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-B0282AS2
    Acetylcholine-d13 bromide
    		98.55%
    Acetylcholine-d13 (bromide) is the deuterium labeled Acetylcholine bromide[1].
    Acetylcholine-d<sub>13</sub> bromide
  • 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 α6β2 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-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-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
  • 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-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-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)
  • HY-N12511
    Aristoquinoline
    		Inhibitor
    Aristoquinoline (Compound 1) is an alkaloid can be isolated from Aristotelia chilensis. Aristoquinoline has α3β4 nAChR inhibitory activity.
    Aristoquinoline
  • HY-B1178A
    R-(+)-Cotinine
    R-(+)-Cotinine ((+)-Cotinine), a Nicotine metabolite, lacks significant activity across a wide range of pharmacological targets. R-(+)-Cotinine can enhance the Ach-evoked current in human α7 nAChRs.
    R-(+)-Cotinine
  • HY-N0443R
    N-Methylcytisine (Standard)
    N-Methylcytisine (Standard) is the analytical standard of N-Methylcytisine. This product is intended for research and analytical applications. N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia.
    N-Methylcytisine (Standard)
  • HY-14319A
    Sazetidine A hydrochloride
    Sazetidine A hydrochloride is a potent ligand for the α4β2 nicotinic acetylcholine receptor, exhibiting high binding affinities and selectivity towards this subtype. Sazetidine A hydrochloride demonstrates promising pharmacological properties that could potentially contribute to the development of therapies targeting nicotinic receptor-related conditions. Sazetidine A hydrochloride has been implicated in studies examining the binding affinities of various analogs, highlighting its significance in understanding subtype selectivity among nAChR ligands.
    Sazetidine A hydrochloride
  • HY-B1395S1
    Mecamylamine hydrochloride-13C4,15N
    		Antagonist
    Mecamylamine (hydrochloride)-13C4,15N is the 13C-labeled and 15N-labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
    Mecamylamine hydrochloride-<sup>13</sup>C<sub>4</sub>,<sup>15</sup>N
Cat. No. Product Name / Synonyms Application Reactivity