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nAChRs

" in MedChemExpress (MCE) Product Catalog:

207

Inhibitors & Agonists

4

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36

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25

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12

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P3654

    nAChR Neurological Disease
    α-Conotoxin SIA is a selective nicotinic acetylcholine receptor (nAChR) antagonist with high affinity for the muscle nAChR. α-Conotoxin SIA preferentially targets the α/δ interface of the muscle nAChR in mouse muscle. In contrast, for Torpedo nAChR, α-Conotoxin SIA has a much higher affinity for the α/γ than for the α/δ interface .
    α-Conotoxin S IA
  • HY-145299

    nAChR Infection
    nAChR modulator-1, a insecticide, is a insect nAChR orthosteric modulator .
    <em>nAChR</em> modulator-1
  • HY-145300

    nAChR Infection
    nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator .
    <em>nAChR</em> modulator-2
  • HY-107686

    5-I A-85380 dihydrochloride

    nAChR Neurological Disease
    5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with Kds of 12 and 14 pM,respectively .
    5-Iodo-A-85380 dihydrochloride
  • HY-P5188A

    nAChR GABA Receptor Neurological Disease
    Waglerin-1, a 22-amino acid peptide, is a competitive antagonist of the muscle nicotinic receptor (nAChR) .
    Waglerin-1
  • HY-10063

    TC-1734; ACD3480

    nAChR Neurological Disease
    Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
    Ispronicline
  • HY-136258

    nAChR Neurological Disease
    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 .
    <em>nAChR</em> agonist CMPI hydrochloride
  • HY-110131

    nAChR Neurological Disease
    A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile .
    A 85380 hydrochloride
  • HY-157958

    nAChR Neurological Disease
    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 <em>nAChR</em> Modulator-3
  • HY-N12511

    nAChR Neurological Disease
    Aristoquinoline (Compound 1) is an alkaloid can be isolated from Aristotelia chilensis. Aristoquinoline has α3β4 nAChR inhibitory activity .
    Aristoquinoline
  • HY-W014928

    (S)-Anabasine hydrochloride; (+)-Anabasine hydrochloride

    nAChR Neurological Disease
    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-145297

    nAChR Neurological Disease
    Flupyrimin acts as an antagonist at the insect nicotinic acetylcholine receptor (nAChR) .
    Flupyrimin
  • HY-146405

    nAChR Neurological Disease Inflammation/Immunology
    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 .
    <em>nAChR</em> antagonist 1
  • HY-110087

    nAChR Neurological Disease
    4BP-TQS is a potent allosteric agonist of α7 nAChR. 4BP-TQS activates nAChRs via an allosteric transmembrane site .
    4BP-TQS
  • HY-10019

    CP 526555

    nAChR Neurological Disease Inflammation/Immunology Cancer
    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
  • HY-10020

    CP 526555 hydrochloride

    nAChR Neurological Disease Inflammation/Immunology
    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 Hydrochloride
  • HY-10021

    CP 526555-18

    nAChR ERK p38 MAPK Others Neurological Disease
    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 Tartrate
  • HY-10019A

    CP 526555 dihydrochloride

    nAChR Neurological Disease Inflammation/Immunology
    Varenicline (CP 526555-18) 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 dihydrochloride
  • HY-138879A

    nAChR Neurological Disease
    (Rac)-CP-601927 hydrochloride is the racemate of CP-601927. CP-601927 is a nAChR agonist with Ki values 1.2 nM and 102 nM for α4β2 and α3β4 nAChR, respectively .
    (Rac)-CP-601927 hydrochloride
  • HY-10021R

    nAChR ERK p38 MAPK Others Neurological Disease
    Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. 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 Tartrate (Standard)
  • HY-131001

    nAChR Neurological Disease
    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 Ca 2+ signalling in the MHb .
    DPNB-ABT594
  • HY-152170

    nAChR Neurological Disease
    bPiDI is a novel selective α6β2 nicotinic receptor antagonist. bPiDI inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
    bPiDI
  • HY-10019S1

    CP 526555-15N,13C,d2

    nAChR Isotope-Labeled Compounds Neurological Disease Inflammation/Immunology Cancer
    Varenicline- 15N, 13C,d2 is 15N and deuterated labeled Varenicline (HY-10019). 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-15N,13C,d2
  • HY-B1532

    (S)-Anabasine; (+)-Anabasine

    nAChR Neurological Disease
    Anabasine ((S)-Anabasine) 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
  • HY-B0823

    nAChR Neurological Disease
    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
  • HY-105170B

    nAChR Neurological Disease
    ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease .
    ABT-418 hydrochloride
  • HY-B1552B

    nAChR Neurological Disease
    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-107680

    3-Pyr-Cyt

    nAChR Neurological Disease
    3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak α4β2 nAChR partial agonist that has been studied as an antidepressant .
    3-Pyr-Cytisine
  • HY-110121

    nAChR Neurological Disease
    NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .
    NS3861 fumarate
  • HY-110121A

    nAChR Neurological Disease
    NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .
    NS3861
  • HY-124874

    (rel)-Aspergillimide; (rel)-VM55598

    nAChR Neurological Disease
    (rel)-Asperparaline A ((rel)-Aspergillimide), an anthelmintic metabolite, is isolated from okara that has been fermented with Aspergillus japonicas JV-23. (rel)-Asperparaline A is also a potent and selective antagonist of nAChR. (rel)-Asperparaline A exhibits paralytic activity in silk worms .
    (rel)-Asperparaline A
  • HY-N2326

    nAChR Neurological Disease
    (±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM) .
    (±)-Anatoxin A fumarate
  • HY-B0118A

    ORG NC 45

    nAChR Neurological Disease Cancer
    Vecuronium (ORG NC 45) bromide is a non-depolarizing neuromuscular blocking agent that also acts as a nicotinic acetylcholine receptor (nAChR) inhibitor, a muscle relaxant, and can be used for pre-surgical anesthesia .
    Vecuronium bromide
  • HY-10019AS1

    Isotope-Labeled Compounds Inflammation/Immunology
    Varenicline-d4 hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .
    Varenicline-d4 hydrochloride
  • HY-P5306

    nAChR Neurological Disease
    α-Conotoxin TxID is a potent α3β4 nAChR antagonist with an IC50 value of 12.5 nM. α-Conotoxin TxID has weak inhibition activity of closely related α6/α3β4 nAChR (IC50= 94 nM). α-Conotoxin TxID has the potential for novel smoking cessation drug development .
    α-Conotoxin TxID
  • HY-B0379A

    nAChR Neurological Disease
    Adiphenine hydrochloride 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 hydrochloride has anticonvulsant effects .
    Adiphenine hydrochloride
  • HY-145295

    nAChR Infection
    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
  • HY-A0106
    Levamisole
    3 Publications Verification

    (-)-Tetramisole

    nAChR Parasite Infection Inflammation/Immunology Cancer
    Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active .
    Levamisole
  • HY-N10132

    nAChR Infection Neurological Disease
    Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM .
    Microgrewiapine A
  • HY-135483A

    nAChR Neurological Disease
    AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways .
    AR-R17779 hydrochloride
  • HY-105670A

    nAChR Neurological Disease
    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-A0106R

    Infection Inflammation/Immunology Cancer
    Levamisole (Standard) is the analytical standard of Levamisole. This product is intended for research and analytical applications. Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active .
    Levamisole (Standard)
  • HY-P1271

    nAChR Cardiovascular Disease
    Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
    Catestatin
  • HY-59201A

    nAChR 5-HT Receptor Neurological Disease
    A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .
    A-582941 dihydrochloride
  • HY-P1271A

    nAChR Cardiovascular Disease
    Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
    Catestatin TFA
  • HY-128575

    nAChR Neurological Disease
    BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-agent like properties and clinical candidate potential. .
    BNC375
  • HY-P5823

    nAChR Neurological Disease
    Azemiopsin is a potent nicotinic acetylcholine receptor (nAChR) inhibitor with IC50s of 0.18 μM and 22 μM against T. californica nAChR and human α7 nAChR, respectively. Azemiopsin blocks acetylcholine-induced currents in Xenopus oocytes heterologously expressing human muscle-type nAChR .
    Azemiopsin
  • HY-107669

    nAChR Neurological Disease
    nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
    <em>nAChR</em>-IN-1 hydrochloride
  • HY-138953

    nAChR Neurological Disease
    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-138953A

    nAChR Neurological Disease
    Epiboxidine hydrochloride 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 hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418 .
    Epiboxidine hydrochloride

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