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-B1778C
    Succinylcholine iodide
    		Agonist
    Succinylcholine iodide (Suxamethonium iodide) is a depolarizing neuromuscular blocker with rapid onset and short duration of action. Succinylcholine iodide also acts as an agonist of the Acetylcholine receptor. Succinylcholine iodide is used for emergency airway management.
    Succinylcholine iodide
  • HY-106901B
    Asoxime dimesylate
    		Antagonist
    Asoxime dimesylate (HI-6 dimesylate) is an orally active thiosemicarbazone-based antidote. Asoxime dimesylate is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dimesylate significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dimesylate is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dimesylate can serve as an effective immunomodulator, improving the immune effect of the nervous system.
    Asoxime dimesylate
  • HY-160529
    α7 nAChR Modulator-2
    		Modulator
    α7 nAChR Modulator-2 (Compound 7b) is a α7 nAChR positive allosteric modulator (PAM) with an EC50 of 2.1 μM. α7 nAChR Modulator-2 can be used for the research of cognitive disorders.
    α7 nAChR Modulator-2
  • HY-46286
    TTFB
    		Control 99.83%
    TTFB (N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide) is a selective, non-competitive zinc-activated channel (ZAC) antagonist. TTFB inhibits Zn2+- and H+-induced ZAC currents with IC50 values of 3 μM and 8.5 μM, respectively, and has an IC50 of 4.7 μM against spontaneous activity. TTFB shows no significant agonistic, antagonistic or modulatory activity towards representative classical Cys-loop receptors including m5-HT3AR, hα3β4 nAChR, hα1β2γ2S GABAAR and hα1 GlyR. TTFB can be used to investigate the physiological and pathological functions of ZAC.
    TTFB
  • HY-A0009S
    Galanthamine-d3 hydrobromide
    		Agonist
    Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
    Galanthamine-d<sub>3</sub> hydrobromide
  • HY-128420
    Lobeline sulfate
    		Agonist
    Lobeline (α-Lobeline) sulfate is a brain-penetrant nicotinic receptor agonist. Lobeline sulfate increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline sulfate is effective in smoking cessation.
    Lobeline sulfate
  • HY-164034
    Ganglefene
    		Inhibitor
    Ganglefene is a blocker for n-choline receptor, which leads to the sexual dysfunction in the offspring in adulthood, when administrated to pregnant rats.
    Ganglefene
  • HY-14312
    A85380
    		Agonist
    A 85380 is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 exhibits selectivity for the α4β2 nAChR subtypes. A 85380 has a broad-spectrum analgesic profile.
    A85380
  • HY-B1395R
    Mecamylamine hydrochloride (Standard)
    		Antagonist
    Mecamylamine (hydrochloride) (Standard) is the analytical standard of Mecamylamine (hydrochloride). This product is intended for research and analytical applications. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.
    Mecamylamine hydrochloride (Standard)
  • HY-N3359A
    Lupanine perchlorate
    		Inhibitor
    Lupanine (D-Lupanine) perchlorate is a natural ketonic derivative of Sparteine (HY-W008350)with a ganglioplegic activity. Lupanine perchlorate shows binding affinity for nicotinic receptor with a Ki value of 500 nM.
    Lupanine perchlorate
  • HY-118504S
    Sulfoxaflor-d3
    Sulfoxaflor-d3 is the deuterium labeled Sulfoxaflor (HY-118504). 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-d<sub>3</sub>
  • HY-17555A
    Meclofenoxate
    		Inhibitor
    Meclofenoxate (Centrophenoxine) is an ester synthesized from DMAE and pCPA, which has the activity of stimulating memory and improving cognition.
    Meclofenoxate
  • HY-115764
    nAChR agonist 2
    		Agonist
    nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM).
    nAChR agonist 2
  • HY-183204
    TC-2559
    		Agonist
    TC-2559 is an orally active, selective central nervous system Nicotinic acetylcholine receptor agonist with a Ki value of 5 nM. TC-2559 activates central nervous system receptors selectively over peripheral nervous system receptors. TC-2559 improves scopolamine (HY-N0296)-induced cognitive impairment and enhances radial arm maze performance. TC-2559 can be used in the research of neurodegenerative diseases.
    TC-2559
  • HY-10019AS
    Varenicline-d4 dihydrochloride
    Varenicline-d4 (dihydrochloride) is the deuterium labeled Varenicline dihydrochloride.
    Varenicline-d<sub>4</sub> dihydrochloride
  • HY-W747554
    SM 32
    SM 32 is an analgesic. SM 32 produces an increase in ACh release. SM 32 amplifies electrically- and nicotine- evoked guinea-pig ileum contractions. SM32 induces antinociceptive effects through a central cholinergic mechanism.
    SM 32
  • HY-124057
    RO5126946
    		Activator
    RO5126946 is a selective, orally active α7 nAChR allosteric potentiator with EC50 values of 0.06 μM (hα7 nAChR) and 770 nM (α7 nAChR), and it crosses the blood-brain barrier. RO5126946 enhances synaptic transmission and positively modulates GABA-ergic responses by increasing peak current, slowing current decay, and elevating the frequency of spontaneous inhibitory postsynaptic currents, without affecting the recovery of receptors from the desensitized state. RO5126946 not only enhances subthreshold nicotine effects and improves associative learning, but also does not interfere with the original pro-cognitive effects of nicotine. RO5126946 can be used to study cognitive impairments associated with diseases such as Alzheimer's disease and schizophrenia.
    RO5126946
  • HY-P11313
    Catestatin (rat)
    		Antagonist
    Catestatin (rat) (Rat chromogranin A367–387) is a potent, reversible, noncompetitive, and noncooperative nicotinic cholinergic antagonist derived from chromogranin A (A367-387). Catestatin (rat) inhibits norepinephrine release in rat PC12 pheochromocytoma cells (IC50 = 1.2 μM), and blocks desensitization of norepinephrine release (IC50 = 0.62 μM). Catestatin (rat) exerts antiadrenergic effects through the endothelial PI3K-AKT-eNOS pathway in rat papillary muscles and isolated cardiomyocytes. Catestatin (rat) maintains mitochondrial membrane potential in I/R cardiomyocytes and increases phosphorylation of AKT at S473, GSK3β at S9, PLB at T17, and eNOS at S1179. Catestatin (rat) reverses desensitization of 22Na+ uptake. Catestatin (rat) can be used for the study of nicotinic cholinergic receptor regulation and catecholamine release control mechanisms.
    Catestatin (rat)
  • HY-116149
    A-424274
    		Agonist
    A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
    A-424274
  • HY-12560
    PNU-282987 free base
    		Agonist
    PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems.
    PNU-282987 free base
Cat. No. Product Name / Synonyms Application Reactivity