nAChR inhibitor

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

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

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

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.

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.

(+)-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.

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.

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).

Vinblastine sulfate (Vincaleukoblastine sulfate salt) can inhibit the formation of microtubule, it also inhibits nAChR(IC50=8.9 uM).

(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.

Catharanthine ((+)-3,4-Didehydrocoronaridine) suppresses nicotinic receptor-mediated diaphragm contractions with an IC50 of 59.6 μM.

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.

1. N-Methylcytisine (Caulophylline)'s nicotinic receptors have high affinity (KD = 5 nM)to nAChR from squid optical ganglia. 2. N-Methylcytisine and N, N-dimethylcytisine did not displace 14C-tubocurarine at a concentration of .1 mM, cytisine was the only effective inhibitor of 14C-tubocurarine specific binding (Ki=7 nM).

Myosmine is a minor tobacco alkaloid that is structurally related to nicotine.

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

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

Anatoxin-a (ATX-a), a neurotoxic alkaloid, functions as an agonist for the nicotinic acetylcholine receptor (nAChR) and as an inhibitor of Acetylcholinesterase (AChE) [1] [2].

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 >