Methyllycaconitine citrate
Chemical Name: [1α,4(S),6β,14α,16β]-20-Ethyl-1,6,14,16-tetramethoxy-4-[[[2-(3-methyl-2,5-dioxo-1-pyrrolidinyl)benzoyl]oxy]methyl]aconitane-7,8-diol citrate
Purity: ≥95%
Biological Activity
Methyllycaconitine citrate is a potent antagonist for α7-containing neuronal nicotinic receptors (Ki = 1.4 nM). Interacts with α4β2 and α6β2 receptors at concentrations > 40 nM. Attenuates METH-induced neurotoxicity in mouse striatum in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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The role of alpha7 nicotinic acetylcholine receptor in modulation of heart rate dynamics in endotoxemic rats.
Mazloom R, Eftekhari G, Rahimi M, Khori V, Hajizadeh S, Dehpour A, Mani A
PLoS ONE, 2013;8(12):e82251. -
Acetylcholinesterase inhibitors for Alzheimer's disease treatment ameliorate acetaminophen-induced liver injury in mice via central cholinergic system regulation
J Pharmacol Exp Ther, 2016;0(0):. -
High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Nicotine induces the up-regulation of the alpha7-nicotinic receptor (alpha7-nAChR) in human squamous cell lung cancer cells via the Sp1/GATA protein pathway.
Brown K, Perry H, Lau J, Jones D, Pulliam J, Thornhill B, Crabtree C, Luo H, Chen Y, Dasgupta P
J Biol Chem, 2013;288(46):33049-59. -
Effects of delphinium alkaloids on neuromuscular transmission.
Dobelis et al.
J.Pharmacol.Exp.Ther., 1999;291:538 -
Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum: involvement of α7 nicotinic receptors.
Escubedo et al.
J.Pharmacol.Exp.Ther., 2005;315:658 -
Methyllycaconitine: a selective probe for neuronal a-bungarotoxin binding sites.
Ward et al.
FEBS Lett., 1990;270:45
Product Datasheets
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Citations for Methyllycaconitine citrate
The citations listed below are publications that use Tocris products. Selected citations for Methyllycaconitine citrate include:
30 Citations: Showing 1 - 10
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Amphetamine enantiomers inhibit homomeric α7 nicotinic receptor through a competitive mechanism and within the intoxication levels in humans.
Authors: Garton Et al.
Neuropharmacology 2019;144:172
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Alcohol exposure disrupts mu opioid receptor-mediated long-term depression at insular cortex inputs to dorsolateral striatum.
Authors: Muñoz Et al.
Nat Commun 2018;9:1318
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GABAergic inhibition in dual-transmission cholinergic and GABAergic striatal interneurons is abolished in Parkinson disease.
Authors: Lozovaya Et al.
Nat Commun 2018;9(1):1422
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Differential processing of thalamic information via distinct striatal interneuron circuits.
Authors: Assous
Nat Commun 2017;8:15860
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A cholinergic basal forebrain feeding circuit modulates appetite suppression
Authors: Herman Et al.
Nature 2016;538:253
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Acetylcholinesterase inhibitors for Alzheimer's disease treatment ameliorate acetaminophen-induced liver injury in mice via central cholinergic system regulation
Authors: Zhang Et al.
the Journal of Pharmacology and Experimental Thera 2016;
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Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells.
Authors: Elgueta Et al.
J Neurosci 2015;9:6
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Nicotine receptors mediating sensorimotor gating and its enhancement by systemic nicotine.
Authors: Pinnock Et al.
Arch Neurol 2015;9:30
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Modulation of AMPA receptor mediated current by nicotinic acetylcholine receptor in layer I neurons of rat prefrontal cortex.
Authors: Tang Et al.
PLoS One 2015;5:14099
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Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors.
Authors: Brown and Wonnacott
Sci Rep 2015;40:2047
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Corelease of acetylcholine and GABA from cholinergic forebrain neurons.
Authors: Saunders Et al.
Neurochem Res 2015;4
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Synergy of direct and indirect cholinergic septo-hippocampal pathways coordinates firing in hippocampal networks.
Authors: Dannenberg Et al.
J Neurosci 2015;35:8394
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Nicotinic acetylcholine receptors containing the α7-like subunit mediate contractions of muscles responsible for space positioning of the snail, Helix pomatia L. tentacle.
Authors: Kiss Et al.
PLoS One 2014;9:e109538
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Stimulation of the α7 nicotinic acetylcholine receptor protects against sepsis by inhibiting Toll-like receptor via phosphoinositide 3-kinase activation.
Authors: Kim Et al.
J Infect Dis 2014;209:1668
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Nicotine attenuates activation of tissue resident macrophages in the mouse stomach through the β2 nicotinic acetylcholine receptor.
Authors: Némethova Et al.
Front Behav Neurosci 2013;8:e79264
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Positive allosteric modulator of α7 nicotinic-acetylcholine receptors, PNU-120596 augments the effects of donep. on learning and memory in aged rodents and non-human primates.
Authors: Callahan Et al.
Neuropharmacology 2013;67:201
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Design, synthesis, and activity of a series of arylpyrid-3-ylmethanones as type I positive allosteric modulators of α7 nicotinic acetylcholine receptors.
Authors: Hogenkamp Et al.
J Med Chem 2013;56:8352
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Nicotine induces the up-regulation of the α7-nicotinic receptor (α7-nAChR) in human squamous cell lung cancer cells via the Sp1/GATA protein pathway.
Authors: Brown Et al.
J Biol Chem 2013;288:33049
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Synthesis of selective agonists for the α7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates.
Authors: Yamauchi Et al.
J Pharmacol Exp Ther 2012;82:687
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OLM interneurons differentially modulate CA3 and entorhinal inputs to hippocampal CA1 neurons.
Authors: Leão Et al.
Nat Neurosci 2012;15:1524
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Generation of candidate ligands for nicotinic acetylcholine receptors via in situ click chemistry with a soluble acetylcholine binding protein template.
Authors: Grimster Et al.
J Am Chem Soc 2012;134:6732
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Effects of drugs of abuse on putative rostromedial tegmental neurons, inhibitory afferents to midbrain DA cells.
Authors: Lecca Et al.
Neuropsychopharmacology 2011;36:589
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Regulation of glutamate release by α7 nicotinic receptors: differential role in methamphetamine-induced damage to DArgic and serotonergic terminals.
Authors: Northrop Et al.
Am J Physiol Renal Physiol 2011;336:900
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Nicotinic acetylcholine receptor transmembrane mutations convert iverm. from a positive to a negative allosteric modulator.
Authors: Collins and Millar
Mol Pharmacol 2010;78:198
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Activation of muscarinic acetylcholine receptors induces a nitric oxide-dependent long-term depression in rat medial prefrontal cortex.
Authors: Huang and Hsu
Cereb Cortex 2010;20:982
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Cytisine induces autonomic cardiovascular responses via activations of different nicotinic receptors.
Authors: Li Et al.
Auton Neurosci 2010;154:14
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Cortical α7 nicotinic acetylcholine receptor and β-amyloid levels in early Alzheimer disease.
Authors: Ikonomovic Et al.
Mol Pharmacol 2009;66:646
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Specific subtypes of nicotinic cholinergic receptors involved in sympathetic and parasympathetic cardiovascular responses.
Authors: Li Et al.
Neurosci Lett 2009;462:20
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Expression of functional nicotinic acetylcholine receptors in rat urinary bladder epithelial cells.
Authors: Beckel Et al.
Front Cell Neurosci 2006;290:F103
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Structures of Aplysia AChBP complexes with nicotinic agonists and antagonists reveal distinctive binding interfaces and conformations.
Authors: Hansen Et al.
EMBO J 2005;24:3635
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