nicotinic acetylcholine receptors

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.

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).

(R,S)-Anatabine is a minor tobacco alkaloid found in the Solanaceae family of plants, and serves as a specific marker for detecting tobacco use.

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.

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.

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

(+)-Sparteine (Pachycarpine) is a natural product extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic 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.

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.

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

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.

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.

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.

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

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

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.

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

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

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.

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.

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.

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

SIB 1553A is an orally available and selective agonist of nicotinic acetylcholine receptors (nAChRs), which are subtype-selective ligands for nicotinic acetylcholine receptors.SIB-1553A is a cognitive enhancer that may be used in the study of neurodegenerative-related diseases such as Alzheimer's disease.

[D-Trp7,9,10]-Substance P acetate is an analogue of substance P which inhibits ion conductance through nicotinic acetylcholine receptors.

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.

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

AZD 3043 (THRX 918661) is a variant modulator of the γ-aminobutyric acid type A receptor, a novel sedative-hypnotic and a potential short-acting anesthetic that produces hypnosis and EEG suppression in rats.AZD 3043 potentiates the γ-aminobutyric acid type A receptor and inhibits neuronal nicotinic acetylcholine receptors.

Pyrantel tartrate (Banminth) is broad spectrum anthelmintic for livestock.

PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).

(S)-Coclaurine (Coclaurine) is an antagonist of nAChR isolated from Sarcopetalum harveyanum.

SEN12333 is an α7 nicotinic acetylcholine receptor (nAChR) agonist

A-867744 is an effective and selective type II positive allosteric modulator of the α7 nAChR (EC50: 1.0 μM).

PSEM 89S TFA is a brain-penetrant and selective ion channels agonist, and is orthogonally selective for Q79G and L141F, respectively.

beta-Eudesmol (Beta-Selinenol) is a noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). It is a sesquiterpene that has been found in a variety of plants, including Cannabis, and has diverse biological activities.

suvn-911 is a potent and selective antagonist of neuronal nicotinic acetylcholine α4β2 receptor (Ki = 1.5 nM) with antidepressant activity.

PNU-282987 S enantiomer free base is an agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR).

NS9283 is a positive allosteric modulator of α4β2 receptor.

NS 1738 (NSC-213859) is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nAChRs)

TQS (4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) is a positive allosteric modulator of α7 nACh receptors.

Iptakalim, 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 is also a K(ir) 6.1/SUR2B activator that can attenuate hypoxia-induced pulmonary arterial hypertension in rats by endothelial function protection.

Varenicline dihydrochloride is a Selective α4β2 nicotinic acetylcholine receptor partial agonist.

Varenicline Tartrate (CP 526555-18) is a benzazepine derivative that functions as an ALPHA4 BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.

(-)-(S)-B-973B is an effective allosteric agonist and positive allosteric modulator of α7 nAChR.

α-Conotoxin MII is a highly potent and selective competitive antagonist for α3β2 subunit-containing nicotinic receptors (IC50 = 0.5 - 3.5 nM at α3β2 expressed in Xenopus oocytes). Also potently blocks β3-containing neuronal nicotinic receptors. Displays >

ZSET1446 (ST-101) is a T-type calcium channel activator potentially for the treatment of learning deficits in various types of Alzheimer disease (AD) models.

The quinuclidine PHA 568487 free base is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.

Tropisetron (ICS 205-930) is an α7-nicotinic receptor agonist and 5-HT3 receptor antagonist with Kis of 6.9 nM and 5.3 nM, respectively.

(R)-Dinotefuran ((R)-MTI-446), a neonicotinoid pesticide, demonstrates insecticidal activities 1.7-2.4 times more effective against typical sucking pests like Aphis gossypii and Apolygus lucorum compared to its racemic mixtures, by targeting nicotinic acetylcholine receptors, and is effective in managing these pests while posing a reduced risk to honeybees [1].

(S)-Dinotefuran ((S)-MTI-446), a neonicotinoid pesticide, exhibits toxicity through interaction with the α8 subunit of the nAChR in the honeybee Apis mellifera (Apis mellifera Linnaeus), demonstrating greater toxicity to Apis mellifera compared to its R-dinotefuran counterpart [1].