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nAChR Inhibitor

" in MedChemExpress (MCE) Product Catalog:

75

Inhibitors & Agonists

1

Screening Libraries

7

Peptides

13

Natural
Products

4

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0282
    Acetylcholine chloride
    20+ Cited Publications

    ACh chloride

    		 nAChR Calcium Channel Endogenous Metabolite Infection Neurological Disease Cancer
    Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
    Acetylcholine chloride
  • HY-15310
    Ivermectin
    Maximum Cited Publications
    48 Publications Verification

    MK-933; CD-5024; K-237

    		 Environmental Pollutants Antibiotic Mitophagy Bacterial Parasite Autophagy Flavivirus HSV HIV SARS-CoV Dengue Virus Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
    Ivermectin
  • HY-13780
    Vinblastine sulfate
    15+ Cited Publications

    Vincaleukoblastine sulfate salt

    		 Microtubule/Tubulin nAChR Autophagy Cancer
    Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
    Vinblastine sulfate
  • 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-B0118A
    Vecuronium bromide

    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-B0282S
    Acetylcholine-d4 chloride

    ACh-d4 chloride

    		 nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
    Acetylcholine-d4 chloride
  • HY-A0009
    Galanthamine hydrobromide
    10+ Cited Publications

    Galantamine hydrobromide

    		 Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
    Galanthamine hydrobromide
  • HY-14774
    Monepantel
    1 Publications Verification

    AAD1566; NUZ-001

    		 mTOR Parasite nAChR Autophagy Infection Neurological Disease Cancer
    Monepantel (AAD1566, NUZ-001), an antiparasitic agent, is an orally active mTOR inhibitor. Monepantel triggers autophagy through the deactivation of mTOR/p70S6K signalling pathway. Monepantel is a positive allosteric modulator of a nematode-specific clade of nAChR subunits. Monepantel can be used for the study of amyotrophic lateral sclerosis (ALS) and ovarian cancer .
    Monepantel
  • HY-P0102
    Dipeptide diaminobutyroyl benzylamide diacetate

    		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-125159
    Derquantel

    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-B1700A
    Mivacurium dichloride

    		nAChR Neurological Disease
    Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell .
    Mivacurium dichloride
  • HY-172236
    Soclenicant

    BNC210; IW-2143

    		 nAChR Neurological Disease
    Soclenicant (BNC210) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. Soclenicant exhibits acute anxiolytic activity in rodent models of anxiety. Soclenicant inhibits rat and human α7 nAChR currents (in stably transfected cell lines) induced by acetylcholine, nicotine, choline, and the a7-specific agonist PNU-282987 (HY-12560A) with IC50 values in the range of 1.2 to 3 μM. Soclenicant can be used in studies of anxiety, trauma, and stressor-related disorders .
    Soclenicant
  • HY-B0379A
    Adiphenine hydrochloride
    3 Publications Verification

    		 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-116522
    AR420626
    4 Publications Verification

    		 Free Fatty Acid Receptor Histone Methyltransferase HDAC mTOR CaMK p38 MAPK Epigenetic Reader Domain GLUT nAChR TNF Receptor Metabolic Disease Inflammation/Immunology Cancer
    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC50=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca 2+ signal-mediated glucose uptake and improve diabetes .
    AR420626
  • HY-14316A
    Tebanicline dihydrochloride

    Ebanicline dihydrochloride; ABT-594 dihydrochloride

    		 nAChR Neurological Disease
    Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
    Tebanicline dihydrochloride
  • 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-B0827
    Dinotefuran
    4 Publications Verification

    MTI-446

    		 Environmental Pollutants Parasite nAChR Infection Cardiovascular Disease
    Dinotefuran is an orally active and competitive inhibitor and insecticide targeting insect nicotinic acetylcholine receptors (nAChRs). Dinotefuran blocks neural signaling and induces neural dysfunction in insects. Dinotefuran binds to [ 3H]epibatidine in the neural cord membrane of American cockroach with an IC50 of 890 nM and to [ 3H]α-bungarotoxin with an IC50 of 36.1 μM. Dinotefuran exhibits knockdown activity (KD50=0.351 nmol/g) and lethal activity (LD50=0.173 nmol/g) against German cockroach. Dinotefuran is mainly used for agricultural pest control, such as field control of piercing-sucking and chewing insects (e.g., aphids, planthoppers), while its environmental toxicological effects (e.g., oxidative stress and reproductive neurotoxicity on earthworms) are also a research focus to assess ecological risks .
    Dinotefuran
  • HY-146066
    α7 nAchR-JAK2-STAT3 agonist 1

    		nAChR JAK STAT NO Synthase Interleukin Related Inflammation/Immunology
    α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
    α7 nAchR-JAK2-STAT3 agonist 1
  • HY-18060
    Bradanicline

    TC-5619

    		 nAChR Neurological Disease
    Bradanicline (TC-5619) is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
    Bradanicline
  • HY-105118A
    Zaldaride maleate

    CGS-9343B; KW 5617

    		 Calmodulin Neurological Disease Metabolic Disease Inflammation/Immunology
    Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM . Zaldaride maleate prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR .
    Zaldaride maleate
  • HY-B0282S1
    Acetylcholine-d9 chloride

    ACh-d9 chloride

    		 nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
    Acetylcholine-d9 chloride
  • HY-106901A
    Asoxime dichloride

    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

    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-13780R
    Vinblastine sulfate (Standard)

    Vincaleukoblastine sulfate salt (Standard)

    		 Reference Standards Microtubule/Tubulin Autophagy nAChR Cancer
    Vinblastine (sulfate) (Standard) is the analytical standard of Vinblastine (sulfate). This product is intended for research and analytical applications. Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
    Vinblastine sulfate (Standard)
  • HY-B0282R
    Acetylcholine chloride (Standard)

    ACh chloride (Standard)

    		 Reference Standards nAChR Calcium Channel Endogenous Metabolite Neurological Disease Cancer
    Acetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
    Acetylcholine chloride (Standard)
  • HY-N8249
    Cynandione A

    		nAChR Interleukin Related Inflammation/Immunology
    Cynandione A is an acetophenone that can be isolated from Cynanchum Wilfordii Radix. Cynandione A protects hepatocytes and cortical neurons from toxicity and improves neurological deficits in a rat model of cerebral ischemia. On the other hand, cynandione A has significant anti-inflammatory effects and inhibits inflammation by activating macrophage α7 nAChR and IL-10 expression .
    Cynandione A
  • HY-161671
    GAT2711

    		nAChR Neurological Disease Inflammation/Immunology
    GAT2711 is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 shows 340-fold selective for α9 over α7 nAChRs. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells. GAT2711 retains full analgesic activity in α7 nAChR knockout mice .
    GAT2711
  • 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-17590
    Radafaxine hydrochloride
    1 Publications Verification

    (S,S)-Hydroxybupropion hydrochloride; GW-353162A; BW-306U

    		 Monoamine Transporter Neurological Disease
    Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
    Radafaxine hydrochloride
  • HY-149483
    CVN417

    		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-P5823
    Azemiopsin

    		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-146066A
    (R)-α7 nAchR-JAK2-STAT3 agonist 1

    		nAChR JAK STAT NO Synthase Others
    (R)-α7 nAchR-JAK2-STAT3 agonist 1 is the R-enantiomer of α7 nAchR-JAK2-STAT3 agonist 1 (HY-146066). α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
    (R)-α7 nAchR-JAK2-STAT3 agonist 1
  • HY-P1271A
    Catestatin TFA

    		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-126049
    (S)-Oxiracetam

    (S)-(-)-Oxiracetam; (S)-ISF2522

    		 Apoptosis Neurological Disease
    (S)-oxiracetam (S-ORC) is an inhibitor targeting apoptosis. S-ORC reduces brain infarct size and lessens neurological dysfunction in middle cerebral artery occlusion/reperfusion (MCAO/R) models. S-ORC prevents neuronal apoptosis via activating PI3K/Akt/GSK3β signaling pathway via α7 nAChR after ischemic stroke. S-ORC can prevent neuronal death after ischemic stroke .
    (S)-Oxiracetam
  • 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-175607
    AChE/nAChR-IN-1

    		Cholinesterase (ChE) nAChR Infection Neurological Disease
    AChE/nAChR-IN-1 (Compound 1a) is dual-functional inhibitor of AChE and nAChR. AChE/nAChR-IN-1 has potent toxicity and larvicidal effectiveness against Culex pipiens larvae with a LC50 of 4 ng/mL. AChE/nAChR-IN-1 can be used as larvicides for mosquito-borne diseases research .
    AChE/nAChR-IN-1
  • HY-151129
    nAChR-IN-1

    		nAChR Neurological Disease
    nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) 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 .
    nAChR-IN-1
  • HY-114791
    Lobelanidine

    		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-107674
    bPiDDB

    		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-P10898
    GeX-2

    		nAChR Calcium Channel GABA Receptor Neurological Disease
    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-19918A
    Anatabine dicitrate
    1 Publications Verification

    		 NF-κB Amyloid-β nAChR Neurological Disease Inflammation/Immunology
    Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
    Anatabine dicitrate
  • HY-171807
    TC-2559 free base

    		nAChR STAT Neurological Disease Inflammation/Immunology
    TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain .
    TC-2559 free base
  • HY-A0009R
    Galanthamine hydrobromide (Standard)

    Galantamine hydrobromide (Standard)

    		 nAChR Cholinesterase (ChE) Reference Standards Neurological Disease
    Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
    Galanthamine hydrobromide (Standard)
  • HY-W856819
    Eseroline

    		Opioid Receptor Cholinesterase (ChE) Drug Metabolite nAChR Neurological Disease
    Eseroline is a potent μ-opioid receptor agonist, which is the hydrolytic metabolite of Physostigmine (HY-N6608). Eseroline is a selective and competitive acetylcholinesterase (AChE) inhibitor, with its Ki values for AChE and BuChE being 0.1 μM and 200 μM respectively. Eseroline has nicotinic acetylcholine receptor allosteric enhancing ligand (nAChR-APL) activity, meaning it does not activate the receptor but significantly enhances the signal transduction of Ach triggered by the receptor. Eseroline is neurotoxic, causing cell membrane damage (LDH leakage) and energy metabolism collapse (ATP depletion). Eseroline can be used for the study of Alzheimer's disease .
    Eseroline
  • HY-59201A
    A-582941 dihydrochloride

    		ERK 5-HT Receptor Epigenetic Reader Domain nAChR Neurological Disease Metabolic Disease
    A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia .
    A-582941 dihydrochloride
  • HY-B0118AR
    Vecuronium bromide (Standard)

    ORG NC 45 (Standard)

    		 Reference Standards nAChR Neurological Disease Cancer
    Vecuronium (bromide) (Standard) is the analytical standard of Vecuronium (bromide). This product is intended for research and analytical applications. 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 (Standard)
  • HY-N12511
    Aristoquinoline

    		nAChR Neurological Disease
    Aristoquinoline (Compound 1) is an alkaloid can be isolated from Aristotelia chilensis. Aristoquinoline has α3β4 nAChR inhibitory activity .
    Aristoquinoline
  • HY-107669
    nAChR-IN-1 hydrochloride

    		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 .
    nAChR-IN-1 hydrochloride
  • HY-14316B
    Tebanicline hydrochloride

    Ebanicline hydrochloride; ABT-594 hydrochloride

    		 nAChR Neurological Disease
    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-157958
    α7 nAChR Modulator-3

    		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 nAChR Modulator-3

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