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-123858
    VU6001221
    		Activator
    VU6001221 is a blood-brain barrier permeable Choline Transporter (CHT) inhibitor (IC50 = 270 nM). VU6001221 increases the likelihood of extracellular choline elevation activating synaptic α7 nicotine ACh receptors. VU6001221 attenuates potassium-induced ACh levels in the prefrontal cortex.
    VU6001221
  • HY-B0827R
    Dinotefuran (Standard)
    		Inhibitor
    Dinotefuran (Standard) is the analytical standard of Dinotefuran. This product is intended for research and analytical applications.
    Dinotefuran (Standard)
  • HY-14318
    Altinicline
    		Agonist
    Altinicline (SIB-1508Y free base) is a selective α4β2 nicotinic acetylcholine receptor (nAChR) agonist, with no activity against α7 or α1β1γδ nAChRs and only extremely low activity against α3β4 nAChRs. Altinicline reverses escape deficits and increases avoidance responses. Altinicline is applicable to research related to depression.
    Altinicline
  • HY-N18367
    Lemairamin
    		Activator
    Lemairamin (Wgx-50) is a hydroxylamine compound. Lemairamin can be isolated from the pericarps of the Zanthoxylum plants. Lemairamin activates α7nAChR, stimulates the expression of IL-10 and POMC. Lemairamin shows a decrease in Akt. Lemairamin attenuates DSS-induced intestinal inflammation. Lemairamin alleviates pain hypersensitivity.
    Lemairamin
  • HY-B0827A
    (R)-Dinotefuran
    		Inhibitor
    (R)-Dinotefuran ((R)-MTI-446), a neonicotinoid pesticide, exhibits comparative insecticidal activities (1.7-2.4 times) to typical sucking pests Aphis gossypii and Apolygus lucorum compared to racemic mixtures by inhibiting nicotinic acetylcholine receptors. (R)-Dinotefuran has a good efficacy in controlling target pests while minimizing hazard to honeybees.
    (R)-Dinotefuran
  • HY-W014928
    Anabasine hydrochloride
    		Agonist
    Anabasine ((S)-Anabasine) hydrochloride 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 hydrochloride
  • HY-B1191S1
    Nanofin-d5
    Nanofin-d5 (2,6-Lupetidine-d5) 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>5</sub>
  • HY-167741
    Chlorisondamine
    		Antagonist
    Chlorisondamine is a nicotinic antagonist that acts as a ganglionic blocker and has been utilized to evaluate the neurogenic contributions to blood pressure and sympathetic vasomotor tone in animal models. Chlorisondamine has demonstrated antihypertensive properties, primarily being assessed through its effects on blood pressure, cardiac output, and heart rate in various experimental settings, particularly in mice.
    Chlorisondamine
  • HY-136258
    nAChR agonist CMPI hydrochloride
    		Agonist
    nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.
    nAChR agonist CMPI hydrochloride
  • HY-18176
    SEN 78702
    		Agonist
    SEN 78702 is an orally active, selective, full α7 nAChR agonist, with a pEC50 of 6.13. SEN 78702 has an acceptable hERG inhibition (IC50: 15.8 μM). SEN 78702 induces memory enhancement.
    SEN 78702
  • HY-134045
    (-)-Anatoxin A
    		Agonist
    (-)-Anatoxin A is an enantiomer of (±)-Anatoxin A (HY-N2326). (-)-Anatoxin A is a neuronal nicotinic acetylcholine receptor agonist. (-)-Anatoxin A can be used for pain and inflammation research.
    (-)-Anatoxin A
  • HY-W756217
    (R)-Monepantel
    		Control 99.95%
    (R)-Monepantel (AAD2224) is the optical R-enantiomer of monepantel. (R)-Monepantel has no nematocidal effect, is inactive.
    (R)-Monepantel
  • HY-B1423
    Lobeline
    		Agonist
    Lobeline (α-Lobeline) is a brain-penetrant nicotinic receptor agonist. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline is effective in smoking cessation.
    Lobeline
  • HY-P10898
    GeX-2
    		Antagonist
    GeX-2 is a truncated analogue of αO-conotoxin. GeX-2 activates GABAB receptor. GeX-2 inhibits α9α10 nAChR and CaV2.2 channels. GeX-2 alleviates pain in the rat model of chronic constriction injury.
    GeX-2
  • HY-14316B
    Tebanicline hydrochloride
    		Modulator
    Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
    Tebanicline hydrochloride
  • HY-59201
    A-582941
    		Agonist
    A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia.
    A-582941
  • HY-131001
    DPNB-ABT594
    		Agonist
    DPNB-ABT594 is a nitrobenzyl-caged ABT594 (HY-14316A) and activates nAChRs containing the α4β2 subunits with good selectivity than the α7 subunit. DPNB-ABT594 can be used to map the distribution of nAChRs on neurons of the medial habenula (MHb) and helps to gain a deeper understanding of the nAChR-mediated Ca2+ signalling in the MHb.
    DPNB-ABT594
  • HY-10020S
    Varenicline-15N3 Hydrochloride
    		Agonist
    Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). 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<sub>3</sub> Hydrochloride
  • HY-137231A
    (S)-UFR2709
    		Antagonist
    (S)-UFR2709 is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 acts as an anxiolytic agent and can be used for the study of nicotine addiction.
    (S)-UFR2709
  • HY-B1552B
    Benzoquinonium dibromide
    		Antagonist
    Benzoquinonium dibromide is a nicotinic acetylcholine receptors (nAChRs) antagonist, with an IC50 of 0.46 μM. Benzoquinonium dibromide can block neuromuscular and ganglionic transmission.
    Benzoquinonium dibromide
Cat. No. Product Name / Synonyms Application Reactivity