nicotinic receptor

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.

Arecoline is a natural alkaloid derived from areca nut in the palm family and is a potent nicotine and partial agonist of muscarinic acetylcholine receptors. Arecoline has anti-anxiety and anti-parasitic activity, can induce oxidative stress and can be used to study Alzheimer's disease and Alzheimer's disease.

Anisodamine (6-beta-Hydroxyhyoscyamine) is an antagonist of muscarinic and nicotinic cholinoceptor with similar affinities at the muscarinic receptor as scopolamine and atropine. Anisodamine improve the microcirculation in states of shock and can be used in studies about organophosphate poisoning.

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

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.

Catharanthine inhibits nicotinic receptor-mediated diaphragm contractions.

Coniine hydrochloride, a polyketide-derived alkaloid, is poisonous to humans and animals. It is a nicotinic acetylcholine receptor antagonist, which leads to inhibition of the nervous system.

(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.

Hirsuteine is a natural product. It non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes.

Lupanine ((+)-Lupanine), a naturally occurring quinolizidine alkaloid, potently affinity and activates nicotinic acetylcholine receptor (nAChR) (Ki=500 nM), and shows significant neuroprotection against soluble amyloid β-oligomers (SO-Aβ) toxicity in cellular models in association with the anti-apoptotic PI3K Akt Bcl-2 signaling pathway with anti-Alzheimer's disease potential. Improves glucose homeostasis by affecting KATP channels and enhancing insulin secretion with therapeutic potential for type 2 diabetes.

Cotinine (NIH-10498) is an alkaloid found in tobacco and is also the predominant metabolite of nicotine.

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].

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.

Dihydro-β-erythroidine, a competitive nicotinic receptor antagonist, effectively blocks the discriminative stimulus properties and inhibits the anxiolytic effects induced by nicotine.

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

Lobeline hydrochloride (α-Lobeline hydrochloride) is a nicotinic receptor agonist, acting as an effective antagonist at both α4β2 and α3β2 neuronal nicotinic receptor subtypes.

Gardneramine has a mild central depressive effect. Gardneramine and hirsutine show a local anesthetic action, they also can inhibit the ganglionic transmission of the dog urinary bladder and that the blockade of the nicotinic receptor plays a main role.

Microgrewiapine A is a selective cytotoxic agent for colon cancer cells over normal colon cells and to exhibit nicotinic receptor antagonistic activity for both the hα3β4 and hα4β2 receptor subtypes.

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).

Kynurenic acid (Quinurenic acid) is an endogenous tryptophan active metabolite, a triple antagonist of NMDA, glutamate, α7 nicotinic acetylcholine receptor, and an agonist of GPR35 CXCR8 with neuroprotective and anticonvulsant properties. It has neuroprotective and anticonvulsant properties and can be used to study neurodegeneration and metabolism-related diseases.

Lupanine hydrochloride, a natural ketonic derivative of Sparteine ((+)-Sparteine), exhibits ganglioplegic activity and binds to the nicotinic receptor (nAChR) with a K i value of 500 nM [1].