Catalog Number: 1029
Alternate 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
Biological Activity
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
  • M.Wt:
    874.93
  • Formula:
    C37H50N2O10.C6H8O7
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Storage:
    Desiccate at -20°C
  • CAS No:
    112825-05-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Effects of delphinium alkaloids on neuromuscular transmission.
    Dobelis et al.
    J.Pharmacol.Exp.Ther., 1999;291:538
  2. Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum: involvement of α7 nicotinic receptors.
    Escubedo et al.
    J.Pharmacol.Exp.Ther., 2005;315:658
  3. Methyllycaconitine: a selective probe for neuronal a-bungarotoxin binding sites.
    Ward et al.
    FEBS Lett., 1990;270:45
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Methyllycaconitine citrate include:

22 Citations: Showing 1 - 10
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  1. Differential processing of thalamic information via distinct striatal interneuron circuits.
    Authors: Assous
    Nat Commun 2017;8:15860
  2. A cholinergic basal forebrain feeding circuit modulates appetite suppression
    Authors: Herman Et al.
    Nature 2016;538:253
  3. 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;
  4. 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
  5. Nicotine receptors mediating sensorimotor gating and its enhancement by systemic nicotine.
    Authors: Pinnock Et al.
    Arch Neurol 2015;9:30
  6. 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
  7. Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors.
    Authors: Brown and Wonnacott
    Sci Rep 2015;40:2047
  8. Corelease of acetylcholine and GABA from cholinergic forebrain neurons.
    Authors: Saunders Et al.
    Neurochem Res 2015;4
  9. 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
  10. 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
  11. Positive allosteric modulator of α7 nicotinic-acetylcholine receptors, PNU-120596 augments the effects of donepezil on learning and memory in aged rodents and non-human primates.
    Authors: Callahan Et al.
    Neuropharmacology 2013;67:201
  12. 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
  13. 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
  14. OLM interneurons differentially modulate CA3 and entorhinal inputs to hippocampal CA1 neurons.
    Authors: Leão Et al.
    Nat Neurosci 2012;15:1524
  15. 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
  16. Regulation of glutamate release by α7 nicotinic receptors: differential role in methamphetamine-induced damage to dopaminergic and serotonergic terminals.
    Authors: Northrop Et al.
    Am J Physiol Renal Physiol 2011;336:900
  17. Nicotinic acetylcholine receptor transmembrane mutations convert ivermectin from a positive to a negative allosteric modulator.
    Authors: Collins and Millar
    Mol Pharmacol 2010;78:198
  18. Cytisine induces autonomic cardiovascular responses via activations of different nicotinic receptors.
    Authors: Li Et al.
    Auton Neurosci 2010;154:14
  19. Cortical α7 nicotinic acetylcholine receptor and β-amyloid levels in early Alzheimer disease.
    Authors: Ikonomovic Et al.
    Mol Pharmacol 2009;66:646
  20. Specific subtypes of nicotinic cholinergic receptors involved in sympathetic and parasympathetic cardiovascular responses.
    Authors: Li Et al.
    Neurosci Lett 2009;462:20
  21. Expression of functional nicotinic acetylcholine receptors in rat urinary bladder epithelial cells.
    Authors: Beckel Et al.
    Front Cell Neurosci 2006;290:F103
  22. 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
Expand to show all 22 Citations

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