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nAChR antagonist

" in MedChemExpress (MCE) Product Catalog:

64

Inhibitors & Agonists

8

Peptides

8

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4

Isotope-Labeled Compounds

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Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-N2332A
    Methyllycaconitine citrate
    Maximum Cited Publications
    43 Publications Verification

    MLA citrate

    nAChR Neurological Disease
    Methyllycaconitine (MLA) citrate is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine citrate alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine citrate prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine citrate can be used for neurological disease research, such as Alzheimer’s disease .
    Methyllycaconitine citrate
  • HY-B1395
    Mecamylamine hydrochloride
    5 Publications Verification

    nAChR Histamine Receptor Cardiovascular Disease Neurological Disease
    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
  • 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-B1240
    Droperidol
    5 Publications Verification

    Dehydrobenzperidol

    Dopamine Receptor GABA Receptor nAChR Neurological Disease
    Droperidol (Dehydrobenzperidol) is a butyrophenone pamine-2 receptor antagonist that inhibits the activation of GABA(A) and neuronal nicotinic receptors (nAChR), with IC50 values of 12.6 nM and 5.8 μM. Droperidol has anesthetic and sedative properties .
    Droperidol
  • HY-12560A
    PNU-282987
    10+ Cited Publications

    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-14564A
    GTS-21 dihydrochloride
    10+ Cited Publications

    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-B0567

    Potassium Channel nAChR Apoptosis Bacterial Parasite Infection Cancer
    Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity .
    Dequalinium Chloride
  • HY-107670
    Dihydro-β-erythroidine hydrobromide
    1 Publications Verification

    DHβE hydrobromide

    nAChR Neurological Disease
    Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities .
    Dihydro-β-erythroidine hydrobromide
  • 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-B0569
    Hexamethonium Bromide
    4 Publications Verification

    nAChR Apoptosis Cardiovascular Disease Neurological Disease
    Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models .
    Hexamethonium Bromide
  • 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-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-P1050
    COG 133
    2 Publications Verification

    nAChR Neurological Disease Inflammation/Immunology
    COG 133 is a fragment of Apolipoprotein E (APOE) peptide. COG 133 competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC50 of 445 nM .
    COG 133
  • 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-P1050A
    COG 133 TFA
    2 Publications Verification

    Apolipoprotein nAChR Neurological Disease Inflammation/Immunology
    COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM .
    COG 133 TFA
  • HY-N2255
    Crebanine
    4 Publications Verification

    Akt Apoptosis NF-κB Reactive Oxygen Species (ROS) p38 MAPK ERK Interleukin Related TNF Receptor NO Synthase nAChR Bacterial Cancer
    Crebanine is an isoquinoline-like alkaloid that can be derived from Stephania. Crebanine is an antagonist of the α7-nAChR with an IC50 of 19.1 μM. Crebanine suppresses the proliferation, migration, and invasion of cancer cells, triggers reactive oxygen species (ROS) burst, and promotes apoptosis. Crebanine inhibits the AKT/FoxO3a, NF-κB and MAPK signaling pathways. Crebanine attenuates NOX2 hyperactivation, exhibits antioxidant properties by reducing reactive oxygen species and peroxidation in microglia cells. Crebanine inhibits voltage-dependent Na + current in guinea-pig ventricular myocytes. Crebanine has high inhibitory activity against gram-positive animal pathogenic bacteria. Crebanine ameliorates ischemia-reperfusion brain damage in middle cerebral artery occlusion and reperfusion (MCAO/R) rats. Crebanine significantly improves Scopolamine (HY-N0296)-induced cognitive deficits in ICR mice. Crebanine can be used for the study of hepatocellular carcinoma (HCC), cerebral ischemia and Alzheimer's disease .
    Crebanine
  • HY-B0743A

    nAChR Neurological Disease
    Pipecuronium bromide is a potent long-acting nondepolarizing steroidal neuromuscular blocking agent (NMBA), and a bisquaternary ammonium compound. Pipecuronium bromide is a powerful competitive nAChR antagonist with a Kd of 3.06 μM .
    Pipecuronium bromide
  • 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-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-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-W013113

    Environmental Pollutants nAChR Neurological Disease
    BTMPS is a nicotine receptor (nAChR) antagonist that can lessen the negative effects of morphine on rats .
    BTMPS
  • HY-107672

    Stilonium iodide

    nAChR Neurological Disease
    MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM .
    MG624
  • 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-108057A

    RG3487 hydrochloride

    nAChR 5-HT Receptor Neurological Disease
    Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
    Facinicline 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-152170
    bPiDI
    1 Publications Verification

    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-149483

    nAChR Neurological Disease
    CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease .
    CVN417
  • 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-137231B

    nAChR Neurological Disease
    (S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist?and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction .
    (S)-UFR2709 hydrochloride
  • HY-B1395A

    nAChR Histamine Receptor Cardiovascular Disease Neurological Disease
    Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
    Mecamylamine
  • 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-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-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-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 .
    nAChR antagonist 1
  • HY-U00139

    mAChR nAChR Neurological Disease
    Cyclodrine hydrochloride is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.
    Cyclodrine hydrochloride
  • 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-146404

    nAChR Neurological Disease
    T761-0184 is a potent α7 nicotinic receptor (nAChR) antagonist .
    T761-0184
  • HY-107674

    nAChR Neurological Disease
    bPiDDB is a potent nAChR antagonist. bPiDDB potently (IC50=2 nM) inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
    bPiDDB
  • 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-B0567R

    Reference Standards Potassium Channel nAChR Apoptosis Bacterial Parasite Infection Cancer
    Dequalinium (Chloride) (Standard) is the analytical standard of Dequalinium (Chloride). This product is intended for research and analytical applications. Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity .
    Dequalinium Chloride (Standard)
  • 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-180559

    nAChR Interleukin Related Inflammation/Immunology
    nAChR antagonist 2 is a selective nAChR antagonist. nAChR antagonist 2 inhibits nAChR subtype including hα9α10, hα9, and hα7 with IC50 values of 16.0 nM, 26.2 nM, and 336.3 nM, respectively, in Xenopus oocytes. nAChR antagonist 2 suppresses ATP-induced IL-1β release at nanomolar concentrations. nAChR antagonist 2 can be used for nonopioid analgesics and immunomodulators research .
    nAChR antagonist 2
  • 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-182010

    nAChR Neurological Disease
    nAChR antagonist 3 is a selective α7 nAChR antagonist with an IC50 of 0.86 μM. nAChR antagonist 3 exerts a protective effect against paraoxon-induced toxicity. nAChR antagonist 3 can be used for the research of organophosphate poisoning .
    nAChR antagonist 3
  • HY-107679

    nAChR Neurological Disease
    SR 16584 is a selective antagonist of α3β4 nAChR with an IC50 of 10.2 μM .
    SR 16584
  • HY-137231A

    nAChR Neurological Disease
    (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

    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

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