Description
Lappaconitine is an alkaloid originally found in species of Aconitum that exhibits analgesic, antinociceptive, anti-inflammatory, anti-arrhythmic, and antiepileptic/anticonvulsant activities. Lappaconitine increases pain threshold and downregulates expression of P2X3 receptors in dorsal root ganglion (DRG) neurons in models of chronic constrictive injury. Lappaconitine also inhibits paw and ear edema in vivo. In vitro, this compound inhibits excitability of hippocampal pyramidal cells and decreases epileptiform burst duration. Additionally, lappaconitine displays class I anti-arrhythmic activity, inducing negative inotropic activity in vivo and inhibiting human heart Na+ channels by binding at neurotoxin site 2.
References
Ou S, Zhao YD, Xiao Z, et al. Effect of lappaconitine on neuropathic pain mediated by P2X3 receptor in rat dorsal root ganglion. Neurochem Int. 2011 Apr;58(5):564-73. PMID: 21272608.
Wang YZ, Xiao YQ, Zhang C, et al. Study of analgesic and anti-inflammatory effects of lappaconitine gelata. J Tradit Chin Med. 2009 Jun;29(2):141-5. PMID: 19663103.
Wright SN. Irreversible block of human heart (hH1) sodium channels by the plant alkaloid lappaconitine. Mol Pharmacol. 2001 Feb;59(2):183-92. PMID: 11160852.
Heubach JF, Schüle A. Cardiac effects of lappaconitine and N-deacetyllappaconitine, two diterpenoid alkaloids from plants of the Aconitum and Delphinium species. Planta Med. 1998 Feb;64(1):22-6. PMID: 9491764.
Ameri A, Gleitz J, Peters T. Bicuculline-induced epileptiform activity in rat hippocampal slices: suppression by Aconitum alkaloids. Planta Med. 1997 Jun;63(3):228-32. PMID: 9225604.
