-118504
    Sulfoxaflor
    		Agonist 99.92%
    Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc.
    Sulfoxaflor
  • HY-112217A
    PSEM 89S TFA
    		Agonist 99.85%
    PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.
    PSEM 89S TFA
  • HY-P0099
    Pentapeptide-3
    		Antagonist 99.83%
    Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides.
    Pentapeptide-3
  • HY-136207
    TC-2559 difumarate
    		Agonist 98.4%
    TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
    TC-2559 difumarate
  • HY-B1219
    Pentolinium tartrate
    		Antagonist 99.97%
    Pentolinium tartrate is a ganglionic blocking agent. Pentolinium tartrate lowers blood pressure and permits regression of the signs and symptoms associated with severe hypertension.
    Pentolinium tartrate
  • HY-110241
    Dianicline dihydrochloride
    		Agonist 99.97%
    Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner.
    Dianicline dihydrochloride
  • HY-14774S
    (Rac)-Monepantel-d5
    		Agonist 99.4%
    (Rac)-Monepantel-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
    (Rac)-Monepantel-d<sub>5</sub>
  • HY-W002112S
    (±)-Nornicotine-d4
    		98.0%
    (±)-Nornicotine-d4 is the deuterium labeled (±)-Nornicotine (HY-W002112). (±)-Nornicotine is a major metabolite of Nicotine. (±)-Nornicotine is a partial nAChRs agonist, specifically activating receptor subtypes containing α7 and α6 subunits. (±)-Nornicotine disrupts β-catenin and ZO-1, and induces F-actin depolymerization. (±)-Nornicotine supports self-administration behavior. (±)-Nornicotine can be used in the research of atherosclerosis, Alzheimer's disease, and schizophrenia.
    (±)-Nornicotine-d<sub>4</sub>
  • HY-P1271
    Catestatin
    		98.17%
    Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
    Catestatin
  • HY-101392A
    Harmane hydrochloride
    		Inhibitor 99.88%
    Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harmane hydrochloride
  • HY-110131
    A 85380 hydrochloride
    		Agonist 98.86%
    A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile.
    A 85380 hydrochloride
  • HY-13780R
    Vinblastine sulfate (Standard)
    		Inhibitor
    Vinblastine (sulfate) (Standard) is the analytical standard of Vinblastine (sulfate). This product is intended for research and analytical applications. Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
    Vinblastine sulfate (Standard)
  • HY-12150
    CCMI
    		Agonist 99.97%
    CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction.
    CCMI
  • HY-136146
    SUVN-911
    		Antagonist 99.13%
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
    SUVN-911
  • HY-10019A
    Varenicline dihydrochloride
    		Agonist 98.85%
    Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.
    Varenicline dihydrochloride
  • HY-11053
    S 24795
    		Agonist 99.66%
    S 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the research of aging-related memory disturbances.
    S 24795
  • HY-125159
    Derquantel
    		Antagonist 98.4%
    Derquantel, a spirocyclic anthelmintic, is a competitive, orally active nicotinic acetylcholine receptor (nAChR) antagonist. Derquantel inhibits ACh-induced depolarization with an IC50 of 0.22 μM. By selectively antagonizing nAChRs on the somatic muscles of nematodes, Derquantel causes flaccid paralysis of muscles, thereby dislodging parasites from the host's gastrointestinal tract. Derquantel is applicable to research related to Haemonchus contortus infection and Ascaris suum infection.
    Derquantel
  • HY-107682
    TQS
    		Modulator 99.84%
    TQS is a α7 nicotinic acetylcholine receptor (nAChR) positive allosteric modulator. TQS can be used for the research of neuroinflammatory pain.
    TQS
  • HY-111143
    SCH-900271
    		Agonist 98.84%
    SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA).
    SCH-900271
Cat. No. Product Name / Synonyms Application Reactivity