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-121027A
    Anagyrine hydrochloride
    		Antagonist
    Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR.
    Anagyrine hydrochloride
  • HY-146405
    nAChR antagonist 1
    		Antagonist
    nAChR antagonist 1 (compound B15) is an excellent α7 nAChR antagonist with an IC50 value of 3.3 μM. nAChR antagonist 1 can be used for researching schizophrenia, Alzheimer’s disease and inflammatory disorders.
    nAChR antagonist 1
  • HY-W099757
    (±)-Coniine hydrochloride
    		Agonist ≥98.0%
    (±)-Coniine hydrochloride (2-Propylpiperidine hydrochloride) is a potent nAChR agonist with an EC50 value of 0.3 mM. (±)-Coniine hydrochloride shows acute toxicity with an LD50 value of 7.7 mg/kg.
    (±)-Coniine hydrochloride
  • HY-N3894
    Ferulamide
    		Inhibitor
    Ferulamide is a Ferulic acid derivative isolated from Portulaca oleracea L. with anticholinesterase activities.
    Ferulamide
  • HY-149776
    RGH-560
    RGH-560 (compound 53) shows highly advanced α7 nAChR positive modulator properties and favorable physicochemical features. RGH-560 has robust procognitive in vivo potential. RGH-560 can be used to study Scopolamine (HY-N0296) -induced amnesia in mice.
    RGH-560
  • HY-121141
    Adiphenine
    		Inhibitor
    Adiphenine is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine has anticonvulsant effects.
    Adiphenine
  • HY-14565
    Pozanicline
    		Antagonist
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
    Pozanicline
  • 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-19490A
    (S)-VQW-765
    		Agonist 98.00%
    (S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia.
    (S)-VQW-765
Cat. No. Product Name / Synonyms Application Reactivity