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Submit ReviewMethyllycaconitine citrate
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% (HPLC)
Biological Activity for Methyllycaconitine citrate
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 for Methyllycaconitine citrate
| M. Wt | 874.93 |
| Formula | C37H50N2O10.C6H8O7 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 351344-10-0 |
| PubChem ID | 90479749 |
| InChI Key | INBLZNJHDLEWPS-IRPACCRLSA-N |
| Smiles | OC(=O)CC(O)(CC(O)=O)C(O)=O.[H][C@@]12C[C@H]3[C@H](OC)[C@]1([H])[C@](O)(C[C@@H]3OC)[C@]1(O)[C@@H](OC)C3[C@@]22[C@H]1N(CC)C[C@]3(COC(=O)C1=CC=CC=C1N1C(=O)C[C@H](C)C1=O)CC[C@@H]2OC |
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.
Solubility Data for Methyllycaconitine citrate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 87.49 | 100 | |
| DMSO | 87.49 | 100 |
Preparing Stock Solutions for Methyllycaconitine citrate
The following data is based on the product molecular weight 874.93. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.14 mL | 5.71 mL | 11.43 mL |
| 5 mM | 0.23 mL | 1.14 mL | 2.29 mL |
| 10 mM | 0.11 mL | 0.57 mL | 1.14 mL |
| 50 mM | 0.02 mL | 0.11 mL | 0.23 mL |
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Product Datasheets for Methyllycaconitine citrate
References for Methyllycaconitine citrate
References are publications that support the biological activity of the product.
Dobelis et al (1999) Effects of delphinium alkaloids on neuromuscular transmission. J.Pharmacol.Exp.Ther. 291 538 PMID: 10525069
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
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.
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Keywords: Methyllycaconitine citrate, Methyllycaconitine citrate supplier, α7, alpha7, a7, neuronal, nicotinic, receptors, antagonists, Nicotinic, Acetylcholine, nAChR, MLA, (a7), Receptors, 1029, Tocris Bioscience
30 Citations for Methyllycaconitine citrate
Citations are publications that use Tocris products. Selected citations for Methyllycaconitine citrate include:
Ikonomovic et al (2009) Cortical α7 nicotinic acetylcholine receptor and β-amyloid levels in early Alzheimer disease. Mol Pharmacol 66 646 PMID: 19433665
Garton et al (2019) Amphetamine enantiomers inhibit homomeric α7 nicotinic receptor through a competitive mechanism and within the intoxication levels in humans. Neuropharmacology 144 172 PMID: 30359640
Brown and Wonnacott (2015) Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors. Sci Rep 40 2047 PMID: 24728867
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 donep. on learning and memory in aged rodents and non-human primates. Neuropharmacology 67 201 PMID: 23168113
Lecca et al (2011) Effects of drugs of abuse on putative rostromedial tegmental neurons, inhibitory afferents to midbrain DA cells. Neuropsychopharmacology 36 589 PMID: 21048703
Li et al (2009) Specific subtypes of nicotinic cholinergic receptors involved in sympathetic and parasympathetic cardiovascular responses. Neurosci Lett 462 20 PMID: 19573576
Assous (2017) Differential processing of thalamic information via distinct striatal interneuron circuits. Nat Commun 8 15860 PMID: 28604688
Dannenberg et al (2015) Synergy of direct and indirect cholinergic septo-hippocampal pathways coordinates firing in hippocampal networks. J Neurosci 35 8394 PMID: 26041909
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
Pinnock et al (2015) Nicotine receptors mediating sensorimotor gating and its enhancement by systemic nicotine. Arch Neurol 9 30 PMID: 25717295
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
Huang and Hsu (2010) Activation of muscarinic acetylcholine receptors induces a nitric oxide-dependent long-term depression in rat medial prefrontal cortex. Cereb Cortex 20 982 PMID: 19666830
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
Kim et al (2014) Stimulation of the α7 nicotinic acetylcholine receptor protects against sepsis by inhibiting Toll-like receptor via phosphoinositide 3-kinase activation. J Infect Dis 209 1668 PMID: 24298024
Hogenkamp et al (2013) Design, synthesis, and activity of a series of arylpyrid-3-ylmethanones as type I positive allosteric modulators of α7 nicotinic acetylcholine receptors. J Med Chem 56 8352 PMID: 24098954
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
Collins and Millar (2010) Nicotinic acetylcholine receptor transmembrane mutations convert iverm. 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
Lozovaya et al (2018) GABAergic inhibition in dual-transmission cholinergic and GABAergic striatal interneurons is abolished in Parkinson disease. Nat Commun 9 1422 PMID: 29651049
Herman et al (2016) A cholinergic basal forebrain feeding circuit modulates appetite suppression Nature 538 253 PMID: 27698417
Muñoz et al (2018) Alcohol exposure disrupts mu opioid receptor-mediated long-term depression at insular cortex inputs to dorsolateral striatum. Nat Commun 9 1318 PMID: 29615610
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 DArgic and serotonergic terminals. Am J Physiol Renal Physiol 336 900 PMID: 21159748
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
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
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
Beckel et al (2006) Expression of functional nicotinic acetylcholine receptors in rat urinary bladder epithelial cells. Front Cell Neurosci 290 F103 PMID: 16144967
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blocking the activity of nicotinic receptor agonist.
By
Anonymous on 10/30/2019
Assay Type: In Vivo
Species: Rat
Dosed to rats as nicotininc receptor antagonist
Literature in this Area
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Nicotinic ACh Receptors Scientific Review
Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.
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