METHYLLYCACONITINE PERCHLORATE - LATOXAN Technical Data Sheet
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L6201 METHYLLYCACONITINE PERCHLORATE

an aBungarotoxin neuronal nicotinic receptor antagonist with selective nanomolar affinity for a subtype of neuronal nAChR in the brain that probably incorporates the Alpha7 subunit, compared with micromolar affinity at muscle nAChR and at aBungarotoxin insensitive neuronal nAChR.

C19-norditerpenoid alkaloid C37H50N2O10.HClO4 derivative of Methyllycaconitine from plants of the Delphinium genus, Ranunculaceae.


PRICES
QuantityUS DollarsEURO
5 mg 46.20 33.00
25 mg 184.80 132.00


  • Molecular Weight : 782 Da.

  • Melting Point : 185-187 °C.

  • Solubility in : slightly in methanol; not well in water, ethanol.

  • Purity min. : 95 % (TLC, NMR).

  • Biological Activity : medium-lasting myorelaxing activity; as a tertiary amine, Methyllycaconitine (MLA) crosses histohematic barriers and is active orally: blockage of Nicotinic cholinoreceptors of striated muscles at 2.5-3.5 mg/kg intravenously and 30-40 mg/kg orally; MLA relates to the non-depolarizing competitive myorelaxing agents, and its antagonists are Galanthamine and Neostigmine. 0.5-2 mg/kg intravenously, has an hypotensive activity due to the inhibition of nervous influx transmission in sympathetic and parasympathetic ganglia. MLA acts directly on the brain and spinal cord; enhances the amplitude of monosynaptic potentials in inhibiting the Nicotinic receptors of Renshaw cells; removes totally the inhibiting effect of Nicotine on spinal cord monosynaptic responses; intravenously in cats, MLA has been shown to interact with brain Nicotinic receptors, eliminating variations of EEG caused by subecholine; recent studies (see attached sheet) show that MLA and some related diterpenoid alkaloids act as neuronal Alpha-Bungarotoxin sensitive brain nicotinic receptors antagonist.

  • Toxicity (LD50) : mice (i.v.): 3.9 mg/kg. mice (i.p.): 19.5 mg/kg. mice (orally): 40.0 mg/kg.

  • Storage recommendations : Storage and reconstitution recommendations: Store at +4°C, in dark place. Dissolves in water :
    - at room temperature : up to 0,15%
    - at 40°C : up to 0,3%

  • CAS Reg. No. : 40819-78-1

  • Bibliography :
    1. Pereira et al., "Identification and functional characterization of a new agonist site on nicotinic acetylcholine receptors of cultured hippocampal neurons." Journ. Pharm. Exp. Ther. 1993 265(3):1474-1491
    2. Alkondon et al., "Blockade of nicotinic currents in hippocampal neurons defines methyllycaconitine as a potent and specific receptor antagonist." Mol. Pharmacol. 1992 41(4):802-808
    3. Machkovski et al., "New neuromuscular blocking agents: basic and applied aspects." Berlin 1986 391-397



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    Revised : 26/04/2007 10:27 - Copyright © Latoxan