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

nAChR

Nicotinic acetylcholine receptors

nAChR

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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-A0215
    Doxacurium chloride
    		Agonist
    Doxacurium chloride (BW A938U) is a potent non-depolarizing neuromuscular blocking agent. Doxacurium chloride binds to cholinergic receptors to antagonize acetylcholine, resulting in a block of neuromuscular transmission. Doxacurium chloride can be used for the research of neurological diseases.
    Doxacurium chloride
  • HY-B0282AS2
    Acetylcholine-d13 bromide
    		98.55%
    Acetylcholine-d13 (bromide) is the deuterium labeled Acetylcholine bromide.
    Acetylcholine-d<sub>13</sub> bromide
  • HY-171807
    TC-2559 free base
    		Agonist
    TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain.
    TC-2559 free base
  • HY-101078
    (±)-Epibatidine
    		Agonist
    (±)-Epibatidine is a nicotinic agonist. (±)-Epibatidine is a neuronal nAChR agonist.
    (±)-Epibatidine
  • HY-B0942S
    Benzethonium-d7 chloride
    		Inhibitor 98.64%
    Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
    Benzethonium-d<sub>7</sub> chloride
  • HY-10019S1
    Varenicline-15N,13C,d2
    		Agonist
    Varenicline-15N,13C,d2 is 15N and deuterated labeled Varenicline (HY-10019). Varenicline (CP 526555) 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-<sup>15</sup>N,<sup>13</sup>C,d<sub>2</sub>
  • HY-N9949
    Sparteine
    		Inhibitor
    Sparteine (Lupinidine) is an alkaloid compound derived from leguminous plants and can act as a ganglionic blocker. Sparteine competitively inhibits the activity of the neuronal nicotinic acetylcholine receptor (nACh receptor).
    Sparteine
  • HY-115766S
    Anabaseine-d4
    Anabaseine-d4 is the deuterium labeled Anabaseine (HY-115766). Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes. Anabaseine is also a weak partial agonist at α4β2 nAChRs.
    Anabaseine-d<sub>4</sub>
  • HY-14564
    GTS-21
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research.
    GTS-21
  • HY-107673
    RJR-2429 dihydrochloride
    		Agonist
    RJR 2429 hydrochloride is a α4β2 and α7 nAChR agonist.
    RJR-2429 dihydrochloride
  • HY-13225H
    Rivanicline hydrochloride
    		Agonist
    Rivanicline (RJR-2403) hydrochloride is a neuronal nicotinic receptor agonist. Rivanicline hydrochloride is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline hydrochloride can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hydrochloride can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease).
    Rivanicline hydrochloride
  • HY-B1532R
    Anabasine (Standard)
    		Agonist
    Anabasine (Standard) is the analytical standard of Anabasine. This product is intended for research and analytical applications. Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 μM).
    Anabasine (Standard)
  • HY-17440R
    Rocuronium Bromide (Standard)
    Rocuronium (Bromide) (Standard) is the analytical standard of Rocuronium (Bromide). This product is intended for research and analytical applications. Rocuronium Bromide (ORG 9426 Bromide) is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia, to facilitate endotracheal intubation and to provide skeletal musclerelaxation during surgery or mechanical ventilation.
    Rocuronium Bromide (Standard)
  • HY-124110
    TC299423
    		Agonist
    TC299423 is an orally active, brain-penetrant, selective and potent agonist for α6β2? and α4β2? nicotinic acetylcholine receptors (nAChRs) with anxiolytic and antinociceptive properties. TC299423 acts primarily through α6β2? nAChRs that are implicated in the anxiolytic effects of nicotine. TC299423 elicits reward-related behavior mediated through α6β2? nAChRs in hypersensitive α6L90’S mice. TC299423 elicits dopamine release and dose not suppress nicotine self-administration in rats. TC299423 is proming for rasearch of addiction and Parkinson’s disease.
    TC299423
  • HY-146404
    T761-0184
    		Antagonist
    T761-0184 is a potent α7 nicotinic receptor (nAChR) antagonist.
    T761-0184
  • HY-B1382A
    Pempidine hydrochloride
    Pempidine (1,2,2,6,6-Pentamethylpiperidine) hydrochloride is an orally active ganglionic blocking agent used in the treatment of hypertension. Pempidine hydrochloride blocks the effects of intravenously administered addictive drugs and peripheral vagal nerve stimulation on blood pressure, and reduces the output of acetylcholine.
    Pempidine hydrochloride
  • HY-13225E
    (E/Z)-Rivanicline
    		Control
    (E/Z)-Rivanicline ((E/Z)-RJR-2403, (E/Z)-Metanicotine) is the E/Z mixture of Rivanicline (HY-13225A). Rivanicline is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype, Ki is 26 nM, which is more than 1000 times more inhibitory than α7 receptor.
    (E/Z)-Rivanicline
  • HY-107666
    PHA 568487
    		Agonist
    PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR).PHA 568487 reduces neuroinflammation and oxidative stress. PHA-568487 has rapid brain penetration.
    PHA 568487
  • HY-P11249
    Mr1.1[S4Dap, C16Pen]
    		Inhibitor
    Mr1.1[S4Dap, C16Pen] is a highly active and selective nAChR (human α9α10 nAChR IC50 = 4.0 nM, rat α9α10 nAChR IC50 = 2.7 nM) inhibitor. Mr1.1[S4Dap, C16Pen] can significantly relieve pain and has significant stability. Mr1.1[S4Dap, C16Pen] can be used for the study of neuropathic pain.
    Mr1.1[S4Dap, C16Pen]
  • HY-W001160R
    5-Hydroxyindole (Standard)
    		Activator
    5-Hydroxyindole (Standard) is the analytical standard of 5-Hydroxyindole (HY-W001160). This product is intended for research and analytical applications. 5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-type calcium channels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders.
    5-Hydroxyindole (Standard)
Cat. No. Product Name / Synonyms Application Reactivity