Methyllycaconitine citrate

Cat. No. 1029

Methyllycaconitine citrate C37H50N2O10.C6H8O7 [112825-05-5]

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Alternative Name: 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

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

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

Escubedo et al (2005) Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum: involvement of α7 nicotinic receptors. J.Pharmacol.Exp.Ther. 315 658. PMID: 16076935.

Dobelis et al (1999) Effects of delphinium alkaloids on neuromuscular transmission. J.Pharmacol.Exp.Ther. 291 538. PMID: 10525069.

Ward et al (1990) Methyllycaconitine: a selective probe for neuronal a-bungarotoxin binding sites. FEBS Lett. 270 45. PMID: 2226787.

If you know of a relevant reference for Methyllycaconitine citrate please let us know.

Citations are publications that use Tocris products. Selected citations for Methyllycaconitine citrate include:

Assous (2017) Differential processing of thalamic information via distinct striatal interneuron circuits. Nat Commun 8 15860. PMID: 28604688.

Herman et al (2016) A cholinergic basal forebrain feeding circuit modulates appetite suppression Nature 538 253. PMID: 27698417.

Zhang et al (2016) Acetylcholinesterase inhibitors for Alzheimer's disease treatment ameliorate acetaminophen-induced liver injury in mice via central cholinergic system regulation the Journal of Pharmacology and Experimental Thera. PMID: 27535978.

Brown and Wonnacott (2015) Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors. Sci Rep 40 2047. PMID: 24728867.

Elgueta et al (2015) Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells. J Neurosci 9 6. PMID: 25709566.

Pinnock et al (2015) Nicotine receptors mediating sensorimotor gating and its enhancement by systemic nicotine. Arch Neurol 9 30. PMID: 25717295.

Saunders et al (2015) Corelease of acetylcholine and GABA from cholinergic forebrain neurons. Neurochem Res 4. PMID: 25723967.

Tang et al (2015) Modulation of AMPA receptor mediated current by nicotinic acetylcholine receptor in layer I neurons of rat prefrontal cortex. PLoS One 5 14099. PMID: 26370265.

Kiss et al (2014) Nicotinic acetylcholine receptors containing the α7-like subunit mediate contractions of muscles responsible for space positioning of the snail, Helix pomatia L. tentacle. PLoS One 9 e109538. PMID: 25303328.

Brown et al (2013) 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. J Biol Chem 288 33049. PMID: 24089524.

Callahan et al (2013) 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. Neuropharmacology 67 201. PMID: 23168113.

Némethova et al (2013) Nicotine attenuates activation of tissue resident macrophages in the mouse stomach through the β2 nicotinic acetylcholine receptor. Front Behav Neurosci 8 e79264. PMID: 24223920.

Grimster et al (2012) Generation of candidate ligands for nicotinic acetylcholine receptors via in situ click chemistry with a soluble acetylcholine binding protein template. J Am Chem Soc 134 6732. PMID: 22394239.

Leão et al (2012) OLM interneurons differentially modulate CA3 and entorhinal inputs to hippocampal CA1 neurons. Nat Neurosci 15 1524. PMID: 23042082.

Yamauchi et al (2012) Synthesis of selective agonists for the α7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates. J Pharmacol Exp Ther 82 687. PMID: 22784805.

Northrop et al (2011) Regulation of glutamate release by α7 nicotinic receptors: differential role in methamphetamine-induced damage to dopaminergic and serotonergic terminals. Am J Physiol Renal Physiol 336 900. PMID: 21159748.

Collins and Millar (2010) Nicotinic acetylcholine receptor transmembrane mutations convert ivermectin from a positive to a negative allosteric modulator. Mol Pharmacol 78 198. PMID: 20463059.

Li et al (2010) Cytisine induces autonomic cardiovascular responses via activations of different nicotinic receptors. Auton Neurosci 154 14. PMID: 19887306.

Ikonomovic et al (2009) Cortical α7 nicotinic acetylcholine receptor and β-amyloid levels in early Alzheimer disease. Mol Pharmacol 66 646. PMID: 19433665.

Li et al (2009) Specific subtypes of nicotinic cholinergic receptors involved in sympathetic and parasympathetic cardiovascular responses. Neurosci Lett 462 20. PMID: 19573576.

Beckel et al (2006) Expression of functional nicotinic acetylcholine receptors in rat urinary bladder epithelial cells. Front Cell Neurosci 290 F103. PMID: 16144967.

Hansen et al (2005) Structures of Aplysia AChBP complexes with nicotinic agonists and antagonists reveal distinctive binding interfaces and conformations. EMBO J 24 3635. PMID: 16193063.

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Keywords: Methyllycaconitine citrate, supplier, α7, alpha7, a7, neuronal, nicotinic, receptors, antagonists, Nicotinic, Acetylcholine, nAChR, Tocris Bioscience, Nicotinic (α7) Receptor Antagonist products

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