acetylcholine

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.

Acetylcholine iodide (Acetylcolina) is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.

Polygalacic acid (Virgaureagenin G)(PA) significantly improves cholinergic system reactivity, as indicated by decreased acetylcholinesterase (AChE) activity, increases choline acetyltransferase (ChAT) activity, and elevates levels of acetylcholine (ACh) in the hippocampus and frontal cortex, PA also significantly ameliorates neuroinflammation and oxidative stress in mice; suggest that PA might exert a significant neuroprotective effect on cognitive impairment, driven in part by the modulation of cholinergic activity and neuroinflammation. Polygalacic acid shows significant postingestive effects on Spodoptera littoralis larvae.

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

L-Hyoscyamine sulfate (Levsin Sulfate) is the sulfate salt of a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. Hyoscyamine functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

Anisodamine Hydrobromide (6-Hydroxyhyoscyamine) is an anticholinergic and α1-adrenergic receptor antagonist used in the treatment of acute circulatory shock.

Pilocarpine nitrate (Pilagan) is a slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.

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

Pilocarpine Hydrochloride (NSC 5746 HCl) , a nonselective muscarinic acetylcholine receptor agonist, is utilized to produce an experimental model of epilepsy.

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.

Thiamine hydrochloride (Vitamin B1) is the hydrochloride salt form of thiamine, a vitamin essential for aerobic metabolism, cell growth, transmission of nerve impulses and acetylcholine synthesis. Upon hydrolysis, Thiamine hydrochloride (Vitamin B1) is phosphorylated by thiamine diphosphokinase to form active thiamine pyrophosphate (TPP), also known as cocarboxylase. TPP is a coenzyme for many enzymatic activities involving fatty acid, amino acid and carbohydrate metabolism.

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.

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

1. Peimisine (Ebeiensine) can affect M-receptor, excit β-receptor, restrain the release of internal calcium, and promote to releaseing nitrogen monoxidum in order to relax tracheal smooth muscle and relieve asthma. 2. Peimisine can attenuate lung tissue injury( ALI), LDH and MDA amount in ALI mice in a dose dependent manner, it also lower the total protein, total white blood cells, lymphocyte and neutrophilic leukocyte in bronchoalveolar lavage fluid( BALF); suggests that peimisine can play a protective role against LPS-induced acute lung injury. 3. Peimisine has the protective effect on the experimental hepatic fibrosis formation, the possible mechanisms are associated with inhibiting fibrogenesis and fibrosis accumulation, and decreasing lipid peroxidation. 4. Peimisine can inhibit angiotensin I converting enzyme activity in a dose-dependent manner, displaying 5 % inhibitory concentration values of 526.5 microM, thus, it may have antihypertensive action.

sn-Glycero-3-phosphocholine (Choline glycerophosphate) is a natural choline compound found in the brain and in milk. It is also a parasympathomimetic acetylcholine precursor which may have a potential for the treatment of Alzheimer's disease and dementia. sn-Glycero-3-phosphocholine rapidly delivers choline to the brain across the blood–brain barrier and is a biosynthetic precursor of the acetylcholine neurotransmitter. It is a non-prescription drug in most countries due to its Generally Recognised As Safe (GRAS) status [1]. Studies have investigated its efficacy for cognitive disorders including stroke and Alzheimer's disease. An Italian multicentre clinical trial on 2, 044 patients suffering from recent stroke were supplied Glycerylphosphorylcholine in doses of 1, 000 mg/day for 28 days and 400 mg three times per day for the five ensuing months. The trial confirmed the therapeutic role of alpha-GPC on the cognitive recovery of patients based on four measurement scales, three of which reached statistical significance [2].

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

Atropine (DL-Hyoscyamine) Sulfate is the sulfate salt of atropine, a naturally-occurring alkaloid isolated from the plant Atropa belladonna. Atropine functions as a sympathetic, competitive antagonist of muscarinic cholinergic receptors, thereby abolishing the effects of parasympathetic stimulation.

Anethole trithione (Anetholtrithion) is a bile secretion-stimulating drug that restores salivation and relieves the discomfort of dry mouth in chemotherapy-induced xerostomia.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Cyclobuxine D is a steroidal alkaloid extracted from Buxus microphylla. Cyclostatin D has obvious bradycardia effect on rat heart, and inhibits acetylcholine and Ba ++ induced longitudinal muscle contraction isolated from rabbit jejunum.

Marmin have anti-ulcer effects, which are ascribed primarily to the maintenance of the mucosal barrier integrity and inhibition of gastric motor activity and secondarily due to the prevention of the effects of endogenous acetylcholine and histamine.

Fustin is the phytogenic flavanol component of the plant Rhus verniciflua Stokes. Fustin shows protective effects on 6-hydroxydopamine-induced neuronal cell death.

Choline bitartrate (2-hydroxyethyl(trimethyl)azanium) is a form of the nutrient choline which is found in foods. Choline is necessary for normal liver and kidney function and a component of the neurotransmitter acetylcholine, a chemical that facilitates communication between the nerves and muscles.

Atropine sulfate (Sulfatropinol) is a competitive antagonist for muscarinic acetylcholine receptor.

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).

Guvacoline hydrochloride (Norarecoline hydrochloride) is a muscarinic agonist.

Cotoin is a natural product isolated from the stem bark of Garcinia virgate.Cotoin has antispasmodic activity and reduces the tone and contraction of isolated rabbit intestine. It partially inhibits the effects of acetylcholine, trichothecenes and BaCl on the isolated intestine.

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.

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 >

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

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).

(-)-Pluviatolide can inhibit electrically-induced and acetylcholine-induced contraction in the isolated guinea-pig ileum.

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.

Smilagenin acetate is a sapogenin derivative that has been shown to upregulate the expression of the acetylcholine M2 receptor in cell assays, making it a candidate for dementia research.

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,

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

GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD (cGMP sodium salt) , also known as cGMP, is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin. GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD activates protein kinase G (PKG) and modulates ion channel conductance, with signaling affecting diverse processes including smooth muscle relaxation and proliferation, phototransduction, and energy homeostasis.

D-Panthenol (D-Pantothenyl alcohol) is an alcoholic analogue of D-pantothenic acid and cholinergic agent. D-Panthenol acts as a precursor of coenzyme A necessary for acetylation reactions and is involved in the synthesis of acetylcholine. Although the exact mechanism of the actions of D-Panthenol is unclear, it may enhance the effect of acetylcholine. D-Panthenol acts on the gastrointestinal tract and increases lower intestinal motility. It is also applied topically to the skin to relieve itching and to promote healing.

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

Citicoline sodium (CDP-choline) is an endogenous intermediate in the synthesis of phosphatidylcholine. It also serves as a choline donor in the biosynthesis of the neurotransmitter acetylcholine. Citicoline sodium demonstrates protective effects in cerebral ischemia, traumatic brain injury, and memory disorders. Exogenous administration of citicoline to rodents (500 mg/kg i.p. immediately after ischemia and at 3-h reperfusion) has been shown to stimulate the synthesis of phosphatidylcholine, sphingomyelin, and cardiolipin and to attenuate the release of arachidonic acid and the accumulation of ceramide.

Hupehenine is a steriodal alkaloid extracted from the bulbs of Fritillaria Hupehensis, with the potential for inhibiting acetylcholine, antagonism for muscarinic receptors and cholinesterase inhibition.

L-Hyoscyamine (Daturine) functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. Hyoscyamine is a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

Atropine sulfate monohydrate (Atropine sulfate hydrate), the sulfate salt of atropine, is a competitive muscarinic acetylcholine receptor antagonist.

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.

Trifolirhizin exerts varying degrees of inhibition on tyrosinase-dependent melanin biosynthesis, and therefore, are candidates as skin-whitening agents.Trifolirhizin possesses potential anti-inflammatory and anti-cancer activities.Trifolirhizin shows in vitro inhibitory effects on the growth of human A2780 ovarian and H23 lung cancer cells. Trifolirhizin inhibits acetylcholine mediated airway smooth muscle (ASM) contraction or directly relaxes pre-contracted ASM independent of β 2 -adrenoceptors.

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

(R,S)-Anatabine is a minor tobacco alkaloid found in the Solanaceae family and can be used for the detection of specific markers in tobacco use. (R,S)-Anatabine is an agonist of the α4β2 and α6/α3β2β4 subunit nicotinic acetylcholine receptors (nAChRs).

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

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).