Soluble in DMSO (12 mg/mL) at 40 °C, ethanol (12 mg/mL) at 40 °C, DMF (25 mg/mL), methanol, and dilute hydrochloric acid (slightly soluble). Insoluble in water.
Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
生化机理
Lamotrigine is a phenyltriazine sodium channel protein inhibitor of presynaptic neurons. Studies indicate that Lamotrigine blocked sustained repetitive firing of neurons in a dose dependent manner in cultured mouse spinal cords. These studies indicate that Lamotrigine is effective at suppressing the release of glutamate and aspartate, but have no effect on acetylcholine and GABA release. Lamotrigine is inactivated by liver microsomes, via hepatic glucuronidation. It is believed that Lamotrigine modulates the fast voltage-dependent sodium currents in a manner similar to phenytoin and carbamazepine. Futhermore, Lamotrigine displays a small frequency dependent inhibition of depolarized potentials that result from sodium currents. Lamotrigine is an inhibitor of Serotonin.