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-N8249
    Cynandione A
    		Activator
    Cynandione A is an acetophenone that can be isolated from Cynanchum Wilfordii Radix. Cynandione A protects hepatocytes and cortical neurons from toxicity and improves neurological deficits in a rat model of cerebral ischemia. On the other hand, cynandione A has significant anti-inflammatory effects and inhibits inflammation by activating macrophage α7 nAChR and IL-10 expression.
    Cynandione A
  • HY-130432
    DBO-83 dihydrochloride
    		Agonist
    DBO-83 dihydrochloride is a novel nicotinic acetylcholine receptor agonist, and binds to nAChRs in rat cortical membranes with a Ki value of 4.1 nM. DBO-83 dihydrochloride shows antinociceptive and anti-amnesic activities.
    DBO-83 dihydrochloride
  • HY-120946
    VMY-2-95
    VMY-2-95 is an oral active and blood-brain barrier (BBB) penetrant α4β2 nicotinic acetylcholine receptor desensitizer. VMY-2-95 can be used for study of depression or addiction.
    VMY-2-95
  • 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-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-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-10019AS
    Varenicline-d4 dihydrochloride
    Varenicline-d4 (dihydrochloride) is the deuterium labeled Varenicline dihydrochloride.
    Varenicline-d<sub>4</sub> dihydrochloride
  • HY-W777360
    Harman-13C2,15N
    		Inhibitor
    Harman-13C2,15N is 13C and 15N labeled Harmane. Harmane 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 also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harman-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-114791
    Lobelanidine
    		Antagonist
    Lobelanidine is an antagonist for nicotinic acetylcholine receptor (nAChR), which inhibits α7 nAChR response and α3β2/α3β4 nAChR responses, with IC50 of 2.8 and 8.2 μM.
    Lobelanidine
  • HY-149483
    CVN417
    		Antagonist
    CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease.
    CVN417
  • HY-161671
    GAT2711
    		Agonist 98.00%
    GAT2711 is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 shows 340-fold selective for α9 over α7 nAChRs. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells. GAT2711 retains full analgesic activity in α7 nAChR knockout mice.
    GAT2711
  • 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-160959
    AN317
    		Agonist
    AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP+. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB).
    AN317
  • 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