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-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-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-W750777
    Flupyradifurone-d5
    Flupyradifurone-d5 is the deuterium labeled Flupyradifurone (HY-145295). Flupyradifurone is a systemic?nAChR?agonist that interferes with signal transduction in the central nervous system of sucking pests. Flupyradifurone can be used as a butenolide?insecticide.
    Flupyradifurone-d<sub>5</sub>
  • 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-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
  • HY-172704
    DSPE-PEG1000-RVG29
    DSPE-PEG1000-RVG29 is a PEG compound which composed of DSPE and a Rabies virus glycoprotein 29 (RVG29). RVG29 can bind specifically to the nicotinic acetylcholine receptor (nAChR) at the blood-brain barrier (BBB) and cross over the BBB.
    DSPE-PEG1000-RVG29
  • HY-W743727
    Cytisine-d4
    Cytisine-d4 is the deuterium labeled Cytisinicline (HY-N0175). Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs, and partial to full agonist at β4 containing receptors and α7 receptors. Has been used medically to help with smoking cessation.
    Cytisine-d<sub>4</sub>
  • HY-110142
    Thermopsidine
    		Agonist
    Thermopsidine (CC4) is a selective partial agonist at α4β2/α6β2 nAChR with EC50 values of 2.2 μM target α4β2.
    Thermopsidine
  • HY-B0282AS3
    Acetylcholine-d16 bromide
    		≥98.0%
    Acetylcholine-d16 (bromide) is the deuterium labeled Acetylcholine bromide.
    Acetylcholine-d<sub>16</sub> bromide
  • HY-107667
    TC-2559 fumarate
    		Agonist
    TC-2559 fumarate is a potent and selective neuronal acetylcholine receptor agonist. TC-2559 fumarate is potent and efficacious in the activation of CNS receptors and reduces glutamate-induced neurotoxicity in vitro.
    TC-2559 fumarate
  • HY-118504R
    Sulfoxaflor (Standard)
    		Agonist
    Sulfoxaflor (Standard) is the analytical standard of Sulfoxaflor. This product is intended for research and analytical applications. Sulfoxaflor is a sulfoximine insecticide and is an agonist of nAChR1 and nAChR2 subtypes. Sulfoxaflor is used for the control of sap-feeding insects such as Myzus persicae, Aphis gossypii, Bemissia tabaci and Nilaparvata lugens.
    Sulfoxaflor (Standard)
  • HY-138953
    Epiboxidine
    		Agonist
    Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.
    Epiboxidine
  • HY-120609
    BMS-902483
    		Agonist
    BMS-902483 is a quinuclidine-containing spirooxazolidine that is a partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). BMS-902483 improves cognitive ability in preclinical rodent models..
    BMS-902483
  • HY-B0823R
    Acetamiprid (Standard)
    		Agonist
    Acetamiprid (Standard) is the analytical standard of Acetamiprid. This product is intended for research and analytical applications. Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist, and is shown to be associated with neuromuscular and reproductive disorders.
    Acetamiprid (Standard)
Cat. No. Product Name / Synonyms Application Reactivity