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-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-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-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
  • HY-121027A
    Anagyrine hydrochloride
    		Antagonist
    Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR.
    Anagyrine hydrochloride
  • HY-146405
    nAChR antagonist 1
    		Antagonist
    nAChR antagonist 1 (compound B15) is an excellent α7 nAChR antagonist with an IC50 value of 3.3 μM. nAChR antagonist 1 can be used for researching schizophrenia, Alzheimer’s disease and inflammatory disorders.
    nAChR antagonist 1
  • HY-W099757
    (±)-Coniine hydrochloride
    		Agonist 98.0%
    (±)-Coniine hydrochloride (2-Propylpiperidine hydrochloride) is a potent nAChR agonist with an EC50 value of 0.3 mM. (±)-Coniine hydrochloride shows acute toxicity with an LD50 value of 7.7 mg/kg.
    (±)-Coniine hydrochloride
  • HY-105181
    T 588
    		Activator
    T 588 is an orally active neuroprotective agent. T 588 can increase acetylcholine release from the frontal cortex and hippocampus and meliorate cognitive dysfunction. T 588 can protect cerebellar granule cells from glutamate neurotoxicity. T 588can be used for the research of neurological disease, such as Alzheimer's disease.
    T 588
  • HY-N3894
    Ferulamide
    		Inhibitor 99.10%
    Ferulamide is a Ferulic acid derivative isolated from Portulaca oleracea L. with anticholinesterase activities.
    Ferulamide
  • HY-149776
    RGH-560
    RGH-560 (compound 53) shows highly advanced α7 nAChR positive modulator properties and favorable physicochemical features. RGH-560 has robust procognitive in vivo potential. RGH-560 can be used to study Scopolamine (HY-N0296) -induced amnesia in mice.
    RGH-560
  • HY-121141
    Adiphenine
    		Inhibitor
    Adiphenine is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine has anticonvulsant effects.
    Adiphenine
  • HY-178356
    BChE-IN-44
    		Inhibitor
    BChE-IN-44 is a potent, brain-penetrant, highly selective BChE inhibitor [equine BChE IC50 = 18.00 pM, human BChE IC50 = 1.50 nM]. BChE-IN-44 shows neuroprotective effects against the Aβ1-42-induced injury model and inhibitory effects on Aβ1-42 self-aggregation. BChE-IN-44 reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (HY-D1056)-induced BV2 cells. BChE-IN-44 can significantly ameliorate Scopolamine (HY-N0296)-induced cognition impairment. BChE-IN-44 exhibits capacity in the regulation of BChE and acetylcholine levels in the mouse hippocampus. BChE-IN-44 can be used for the study of Alzheimer’s disease (AD).
    BChE-IN-44
  • HY-14565
    Pozanicline
    		Antagonist
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
    Pozanicline
Cat. No. Product Name / Synonyms Application Reactivity