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.