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Home Page > Alphabetical Index > METHYLLYCACONITINE PERCHLORATE

METHYLLYCACONITINE PERCHLORATE Prod. No L6201 - CAS # 40819-78-1
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Product Name METHYLLYCACONITINE PERCHLORATE
Product Code L6201
METHYLLYCACONITINE PERCHLORATE

C37H50N2O10.HClO4

Molecular Formula C37H50N2O10.HClO4
Description

an α-Bungarotoxin 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 α-Bungarotoxin insensitive neuronal nAChR.

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

 
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 α-Bungarotoxin sensitive brain nicotinic receptors antagonist.

 
Chemical and Physical Properties
 
CAS No. 40819-78-1 Molecular Weight 782 Da.
RTECS Physical Form
Merck Index No (13th Ed.) Melting point 185-187 °C.
PubChem SID Solubility slightly in methanol; not well in water‚ ethanol.
Purity 95 % (TLC‚ NMR). Optical Activity
Toxicity (LD50) mice (i.v.): 3.9 mg/kg.
mice (i.p.): 19.5 mg/kg.
mice (orally): 40.0 mg/kg.
Chemical Names
Storage & Reconstitution 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%
Safety Recommendations
 
Bibliographic References
  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
 
Prices
Code
Quantity
US $
€uro
L6201
5 mg
46.20
33.00
25 mg
184.80
132.00
 
External Links PubMed Biomedical Citations From PubMed Toxicology Citations From PubMed PubChem SID

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