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Nicotinic Acetylcholine Receptor Modulators

Description
Biochem/physiol Actions
Product #
A-85380 dihydrochloride solid Potent and selective neuronal nicotinic acetylcholine receptor (nAChR) agonist.
 A251
ABT-418 hydrochloride powder, ≥98% (HPLC) Neuronal nicotinic acetylcholine receptor agonist with cognition enhancing and anxiolytic activities.
 A6476
Acetylcholine chloride ≥99% (TLC) Endogenous neurotransmitter at cholinergic synapses; amplifies action potential of the sarcolemma thereby inducing muscle contractions.
 A6625
Acetylthiocholine iodide ≥98% (TLC), powder A5751
(±)-Anabasine ≥90% (TLC), liquid Tobacco alkaloid; potent nicotinic acetylcholine receptor agonist.
 A5656
Atracurium besylate ≥98% (HPLC), powder Nicotinic acetylcholine receptor antagonist.
 A7604
Bromoacetylcholine bromide B121
α-Bungarotoxin from Bungarus multicinctus (Formosan Banded Krait) solid Neurotoxin which binds irreversibly to motor endplate of acetylcholine receptors; prevents opening of nicotinic receptor-associated ion channels.
 T3019
α-Bungarotoxin-tetramethylrhodamine from Bungarus multicinctus (Formosan Banded Krait) Useful for detecting the distribution of nicotinic acetylcholine receptors at neuromuscular junctions.
 T0195
Chlorisondamine diiodide ≥98% (HPLC), solid Irreversible, long-lasting nicotinic acetylcholine receptor antagonist.
 C5366
Condelphine 95%, solid Nicotinic acetylcholine receptor antagonist.
 C2108
α-Conotoxin Im I ≥97% (HPLC) Nicotinic acetylcholine receptor antagonist in central nervous system.
 C2461
(−)-Cotinine ~98% Major metabolite of nicotine in humans.
 C5923
Cytisine ≥99%, powder Potent agonist at α3β4 and α7 nicotinic acetylcholine receptors and partial agonist at α4β2 nicotinic acetylcholine receptors.
 C2899
DBO-83 solid Novel nicotinic acetylcholine receptor agonist, structurally related to epibatidine, with antinociceptive properties in rodents.
 D7938
Decamethonium bromide crystalline Nicotinic acetylcholine receptor partial agonist and neuromuscular blocking agent; depolarizes striated muscles and blocks their activity.
 D1260
Dihydro-β-erythroidine hydrobromide solid Competitive nicotinic receptor antagonist.
 D149
1,1-Dimethyl-4-phenylpiperazinium iodide ≥98% (TLC or titration), powder Nicotinic acetylcholine receptor agonist.
 D5891
Diplacine ≥98%, solid A nicotinic cholinoreceptor antagonist at the neuromuscular junction; curare-like ganglioblocker.
 D7564
Diquine ≥98%, solid A nicotinic cholinoreceptor antagonist at the neuromuscular junction; curare-like ganglioblocker.
 D7689
(+)-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.
 E0280
(±)-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.
 E1145
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.
 F6301
Hexamethonium bromide Preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier only at high doses.
 H0879
Linopirdine solid Stimulates release of acetylcholine and other neurotransmitters; cognitive enhancer.
 L134
Mecamylamine hydrochloride Noncompetitive nicotinic acetylcholine receptor antagonist; preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier.
 M9020
Methyllycaconitine citrate hydrate from Delphinium brownii seeds, ≥96% (HPLC) Potent and specific nicotinic receptor antagonist that binds to neuronal α-bungarotoxin sites.
 M168
MG 624 ≥98% Nicotinic acetylcholine receptor antagonist; selectively inhibits neuronal nicotinic α-bungarotoxin sensitive receptors that contain the α7 subunit.
 M3184
NDNI hydriodide solid, (The product is pure based on CHN, NMR, MS) Highly selective α4β2 nicotinic receptor antagonist
 N5537
(−)-Nicotine hydrogen tartrate salt ≥98% (TLC), powder Prototype nicotinic acetylcholine receptor agonist; naturally occurring isomer.
 N5260
(±)-Nicotine ≥98% (TLC), liquid Prototype nicotinic acetylcholine receptor agonist.
 N0267
(±)-Nornicotine ≥99% (TLC), liquid Nicotinic acetylcholine receptor agonist; active metabolite of nicotine; tobacco alkaloid.
 N3018
Pancuronium bromide Aminosteroidal neuromuscular blocking agent; skeletal muscle relaxant
 P1918
Pempidine tartrate ≥98% (TLC), powder Neuronal nicotinic acetylcholine receptor antagonist; potent ganglioblocker; antihypertensive.
 P5114
Quirestine ≥98% (TLC), powder Nicotinic acetylcholine receptor antagonist. Potent short-acting ganglioblocker.
 Q0255
RJR-2403 hemigalactarate ≥98% (HPLC), powder Neuronal nicotinic acetylcholine receptor agonist that displays CNS activity.
 R130
RJR-2429 dihydrochloride solid Nicotinic acetylcholine receptor agonist.
 R131
Temechine hydrobromide ≥98% (TLC), powder Neuronal nicotinic acetylcholine receptor antagonist; potent ganglioblocker.
 T4569
Tempidol hydrochloride ≥98% (TLC) Neuronal nicotinic acetylcholine receptor antagonist; potent ganglioblocker.
 T4944
Tempoxime hydrochloride ≥98% (TLC) Neuronal nicotinic AChR antagonist and potent ganglioblocker.
 T4819
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.
T5576
N,N,N-Trimethyl-1-(4-trans-stilbenoxy)-2-propylammonium iodide Nicotinic acetylcholine receptor antagonist.
 T6692
(+)-Tubocurarine chloride hydrate ≥97% Muscle relaxant; nicotinic acetylcholine receptor antagonist; can induce neuromuscular paralysis.
 T2379

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