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.

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 >

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).

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

(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.

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.

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.

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

Dihydro-β-erythroidine hydrobromide(DHβE) is a potent, oral active and competitive antagonist of neuronal nicotinic acetylcholine receptors (nAChRs). Dihydro-β-carotene hydrobromide showed selectivity to α4β4 and α4β2nAChR, with IC50 of 0.19 and 0.37 μM,

Thiocolchicoside (Thiocolchicine 2-glucoside analog) (Muscoril, Myoril, Neoflax) is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive GABAA receptor antagonist and also glycine receptor antagonist with similar potency and nicotinic acetylcholine receptors to a much lesser extent. It has powerful convulsant activity and should not be used in seizure-prone individuals.

(S)-Laudanosine is the corresponding isomer of Laudanosine, which crosses the blood-brain barrier, causing euphoria and seizures, with potential systemic toxicity and analgesic effects. In the cardiovascular system, high plasma concentrations can lead to hypotension and bradycardia.Laudanosine interacts with γ-aminobutyric acid, opioid, and nicotinic acetylcholine receptors, and inhibits the low-affinity GABA receptor, as well as competitively binds to the opioid receptor Mu-1 receptor.

(+)-Sparteine (sulfate pentahydrate) is a ganglion blocker that competitively inhibits nicotinic acetylcholine receptors in neurons.

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).

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

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

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.

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

Aspergillimide is a fungal metabolite originally isolated from A. japonicus.1 It reduces nicotinic acetylcholine receptor (nAChR) peak and slowly-desensitizing amplitudes induced by acetylcholine in silkworm (B. mori) larval neurons (IC50s = 20.2 and 39.6 nM, respectively) but has no effect on chicken α3β4-, α4β2-, and α7-containing nAChRs.2 Dietary administration of aspergillimide A (10 μg/g of diet) induces paralysis in silkworm fourth instar larvae.1 Aspergillimide A (10 and 20 mg/kg) reduces T. colubriformis fecal egg count in gerbils.3References1. Hayashi, H., Nishimoto, Y., Akiyama, K., et al. New paralytic alkaloids, asperparalines A, B and C, from Aspergillus japonicus JV-23. Biosci. Biotechnol. Biochem. 64(1), 111-115 (2000).2. Hirata, K., Kataoka, S., Furutani, S., et al. A fungal metabolite asperparaline a strongly and selectively blocks insect nicotinic acetylcholine receptors: The first report on the mode of action. PLoS One 6(4), e18354 (2011).3. Banks, R.M., Blanchflower, S.E., Everett, J.R., et al. Novel anthelmintic metabolites from an Aspergillus species; the aspergillimides. J. Antibiot. (Tokyo) 50(10), 840-846 (1997). Aspergillimide is a fungal metabolite originally isolated from A. japonicus.1 It reduces nicotinic acetylcholine receptor (nAChR) peak and slowly-desensitizing amplitudes induced by acetylcholine in silkworm (B. mori) larval neurons (IC50s = 20.2 and 39.6 nM, respectively) but has no effect on chicken α3β4-, α4β2-, and α7-containing nAChRs.2 Dietary administration of aspergillimide A (10 μg/g of diet) induces paralysis in silkworm fourth instar larvae.1 Aspergillimide A (10 and 20 mg/kg) reduces T. colubriformis fecal egg count in gerbils.3 References1. Hayashi, H., Nishimoto, Y., Akiyama, K., et al. New paralytic alkaloids, asperparalines A, B and C, from Aspergillus japonicus JV-23. Biosci. Biotechnol. Biochem. 64(1), 111-115 (2000).2. Hirata, K., Kataoka, S., Furutani, S., et al. A fungal metabolite asperparaline a strongly and selectively blocks insect nicotinic acetylcholine receptors: The first report on the mode of action. PLoS One 6(4), e18354 (2011).3. Banks, R.M., Blanchflower, S.E., Everett, J.R., et al. Novel anthelmintic metabolites from an Aspergillus species; the aspergillimides. J. Antibiot. (Tokyo) 50(10), 840-846 (1997).

Anagyrine hydrochloride ((-)-Anagyrine hydrochloride), a quinolizidine alkaloid discovered in Lupinus albus, interacts with both muscarinic and nicotinic acetylcholine receptors, demonstrating IC50 values of 132 and 2096 µM, respectively. This compound is recognized for its potent and direct ability to desensitize nAChR without the need for metabolic activation [1] [2] [3].

Nereistoxin (Nereistoxine), a neurotoxin derived from Lumbriconereis heteropoda, a marine annelid, functions by inhibiting nicotinic acetylcholine receptors [1].

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

Anabasine ((S)-Anabasine) is an alkaloid extracted from tobacco, acting as a full agonist of nicotinic acetylcholine receptors (nAChRs) with insecticidal activity. It depolarizes TE671 cells that endogenously express human myotypic nAChRs.