Methyllycaconitine citrate

Catalog # Availability Size / Price Qty
Methyllycaconitine citrate | CAS No. 351344-10-0 | Nicotinic (a7) Receptor Antagonists
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Description: Selective α7 neuronal nAChR antagonist
Alternative Names: MLA

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%

Product Details
Citations (30)
Supplemental Products

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

Soluble to 100 mM in water and to 100 mM in DMSO
Store at -20°C

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.

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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

  1. 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
  2. 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
  3. 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
  4. Differential processing of thalamic information via distinct striatal interneuron circuits.
    Authors: Assous
    Nat Commun  2017;8:15860
  5. A cholinergic basal forebrain feeding circuit modulates appetite suppression
    Authors: Herman Et al.
    Nature  2016;538:253
  6. 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;
  7. 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
  8. Nicotine receptors mediating sensorimotor gating and its enhancement by systemic nicotine.
    Authors: Pinnock Et al.
    Arch Neurol  2015;9:30
  9. 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
  10. Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors.
    Authors: Brown and Wonnacott
    Sci Rep  2015;40:2047
  11. Corelease of acetylcholine and GABA from cholinergic forebrain neurons.
    Authors: Saunders Et al.
    Neurochem Res  2015;4
  12. Synergy of direct and indirect cholinergic septo-hippocampal pathways coordinates firing in hippocampal networks.
    Authors: Dannenberg Et al.
    J Neurosci  2015;35:8394
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. 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
  19. 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
  20. OLM interneurons differentially modulate CA3 and entorhinal inputs to hippocampal CA1 neurons.
    Authors: Leão Et al.
    Nat Neurosci  2012;15:1524
  21. 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
  22. Effects of drugs of abuse on putative rostromedial tegmental neurons, inhibitory afferents to midbrain DA cells.
    Authors: Lecca Et al.
    Neuropsychopharmacology  2011;36:589
  23. 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
  24. Nicotinic acetylcholine receptor transmembrane mutations convert iverm. from a positive to a negative allosteric modulator.
    Authors: Collins and Millar
    Mol Pharmacol  2010;78:198
  25. 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
  26. Cytisine induces autonomic cardiovascular responses via activations of different nicotinic receptors.
    Authors: Li Et al.
    Auton Neurosci  2010;154:14
  27. Cortical α7 nicotinic acetylcholine receptor and β-amyloid levels in early Alzheimer disease.
    Authors: Ikonomovic Et al.
    Mol Pharmacol  2009;66:646
  28. Specific subtypes of nicotinic cholinergic receptors involved in sympathetic and parasympathetic cardiovascular responses.
    Authors: Li Et al.
    Neurosci Lett  2009;462:20
  29. Expression of functional nicotinic acetylcholine receptors in rat urinary bladder epithelial cells.
    Authors: Beckel Et al.
    Front Cell Neurosci  2006;290:F103
  30. 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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