88 Results for "

nAChR Inhibitor

" in MedChemExpress (MCE) Product Catalog:
Products (88)

88 Results for "nAChR Inhibitor" in MCE Product Catalog:

  • Targets Recommended:
50
50 Publications Verification
Cat. No.: HY-15310
CAS No.: 70288-86-7
Purity:  98.28%
Synonyms: MK-933; CD-5024; K-237
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 .
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48
48 Cited Publications
Cat. No.: HY-N2332A
CAS No.: 351344-10-0
Synonyms: MLA citrate
Methyllycaconitine (MLA) citrate is a blood-brain barrier-permeable antagonist of α7 nicotinic acetylcholine receptor (α7nAChR) with an IC50 of 2 nM. Methyllycaconitine citrate inhibits25-35-induced autophagy by restoring the mTOR pathway, and prevents reactive oxygen species (ROS) production, microglial activation, reduced dopamine uptake, loss of dopaminergic terminals and catecholamine secretion. Methyllycaconitine citrate induces hippocampal glutamate efflux, enhances long-term potentiation, and improves memory acquisition. Methyllycaconitine citrate can be used in research related to Alzheimer's disease, cerebral palsy, Parkinson's disease and schizophrenia .
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28
28 Cited Publications
Cat. No.: HY-B0282
CAS No.: 60-31-1
Synonyms: ACh 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 .
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19
19 Cited Publications
Cat. No.: HY-13780
CAS No.: 143-67-9
Purity:  99.86%
Synonyms: Vincaleukoblastine sulfate salt
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.
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15
15 Cited Publications
Cat. No.: HY-A0009
CAS No.: 1953-04-4
Synonyms: Galantamine hydrobromide
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) .
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14
14 Cited Publications
Cat. No.: HY-15136
CAS No.: 193275-84-2
Purity:  99.60%
Synonyms: Sch66336
Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria .
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5
5 Cited Publications
Cat. No.: HY-B1240
CAS No.: 548-73-2
Synonyms: Dehydrobenzperidol
Research Areas:  

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 .
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5
5 Cited Publications
Cat. No.: HY-N2255
CAS No.: 25127-29-1
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 .
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4
4 Cited Publications
Cat. No.: HY-116522
CAS No.: 1798310-55-0
Purity:  98.29%
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 .
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4
4 Cited Publications
Cat. No.: HY-B0827
CAS No.: 165252-70-0
Synonyms: MTI-446
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 .
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3
3 Cited Publications
Cat. No.: HY-B0379A
CAS No.: 50-42-0
Target:  

nAChR

Research Areas:  

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 .
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2
2 Cited Publications
Cat. No.: HY-W052144
CAS No.: 13078-04-1
(±) Anabasine is the racemic form of Anabasine (HY-B1532). (±) Anabasine stimulates the release of [ 3H]-Dopamine from mouse striatal synaptosomes. (±) Anabasine inhibits the high-affinity binding of [ 3H]-S-(-)-Nicotine to the striatal membrane. Anabasine is an agonist of α7nAChR and possesses anti-inflammatory and insecticidal activities .
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1
1 Cited Publications
Cat. No.: HY-14774
CAS No.: 887148-69-8
Purity:  99.98%
Synonyms: AAD1566; NUZ-001
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 .
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1
1 Cited Publications
Cat. No.: HY-152170
CAS No.: 525596-64-9
Purity:  99.65%
Target:  

nAChR

Research Areas:  

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 .
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1
1 Cited Publications
Cat. No.: HY-17590
CAS No.: 106083-71-0
Synonyms: (S,S)-Hydroxybupropion hydrochloride; GW-353162A; BW-306U
Target:  

Monoamine Transporter

Research Areas:  

Neurological Disease

Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
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1
1 Cited Publications
Cat. No.: HY-106901AS
Purity:  ≥96.0%
Synonyms: HI-6-d4
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.
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1
1 Cited Publications
Cat. No.: HY-19918A
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 .
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Cat. No.: HY-B0118A
CAS No.: 50700-72-6
Synonyms: ORG NC 45
Target:  

nAChR

Research Areas:  

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 .
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Cat. No.: HY-B0282S
CAS No.: 344298-94-8
Synonyms: ACh-d4 chloride
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 .
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Cat. No.: HY-P0102
CAS No.: 823202-99-9
Target:  

nAChR

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 .
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