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-12149
    A-867744
    		Agonist 99.76%
    A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
    A-867744
  • HY-133086
    Hydrodolasetron
    		Inhibitor 98.96%
    Hydrodolasetron is a metabolite of Dolasetron (HY-B0750). Hydrodolasetron is more potent than Dolasetron in inhibiting nAChR. Hydrodolasetron is a 5-HT(3A)R blocker with an IC50 of 0.29 nM. Hydrodolasetron has antiemetic activity.
    Hydrodolasetron
  • HY-B1191S
    Nanofin-d2
    Nanofin-d2 (2,6-Lupetidine-d2) is the deuterium labeled Nanofin (HY-B1191). Nanofin (2,6-Lupetidine) is a neuro-blocking agent with antihypertensive effects, which can be used for the study of mild to moderate hypertension.
    Nanofin-d<sub>2</sub>
  • HY-B1395A
    Mecamylamine
    		Antagonist
    Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.
    Mecamylamine
  • HY-B0489A
    Arecoline hydrochloride
    		Agonist
    Arecoline hydrochloride, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrochloride exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrochloride also can induce oxidative stress.
    Arecoline hydrochloride
  • HY-105670A
    PHA-543613 hydrochloride
    		Agonist
    PHA-543613 hydrochloride is an oral or active α7 nAChR agonist with brain permeability, For α3β4, α1β1γδ, α4β2 and 5-HT3 receptors selective. PHA-543613 hydrochloride affects sensory gating and memory in an in vivo model of schizophrenia.
    PHA-543613 hydrochloride
  • HY-139581
    Ropanicant
    		Antagonist
    Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression.
    Ropanicant
  • HY-105670B
    PHA-543613 dihydrochloride
    		Agonist ≥99.0%
    PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
    PHA-543613 dihydrochloride
  • HY-157958
    α7 nAChR Modulator-3
    		Modulator
    α7 nAChR modulator-3 (Compound 6p) is a α7 nAChR positive allosteric Modulator with a IC50 value of 1.3 μM. α7 nAChR Modulator-3 can be used to inhibit auditory gating defects in a mouse schizophrenic model.
    α7 nAChR Modulator-3
  • HY-A0258A
    Metubine
    Metubine (Metocurine iodide) is a non-depolarizing muscle relaxant. Metubine has neuromuscular blocking activities.
    Metubine
  • HY-18060A
    Bradanicline hydrochloride
    		Agonist
    Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline hydrochloride exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline hydrochloride possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline hydrochloride requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline hydrochloride is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough.
    Bradanicline hydrochloride
  • HY-B0020R
    Tropisetron Hydrochloride (Standard)
    		Activator
    Tropisetron (Hydrochloride) (Standard) is the analytical standard of Tropisetron (Hydrochloride). Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation.
    Tropisetron Hydrochloride (Standard)
  • HY-111161
    GSK575594A
    		Modulator
    GSK575594A is a modulator of the nicotinic acetylcholine receptor (nAChR) in Ascaris suum. GSK575594A enhances muscle contractions induced by acetylcholine (ACh) by binding to the allosteric binding site between subunits within the transmembrane domain of nAChR. At a concentration of 3 μM, GSK575594A significantly increased the contraction induced by ACh in Ascaris suum (Emax increased from 1.19 g to 1.51 g). GSK575594A may be used in research within the field of antiparasitic studies.
    GSK575594A
  • HY-W698445
    α-Nicotine
    		Control
    α-Nicotine is the α-isomer of Nicotine. Nicotine is a nicotinic acetylcholine receptor (nAChR) agonist. Nicotine is promising for research of neuropsychiatric disorders (e.g., schizophrenia, ADHD).
    α-Nicotine
  • HY-P5833
    κ-Bungarotoxin
    		Antagonist
    κ-Bungarotoxin (κ-Bgt) is a potent, selective, and slowly reversible antagonist of α3β2 neuronal nicotinic acetylcholine receptors with an IC50 of 2.30 nM.
    κ-Bungarotoxin
  • HY-107671
    DMAB-anabaseine dihydrochloride
    		Modulator
    DMAB-anabaseine dihydrochloride is a selective nicotinic α7 receptor partial agonist and an α4β2 nAChR antagonist. DMAB-anabaseine dihydrochloride shows cognition-enhancing effects.
    DMAB-anabaseine dihydrochloride
  • HY-182707
    JWX-A0108
    		Activator
    JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease.
    JWX-A0108
  • HY-180400
    PAM-2
    		Modulator
    PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC50: 39 μM, rat α7 nAChR EC50: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC50 = 174 μM) and CaV2.2 channel (IC50 = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain.
    PAM-2
  • HY-130432
    DBO-83 dihydrochloride
    		Agonist
    DBO-83 dihydrochloride is a brain-penetrant nicotinic acetylcholine receptor (nAChR) agonist. DBO-83 dihydrochloride activates peripheral nicotinic acetylcholine receptors to evoke non-stimulated ileum contractions. 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
Cat. No. Product Name / Synonyms Application Reactivity