Lamotrigine 84057-84-1

Lamotrigine(BW430C) is a novel anticonvulsant drug for inhibition of 5-HT and sodium channelTarget: Sodium ChannelLamotrigine stabilises presynaptic neuronal membranes by blockade of voltage-dependent sodium channels, thus preventing the release of excitatory neurotransmitters, particularly glutamate and aspartate [1]. In rat cerebral cortex tissue incubated with veratrine 10 mg/L, lamotrigine is twice as potent in inhibiting the release of glutamate and aspartate (ED 50 = 5.38 mg/L for
Lamotrigine, also known by the brand name Lamictal®, is a second-generation antiepileptic drug (AED) manufactured by GlaxoSmithKline in the UK and USA. Lamotrigine is a new mazine, glutamate inhibitor anticonvulsant that significantly reduces the incidence of refractory partial seizures. The drug is reported to produce fewer CNS side effects than diazepam or sodium phenytoin. It is also indicated as add-on therapy for the treatment of generalized seizures not satisfactorily controlled by other anti-epileptics.
It is a white to cream coloured powder that is soluble in isopropanol and somewhat soluble in water. It has a melting point of 216-218°C and readily dissolves in organic solvents like benzene, toluene, and hot ethanol.
The development of lamotrigine began in the early 1980s, accidentally discovered by a group of chemists at the Wellcome Research Laboratory while searching for novel antifolate compounds. Initially synthesized as an antifolate analog, subsequent animal model screening revealed its significant anticonvulsant activity, demonstrating its potential as an antiepileptic drug. In 1980, the Wellcome Foundation filed the first synthetic method and related patent applications for lamotrigine (e.g., European Patent EP 0021121), mentioning researchers such as M. G. Baxter. During clinical development, the efficacy of lamotrigine (trade name: lamotrigine tablets) was confirmed, and it was first launched in Ireland in 1991. Subsequently, it was approved by the U.S. Food and Drug Administration (FDA) for the treatment of epilepsy in 1994. In subsequent studies, the clinical applications of lamotrigine have continued to expand, particularly its efficacy as a mood stabilizer. Researchers such as Richard H. Weissler have advanced the application of lamotrigine in the treatment of bipolar disorder, especially in the maintenance treatment of bipolar depression, through clinical observation and research.
ChEBI: Lamotrigine is a member of the class of 1,2,4-triazines in which the triazene skeleton is substituted by amino groups at positions 3 and 5, and by a 2,3-dichlorophenyl group at position 6. It has a role as an anticonvulsant, an antimanic drug, an antidepressant, a non-narcotic analgesic, a calcium channel blocker, an excitatory amino acid antagonist, an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor, an environmental contaminant, a xenobiotic and a geroprotector. It is a member of 1,2,4-triazines, a primary arylamine and a dichlorobenzene.