METHYLLYCACONITINE CITRATE Struktur

METHYLLYCACONITINE CITRATE

Bezeichnung:METHYLLYCACONITINE CITRATE

CAS-Nr112825-05-5

Englisch Name:METHYLLYCACONITINE CITRATE

CBNumberCB8113766

SummenformelC43H58N2O17

Molgewicht874.92

MOL-Datei112825-05-5.mol

METHYLLYCACONITINE CITRATE physikalisch-chemischer Eigenschaften

storage temp.	−20°C
Löslichkeit	H₂O: 42 mg/mL
Aggregatzustand	solid
Farbe	white

Sicherheit

WGK Germany

METHYLLYCACONITINE CITRATE Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Methyllycaconitine citrate salt has been used as an α7 nicotinic acetylcholine receptor (α7 nAChR) antagonist:
- to study its effects on inflammatory response in rats post nicotine treatment
- to block the activity of galantamine
- to study its effects on the hepatic branch of the vagus nerve (hVNS) in rats
Biologische Aktivität
methyllycaconitine citrate(mla) is an antagonist of α7-containing neuronal nicotinic acetylcholine receptors (nachrs; ki = 1.4 nm)[1,2].mla inhibits the decreased cell viability induced by aβ25-35, pretreatment with 5 and 10 μm. aβ25-35 treatment increases lc3-ii levels, which is inhibited by administration of methyllycaconitine citrate. mla also inhibits aβ-induced autophagosome accumulation in sh-sy5y cells[3].mla inhibits methamphetamine(meth)-induced climbing behavior by 50%. mla prevents a decrease in striatal synaptosome dopamine (da) uptake, mla significantly attenuates meth-induced neurotoxicity at 72 h post-treatment. mla fully prevents microglial activation at 24 h post-treatment and tending to confirm its neuroprotective activity[4].[1]. kalappa b i, sun f, johnson s r, et al. a positive allosteric modulator of α7 nachrs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischaemia. brit.j.pharmacol, 2013, 169(8): 1862-1878.[2]. ward j m, cockcroft v b, lunt g g, et al. methyllycaconitine: a selective probe for neuronal α-bungarotoxin binding sites. febs lett, 1990, 270(1-2): 45-48 .[3]. zheng x, et al. methyllycaconitine alleviates amyloid-β peptides-induced cytotoxicity in sh-sy5y cells. plos one, 2014, 9(10): e111536.[4]. escubedo e, et al. methyllycaconitine prevents methamphetamine-induced effects in mouse striatum: involvement of alpha7 nicotinic receptors. j pharmacol exp ther, 2005, 315(2): 658-67.
Biochem/physiol Actions
Methyllycaconitine (MLA) is an α7 nicotinic acetylcholine receptor (α7 nAChR) antagonist. It is a norditerpenoid alkaloid synthesized by several species of Delphinium. MLA binds to the binding site of neuronal α-bungarotoxin. Low doses of MLA are associated with improvement of cognition in animals.

METHYLLYCACONITINE CITRATE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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