Nicotinic Acetylcholine Receptor Modulators

Nicotinic acetylcholine receptors (nAChRs) activate ion channels through the binding of nicotine. This binding causes the channel to open, allowing positively charged sodium ions to enter and positively-charged potassium ions to exit the cell. For several decades, nAChRs served as prototypic molecules for neurotransmitter receptors. Current research suggests they may also be important therapeutic targets for Alzheimer′s and Parkinson′s disease, schizophrenia, as well as lung cancer. Sigma-Aldrich offers several bioactive small molecules with agonistic or antagonistic effects to research the pharmacological activities of nicotinic acetylcholine receptors

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SML1167 4BP-TQS ≥98% (HPLC) 4BP-TQS is an atypical agonist of a7-nAChR that binds to the receptor in an intrasubunit cavity, and activates the channel via a mechanism that is distinct from conventional agonists. Maximal activation of a7-nAChR by 4BP-TQS is eight fold greater than activation by a maximum dose of acetylcholine (Ach), and 4BP-TQS can poteniate an EC10 concentration of ACh to invoke a response that is 540-fold higher than the maximal dose of ACh alone.
SML1487 ABT-089 dihydrochloride ≥98% (HPLC) ABT-089 (Pozanicline) is a subtype-selective neuronal nicotinic receptor partial agonist binding primarily to the α4β2 and also α6β2 subtypes. It has been investigated for alleviating symptoms of nicotine withdrawal including cognitive deficits and anxiety.
A6476 ABT-418 hydrochloride powder, ≥98% (HPLC) Neuronal nicotinic acetylcholine receptor agonist with cognition enhancing and anxiolytic activities.
A6625 Acetylcholine chloride ≥99% (TLC) Acetylcholine chloride, injected at 20 mg/kg body weight, reduces mortality and plasma proinflammatory cytokines in mice with experimentally-induced sepsis . The cholinergicanti-infl ammatory mechanism is probably mediated by interaction of acetylcholine with α7n cholinoreceptor on monocytes, macrophages, and neutrophils, which decreases the levels of proinflammatory cytokines such as TNF-α, IL-1β, and IL-6.
A5751 Acetylthiocholine iodide ≥98% (TLC), powder or crystals  
A5656 (±)-Anabasine ≥90% (TLC), liquid Tobacco alkaloid; potent nicotinic acetylcholine receptor agonist.
SML0182 bPiDl hydrate ≥98% (HPLC) bPiDI is an α6β2-specific antagonist that inhibits nicotine-evoked and endogenous dopamine release from rat striatal slices (IC50 = 150 nM, Imax = 55%). bPiDI treatment decreases nicotine self-administration, and nicotine-induced locomotor activity in rats.
B121 Bromoacetylcholine bromide  
T0195 α-Bungarotoxin-tetramethylrhodamine from Bungarus multicinctus (Formosan Banded Krait) Useful for detecting the distribution of nicotinic acetylcholine receptors at neuromuscular junctions.
α-Bungarotoxin is a high-affinity antagonist for nicotinic acetylcholine receptors (AChRs) from muscle but not the neurons. Labeling α-Bungarotoxin with tetramethylrhodamine enables the detection of bungarotoxin-binding receptors at neuromuscular junctions.
SML0852 CC4 ≥98% (HPLC) CC4 is a a partial agonist of α4β2 and α6β2 nicotinic acetylcholine receptors with low affinity for α3β4 and α7 containing receptors. CC4 reduces nicotine-induced self-administration and conditioned place preference without affecting motor functions.
C5366 Chlorisondamine diiodide ≥98% (HPLC), white solid Irreversible, long-lasting nicotinic acetylcholine receptor antagonist.
A3362 Cisatracurium besylate Cisatracurium besylate is a potent, nondepolarizing neuromuscular blocking agent. It acts on cholinergic receptors to block neuromuscular transmission, which can be antagonized by acetylcholinesterase inhibitors. Cisatracurium besylate is one of the ten stereoisomers of astracurium that does not cause histamine release.
C2108 Condelphine ≥95%, solid Nicotinic acetylcholine receptor antagonist.
C5923 (−)-Cotinine ≥98% Major metabolite of nicotine in humans.
C2899 Cytisine ≥99%, powder Potent agonist at α3β4 and α7 nicotinic acetylcholine receptors and partial agonist at α4β2 nicotinic acetylcholine receptors.
D7938 DBO-83 solid Novel nicotinic acetylcholine receptor agonist, structurally related to epibatidine, with antinociceptive properties in rodents.
D1260 Decamethonium bromide crystalline Nicotinic acetylcholine receptor partial agonist and neuromuscular blocking agent; depolarizes striated muscles and blocks their activity.
SML0303 Deformylflustrabromine hydrochloride ≥98% (HPLC) Desformylflustrabromine (dFBr) is a potent, selective positive allosteric modulator of α4β2 nicotinic receptor; increases efficacy and potency of acetylcholine.
D5891 1,1-Dimethyl-4-phenylpiperazinium iodide ≥98% (TLC or titration), powder Nicotinic acetylcholine receptor agonist.
D7689 Diquine ≥98%, solid A nicotinic cholinoreceptor antagonist at the neuromuscular junction; curare-like ganglioblocker.
E0280 (+)-Epibatidine dihydrochloride ≥98% (HPLC), solid (+)-Epibatidine is a non-opioid analgesic alkaloid isolated from skin of Ecuadoran tree frog, Epipedobates tricolor; naturally-occurring isomer of the most potent nicotinic acetylcholine receptor agonist known. Discoveries in the nAChR field have stimulated interest in nAChR-targeted compounds as potential analgesic agents. Epibatidine has full efficacy relative to opioids in preclinical pain models. Although epibatidine is toxic, these observations demonstrated that modest efficacy is not a general limitation of nAChR agonists. Moreover, exploration of the molecular biology of nAChRs revealed evidence of receptor diversity, suggesting that nAChR subtype-selective agents are less toxic than nicotine; and early medicinal chemistry efforts have resulted in compounds with improved safety profiles.
E1145 (±)-Epibatidine dihydrochloride hydrate ≥98% (HPLC), powder The activity of epibatidine at neuronal and neuromuscular nicotinic acetylcholine receptors was compared with the activity of nicotine and suxamethonium. Activation of ganglionic nicotinic receptors by epibatidine was shown in the guinea-pig ileum (contraction mediated by the cholinergic neurons of the ileum) and in pithed and atropinized rats (rise in blood pressure). Epibatidine also activated nicotinic receptors at the peripheral terminals of afferent C-fibres (rabbit ear) and in the brain (antidiuresis in rats). The agonistic effects of epibatidine were followed by long-lasting receptor desensitization. No antinociceptive effect of epibatidine was seen in rats at a dose free of motor impairment. On muscle end plate nicotinic receptors of the rat diaphragm (not responding to depolarizing agents by contraction), epibatidine was equipotent with suxamethonium in causing neuromuscular inhibition. On an extraocular muscle of the rabbit (responding to depolarizing agents by contraction) epibatidine in vitro and in situ caused a contraction at a 100-fold lower dose than suxamethonium. The Straub tail reaction in mice to epibatidine could be attributed to the sustained stimulation of motor end plate receptors of the "slow contracting" type of muscle fibres by epibatidine. Epibatidine was the most potent agonist on all neuronal and neuromuscular nicotinic receptors examined.
F6301 Fluorocurarine chloride ≥97% (TLC), from Vinca erecta, solid Short-acting selective sympathetic ganglioblocker with weak antagonist activity on the nicotinic receptor at the neuromuscular junction; hypotensive.
SML0326 GTS-21 ≥97% (HPLC) GTS-21 is a selective agonist at α-7 nicotinic receptors with anti-inflammatory and cognition enhancing activities. GTS-21 has also been investigated for the treatment of schizophrenia.
H0879 Hexamethonium bromide Preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier only at high doses.
L134 Linopirdine ≥98% (HPLC) Stimulates release of acetylcholine and other neurotransmitters; cognitive enhancer.
SML0870 LY 2087101 ≥98% (HPLC) LY 2087101 is a selective positive allosteric potentiator of α7 and α4β2 nicotinic acetylcholine receptors (nAChRs). LY 2087101 was shown to not enhance the activity of α3β4 subtype nAChRs.
M9020 Mecamylamine hydrochloride Noncompetitive nicotinic acetylcholine receptor antagonist; preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier.
M168 Methyllycaconitine citrate salt from Delphinium brownii seeds, ≥96% (HPLC) Potent and specific nicotinic receptor antagonist that binds to neuronal α-bungarotoxin sites.
M3184 MG 624 ≥98% Nicotinic acetylcholine receptor antagonist; selectively inhibits neuronal nicotinic α-bungarotoxin sensitive receptors that contain the α7 subunit.
N5537 NDNI hydriodide solid, (The product is pure based on CHN, NMR, MS) Highly selective α4β2 nicotinic receptor antagonist
SML1236 (−)-Nicotine hydrogen tartrate salt ≥98% (HPLC) Prototype nicotinic acetylcholine receptor agonist; naturally occurring isomer.
N0267 (±)-Nicotine ≥99% (TLC), liquid Prototype nicotinic acetylcholine receptor agonist.
N3018 (±)-Nornicotine ≥98% (TLC), liquid Nicotinic acetylcholine receptor agonist; active metabolite of nicotine; tobacco alkaloid.
P1918 Pancuronium bromide Aminosteroidal neuromuscular blocking agent; skeletal muscle relaxant
SML1636 Pipecuronium bromide ≥98% (HPLC) Pipecuronium is a bisquaternary aminosteroid muscle relaxant which acts at the nicotinic acetylcholine receptor of the neuromuscular junction. Pipecuronium is a non-depolarizing neuromuscular blocking agent.
P0043 PNU-120596 ≥98% (HPLC) An allosteric modulator of α7 nicotinic receptors, N-(5-chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligand binding domain similar to those caused by acetylcholinePNU-120596 is a positive allosteric modulator selective for the α7 nicotinic acetylcholine receptor. PNU-120596 produces no detectable change in currents mediated by α4β2, α3β4, α9α10 nAChRs. It increases channel mean open time, but does not affect ion selectivity. It does not bind at the agonist binding site, but induces conformational changes similar to the natural effector.
Q0255 Quirestine ≥98% (TLC), powder Nicotinic acetylcholine receptor antagonist. Potent short-acting ganglioblocker.
R131 RJR-2429 dihydrochloride solid Nicotinic acetylcholine receptor agonist.
R5155 Rocuronium bromide ≥98% (perchloric acid titration) Aminosteroid; neuromuscular blocker for anaesthesia
Rocuronium Bromide is a fumarate, non-depolarizing, neuromuscular blocking agent. It is rapid-acting, relaxes the skeletal muscle and decreases oxygen consumption during surgery. It competes with acetylcholine and bind to cholinergic receptors at neuromuscular junctions.
T4819 Tempoxime hydrochloride ≥98% (TLC) Neuronal nicotinic AChR antagonist and potent ganglioblocker.
T5576 TMPH hydrochloride solid, (Product is pure based on CHN, NMR and MS results) 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH) is a potent inhibitor of neuronal nicotinic receptors. Evaluation of nicotinic acetylcholine receptor (nAChR) subunits expressed in Xenopus laevis oocytes indicated that TMPH can produce a potent and long-lasting inhibition of neuronal nAChR formed by the pairwise combination of the most abundant neuronal alpha (i.e., alpha3 and alpha4) and beta subunits (beta2 and beta4), with relatively little effect, because of rapid reversibility of inhibition, on muscle-type (alpha1beta1gammadelta) or alpha7 receptors. However, the inhibition of neuronal beta subunit-containing receptors was also decreased if any of the nonessential subunits alpha5, alpha6, or beta3 were coexpressed. This decrease in inhibition is shown to be associated with a single amino acid present in the second transmembrane domain of these subunits. TMPH abilitty to relate the diverse central nervous system effects to specific nAChR subtypes makes it a useful tool for studying the functional roles of nAChR.
T2379 Tubocurarine hydrochloride pentahydrate ≥97% Muscle relaxant; nicotinic acetylcholine receptor antagonist; can induce neuromuscular paralysis.