nAChR Inhibitor

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.

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 Ca²⁺ signal-mediated glucose uptake and improve diabetes.

Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes, which has antibacterial, anticancer, antisepsis and disinfection activity. Benzethonium chloride induced Apoptosis and activated caspases in cancer cell lines. Benzethonium chloride ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors in vivo.

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.

Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

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.

Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. Spinosad has an excellent environmental and mammalian toxicological profile. Larvicidal activity.

Meclofenoxate (Centrophenoxine) hydrochloride is an ester synthesized from DMAE and pCPA, capable of crossing the blood-brain barrier, and can stimulate memory and enhance cognition.

(+)-Sparteine is a natural alkaloid acting as a ganglionic blocking agent. (+)-Sparteine competitively blocks nicotinic ACh receptor in the neurons.

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.

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.

Anti-Human/Rat/Fish AChR Antibody (Mab35) is an anti-human/rat/fish AChR IgG1 monoclonal antibody. Anti-Human/Rat/Fish AChR Antibody (Mab35) can attack the AChR of neuromuscular junctions. Anti-Human/Rat/Fish AChR Antibody (Mab35) can be used for the construction of myasthenia gravis models.

Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation.

Catestatin human, a catecholamine release-inhibitory peptide, is a pleiotropic peptide involved in cardiovascular protection with its antihypertensive and angiogenic effects. Catestatin human can be used in the study of inflammatory diseases .

Bupropion morpholinol-d6 is the deuterated form of Bupropion morpholinol. Bupropion morpholinol is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities.

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.

Lupanine (D-Lupanine) is a natural ketonic derivative of Sparteine (HY-W008350) with a ganglioplegic activity. Lupanine shows binding affinity for nicotinic receptor with a K_i value of 500 nM.

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.

Thiamethoxam (Standard) is the analytical standard of Thiamethoxam. This product is intended for research and analytical applications. Thiamethoxam is a broad spectrum neonicotinoid insecticide.

Triflumezopyrim, a mesoionic insecticide, has high efficiency at a low dosage, and is mainly used to control hopper species. Triflumezopyrim mainly acts on the nicotinic acetylcholine receptor (nAChR) inhibition, which is very highly efficient, rapidly effective, and nearly nontoxic to nontarget arthropods.