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nicotinic acetylcholine receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

35

Inhibitors & Agonists

7

Peptides

8

Natural
Products

2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100806
    Kynurenic acid
    Maximum Cited Publications
    10 Publications Verification

    Quinurenic acid

    iGluR Endogenous Metabolite Apoptosis CXCR GPR35 Neurological Disease Inflammation/Immunology Endocrinology
    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
    Kynurenic acid
  • HY-P1264
    α-Bungarotoxin
    5+ Cited Publications

    nAChR Neurological Disease
    α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .
    α-Bungarotoxin
  • HY-12560A
    PNU-282987
    Maximum Cited Publications
    14 Publications Verification

    nAChR 5-HT Receptor Neurological Disease
    PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems .
    PNU-282987
  • HY-100806S
    Kynurenic acid-d5
    1 Publications Verification

    Quinurenic acid-d5

    Isotope-Labeled Compounds iGluR Endogenous Metabolite Apoptosis CXCR GPR35 Neurological Disease Metabolic Disease Inflammation/Immunology
    Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8 .
    Kynurenic acid-d5
  • HY-14564A
    GTS-21 dihydrochloride
    Maximum Cited Publications
    14 Publications Verification

    DMXB-A; DMBX-anabaseine

    nAChR 5-HT Receptor Inflammation/Immunology
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist .
    GTS-21 dihydrochloride
  • HY-107512
    Kynurenic acid sodium
    Maximum Cited Publications
    10 Publications Verification

    iGluR Apoptosis Endogenous Metabolite CXCR GPR35 Neurological Disease Inflammation/Immunology Endocrinology
    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
    Kynurenic acid sodium
  • HY-N0340
    Scopolamine butylbromide
    1 Publications Verification

    Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide

    mAChR Neurological Disease Inflammation/Immunology
    Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (Ki 83 nmol/L), hM2 (Ki 233 nmol/L), rat intestinal M3 (Ki 290 nmol/L) and hM3 (Ki 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .
    Scopolamine butylbromide
  • HY-P0102

    nAChR Neurological Disease Metabolic Disease
    Dipeptide diaminobutyroyl benzylamide diacetate, a Wagerlin-1-mimicking peptide, is a nAChR antagonist. Dipeptide diaminobutyroyl benzylamide diacetate mimics Waglerin-1 to block neuromuscular junction nicotinic acetylcholine receptors, partially inhibits neuronal signal transduction, and relaxes muscles. Dipeptide diaminobutyroyl benzylamide diacetate reduces appearance of facial wrinkles linked to repeated muscle movement.Dipeptide diaminobutyroyl benzylamide diacetate can be used for the research of mild-to-moderate fine and coarse periocular and perioral wrinkles and periorbital ageing .
    Dipeptide diaminobutyroyl benzylamide diacetate
  • HY-N3610
    Coclaurine
    1 Publications Verification

    nAChR Cancer
    Coclaurine is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum with anticancer activity. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist. Coclaurine is a key molecule in S. tetrandra responsible for EFHD2 inhibition. Coclaurine can downregulate EFHD2-related NOX4-ABCC1 signaling and enhanced Cisplatin (HY-17394) sensitivity. Coclaurine suppresses the stemness and metastatic properties of NSCLC cells. Coclaurine disrupts the interaction between the transcription factor FOXG1 and the EFHD2 promoter, leading to a reduction in EFHD2 transcription .
    Coclaurine
  • HY-P1264F

    nAChR Neurological Disease
    FITC-labeled α-Bungarotoxin is FITC-conjugated α-Bungarotoxin (HY-P1264). α-Bungarotoxin acts as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs) .
    α-Bungarotoxin, FITC labeled
  • HY-125159

    PF-00520904

    Parasite nAChR Infection
    Derquantel, a spirocyclic anthelmintic, is a competitive, orally active nicotinic acetylcholine receptor (nAChR) antagonist. Derquantel inhibits ACh-induced depolarization with an IC50 of 0.22 μM. By selectively antagonizing nAChRs on the somatic muscles of nematodes, Derquantel causes flaccid paralysis of muscles, thereby dislodging parasites from the host's gastrointestinal tract. Derquantel is applicable to research related to Haemonchus contortus infection and Ascaris suum infection .
    Derquantel
  • HY-101347

    nAChR Neurological Disease
    Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way .
    Chlorisondamine diiodide
  • HY-100806R
    Kynurenic acid (Standard)
    Maximum Cited Publications
    10 Publications Verification

    Quinurenic acid (Standard)

    Reference Standards iGluR Endogenous Metabolite Apoptosis CXCR GPR35 Neurological Disease Inflammation/Immunology Endocrinology
    Kynurenic acid (Standard) is the analytical standard of Kynurenic acid. This product is intended for research and analytical applications. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
    Kynurenic acid (Standard)
  • HY-135783
    AT 1001
    1 Publications Verification

    nAChR Neurological Disease Metabolic Disease Inflammation/Immunology
    AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .
    AT 1001
  • HY-106901A

    HI-6

    Cholinesterase (ChE) nAChR Neurological Disease
    Asoxime dichloride (HI-6) is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system .
    Asoxime dichloride
  • HY-P1271

    Catestatin (cattle)

    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-136146

    nAChR Neurological Disease
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity .
    SUVN-911
  • HY-P0099

    nAChR Others
    Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .
    Pentapeptide-3
  • HY-W705106
    (-)-Coclaurine hydrochloride
    1 Publications Verification

    (-)-(S)-Coclaurine hydrochloride; L-Coclaurine hydrochloride

    nAChR Neurological Disease
    (-)-Coclaurine hydrochloride (compound I) is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum. (-)-Coclaurine hydrochloride is a nicotinic acetylcholine receptor (nAChRs) antagonist .
    (-)-Coclaurine hydrochloride
  • HY-108069

    Potassium Channel nAChR Neurological Disease
    Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist .
    Iptakalim hydrochloride
  • HY-145297

    nAChR Insecticide Neurological Disease
    Flupyrimin is the antagonist for insect nicotinic acetylcholine receptor (nAChR) that exhibits insecticidal effect by targeting insect nervous system .
    Flupyrimin
  • HY-139581

    SUVN-911 free base

    nAChR Neurological Disease
    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-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-12560

    nAChR 5-HT Receptor Neurological Disease
    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-106901AS
    Asoxime-d4 dichloride
    1 Publications Verification

    HI-6-d4

    Isotope-Labeled Compounds Cholinesterase (ChE) nAChR Neurological Disease
    Asoxime-d4 dichloride (HI-6-d4) is the deuterium labeled Asoxime dichloride. Asoxime dichloride is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system.
    Asoxime-d4 dichloride
  • HY-P5833

    κ-Bgt

    nAChR Neurological Disease
    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-114791

    nAChR Neurological Disease
    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-169870

    (+)-Mecamylamine; TC-5214

    nAChR Neurological Disease
    Dexmecamylamine ((+)-Mecamylamine) is the antagonist for nicotinic acetylcholine receptor (nAChR), that antagonises the α3β4/α4β2/α7/α1β1γδ receptor with IC50 of micromolare levels. Dexmecamylamine exhibits anxiolytic and antidepressant-like activities .
    Dexmecamylamine
  • HY-14564

    nAChR 5-HT Receptor Inflammation/Immunology
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research .
    GTS-21
  • 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-145297R

    Reference Standards nAChR Insecticide Neurological Disease
    Flupyrimin (Standard) is the analytical standard of Flupyrimin. This product is intended for research and analytical applications. Flupyrimin is the antagonist for insect nicotinic acetylcholine receptor (nAChR) that exhibits insecticidal effect by targeting insect nervous system .
    Flupyrimin (Standard)
  • HY-107512R

    iGluR Apoptosis Endogenous Metabolite CXCR GPR35 Reference Standards Neurological Disease Inflammation/Immunology Endocrinology
    Kynurenic acid (sodium) (Standard) is the analytical standard of Kynurenic acid (sodium). This product is intended for research and analytical applications. Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
    Kynurenic acid sodium (Standard)
  • HY-12560C

    nAChR 5-HT Receptor Neurological Disease
    (S)-PNU-282987 hydrochloride is an isoform of PNU-282987 (HY-12560). 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 .
    (S)-PNU-282987 hydrochloride
  • HY-W680961

    nAChR Neurological Disease
    Hydrohydrastinine is a selective α4β2 nicotinic acetylcholine receptor antagonist with an IC50 of 2.6 μM and a Ki of 17 μM. Hydrohydrastinine exhibits weak activity at α4β4 and α3β4 nicotinic acetylcholine receptors. Hydrohydrastinine can be used for the research of depression .
    Hydrohydrastinine
  • HY-106901B

    HI-6 dimesylate

    Cholinesterase (ChE) nAChR Neurological Disease
    Asoxime dimesylate (HI-6 dimesylate) is an orally active thiosemicarbazone-based antidote. Asoxime dimesylate is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dimesylate significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dimesylate is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dimesylate can serve as an effective immunomodulator, improving the immune effect of the nervous system .
    Asoxime dimesylate

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