nachr

nAChR agonist 1 (DUN71755) is a brain-permeable and orally efficacious positive allosteric α7 nicotinic acetylcholine receptor (α7 nAChR)modulator.

Compound 8, identified as a selective alpha4beta2 (α4β2) neuronal acetylcholine receptor (nAChR) agonist, demonstrates a dissociation constant (Kd) of 26 nM, indicating high affinity for this receptor subtype.

nAChR antagonist 1 (compound B15) is a highly effective antagonist of α7 nAChR, with an IC50 value of 3.3 μM, making it an ideal candidate for investigating the pathogenesis of schizophrenia, Alzheimer's disease, and inflammatory disorders [1].

α7 nAchR-JAK2-STAT3 agonist 1 is a potent inhibitor of the α7 nAchR-JAK2-STAT3 pathway that acts on nitric oxide (NO) (IC50: 0.32 μM). It has demonstrated positive effects on iNOS, IL-1β, and IL-1β in murine macrophages RAW264.7, and inhibited the expression of iNOS, IL-1β, and IL-6 in mouse macrophages. Additionally, α7 nAchR-JAK2-STAT3 agonist 1 suppressed LPS-induced NO release, NF-κB activation, and cytokine production, making it useful for studying sepsis.

CMPI hydrochloride, a potent and selective nAChR agonist, functions as a positive allosteric modulator (PAM) specifically targeting the α4:α4 subunit interface of the nAChR. It enhances the response of the (α4)3(β2)2 nAChR to acetylcholine (ACh) (10 μM) with an EC 50 of 0.26 μM. With its potential for researching nicotine dependence and various neuropsychiatric conditions linked to reduced brain cholinergic activity, CMPI hydrochloride stands as a significant compound in neurological research.

nAChR modulator-1, an insecticide, is an orthosteric modulator of insect nAChRs [1].

nAChR modulator-2, an insecticide, functions as an orthosteric modulator of insect nAChR [1].

Cyclodrine (Cyclopent) is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.

Desformylflustrabromine hydrochloride (dFBr hydrochloride) is a selective agonist of nicotinic acetylcholine receptor (nAChR) in α4β2 neurons, with pEC50 of 6.48.

SAK3 is a novel modulator of nAChR activity that enhances T-type voltage-gated Ca2+ channel (T-VGCC) activity, and has potentiating effects on both Cav3.1 and Cav3.3 T-type Ca2+ channel currents.SAK3 is neuroprotective against scopolamine-induced cholinergic dysfunction in human neuroblastoma SH-SY5Y cells.SAK3 is used for the study of memory deficits and Alzheimer's disease. SAK3 can be used to study memory deficits and Alzheimer's disease.

Cynandione A, an acetophenone derived from Cynanchum wilfordii, has anti-inflammatory activity and significantly reduces pro-inflammatory cytokine overexpression via macrophage α7 nAChR activation and subsequent IL-10 expression.

PHA 543613 is a specific agonist of α7 nAChR (Ki = 8.8 nM) and can be used in studies about the cognitive deficits of Alzheimer's disease and schizophrenia.

SIB-1553A hydrochloride is an orally available, selective nicotinic acetylcholine receptor agonist and a selective neuronal nAChR ligand.SIB-1553A hydrochloride enhances cognition and may be useful in the study of Alzheimer's disease and cognitive impairment.

CP-810123 is a new alpha 7 nAChR agonist for the treatment of cognitive impairment associated with psychiatric or neurological disorders such as schizophrenia and Alzheimer's disease.

Simpinicline (OC-02) (OC-02) is a highly selective nicotinic acetylcholine receptor (nAChR) agonist that activates the trigeminal parasympathetic pathway and can be used to treat dry eye.

Spinosad is a naturally-occurring insecticide found in the the soil bacterium S. spinosa. It is a mixture of the macrocyclic lactones spinosyn A and spinosyn D, which act as agonists of insect nicotinic acetylcholinesterase receptors (nAChRs).

Clothianidin (TI 435), an insecticide, acts as an agonist of acetylcholine to stimulate nAChR, thereby activating post-synaptic acetylcholine receptors but not inhibiting AChE.

Atracurium besylate (51W89) is a non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

Cytisinicline (Sophorine), an alkaloid, is found naturally in several plants.

Hexamethonium Bromide (Hexamethonium Dibromide), a specific antagonist of neuronal-type nicotinic AChR in ganglia, is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier.

Decamethonium bromide (Syncurine) is a neuromuscular blocker and nicotinic AChR partial agonist.

Dinotefuran (MTI-446) is an insecticide of the neonicotinoid class for control of insect pests such as aphids, whiteflies, thrips, leafhoppers, leafminers. Its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.

(+)-Sparteine ​​is a quinoline alkaloid extracted from Scotch broom, a sodium channel blocker and a class 1a antiarrhythmic agent. It competitively inhibits the activity of nicotinic acetylcholine receptors in nerve cells and is a ganglionic blocking agent.

Carbachol (Carbamoylcholine chloride), an analog of acetylcholine, serves as a valuable tool in the investigation of various physiological responses mediated by nicotinic (nAChR) and muscarinic (mAChR) acetylcholine receptors. These responses include smooth muscle contraction, gut motility, and neuronal signaling. Known for its agonistic properties, Carbachol activates both nAChR and mAChR, with reported Ki values ranging from 10 to 10,000 nM for different receptor types and experimental preparations.

Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.

Vecuronium bromide (ORG NC 45) is a synthetic, intermediate-acting, mono-quaternary steroid that functions as a non-depolarizing neuromuscular blocking agent with muscle relaxant properties.

Benzethonium chloride (Quatrachlor) is a synthetic quaternary ammonium salt with surfactant, antiseptic, and broad spectrum antimicrobial properties.

Aniracetam (Ro 13-5057)(Ro 13-5057), a nootropic and neuroprotective drug, selectively modulates the AMPA receptor and nAChR.

Cholesterol Myristate (Cholesteryl Myristate) is a natural steroid found in traditional Chinese medicine that interacts with various ion channels, including the GABAA receptor, nicotinic acetylcholine receptor, and the inward-rectifier potassium ion channel.

Procaine hydrochloride (Novocaine HCl) is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodiumchannels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.

Nitenpyram (Capstar) is a nicotinic acetylcholine receptor (AchR) agonist, used as veterinary medicine to treat parasites of livestock and pets.

Choline chloride (Biocoline) is a basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.

Cisatracurium besylate (51W89) is a nondepolarizing skeletal muscle relaxant intended for intravenous administration.

Urethane (Ethylurethane) was an antineoplastic agent .Now is used for other medicinal purposes.

Acetylcholine Chloride is the chloride salt form of acetylcholine, a synthetic, quaternary amino alcohol with cholinergic properties. Acetylcholine chloride (Pilofrin) mimics the parasympathomimetic effect of the endogenous compound acetylcholine. Administered as an ophthalmic solution, this drug stimulates the cholinoceptors in the sphincter muscle of the iris, causing the pupil to constrict.

Arecoline hydrobromide (Arecoline HBr) is a muscarinic acetylcholine receptor agonist.

Adiphenine hydrochloride (Patrovina), a nicotinic receptor inhibitor, can be used as an antispasmodic drug.

Pancuronium dibromide (Pavulon), a competitive AChR antagonist (IC50 = 5.5 nM), acts as a skeletal muscle relaxant. Pancuronium dibromide(Pancuronium bromide) blocking neuromuscular transmission is achieved by competing with acetylcholine for receptor sites on the motor end-plate.

Meclofenoxate hydrochloride (Lucidril) is an ester of DIMETHYLAMINOETHANOL and para-chlorophenoxyacetic acid. It has been shown to improve memory and general cognition, and mentally stimulating effect.

Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist. Acetamiprid is a neonicotinoid insecticide used worldwide. It is shown to be associated with neuromuscular and reproductive disorders.

Pyrantel pamoate (Pyrantel embonate) is a depolarizing neuromuscular blocking agent. This compound is commonly used as an anthelmintic to treat parasitic worm infections, effectively paralyzing nematodes by inhibiting their neuromuscular activity.

α-Conotoxin GI acetate is a competitive antagonist of the muscle-type nicotinic acetylcholine receptors (nAChR).

α-Conotoxin MII acetate is a 16-amino acid peptide from the venom of the marine snail Conus magus. α-Conotoxin MII acetate potently blocks nicotinic acetylcholine receptors composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII acetate potently blocks β3-containing neuronal nicotinic acetylcholine receptors.

(-)-Coclaurine hydrochloride is an antagonist of nAChRs isolated from Sarcopetalum harveyanum.

Lobelanidine (8,10-Diphenyllobelidiol), which can be extracted from the above-ground parts of Lobelia chinensis Lour and Lobelia tupa, is an analogue of lobeline and shows a moderate affinity for nAChR.

α-Conotoxin PIA acetate is an antagonist of nicotinic acetylcholine receptor (nAChR) mainly targeting α6 and α3 subunits.

Ferulamide (4-Hydroxy-3-methoxycinnamide), a Ferulic acid derivative, shows potent inhibitory activity against arachidonic acid-induced platelet aggregation.

UB 165 fumarate is an agonist of the nAChR, a partial agonist of the α4β2 subtype, and a full agonist of the α3β2 subtype, with a Ki value of 0.27 nM for binding to [3H]-nicotine measured in rat brain.