Oxcarbazepine
Oxcarbazepine (OX) is an antiepileptic/anticonvulsant commonly used to treat epilepsy, but also exhibits activity as a treatment for mood disorders and neuropathic pain as well. Administration of oxcarbazepine leads to a reversible reduction in current amplitude from voltage-gated Na+ channels and may suppress current amplitude of delayed rectifying K+ channels; this reduces the amplitude of action potentials and prolongs their duration. This compound also inhibits Na+ channel-dependent Glu release and produces a moderate open channel block on nicotinic acetylcholine receptors (nAChRs), preventing deactivation. Interestingly, oxcarbazepine may have potential as a treatment for substance abuse disorders, as it is moderately effective as a relapse prevention treatment in a clinical trial of recently abstinent alcohol-dependent subjects.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18951599
| Cas No. |
28721-07-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C15H12N2O2 |
| Formula Wt. |
252.27 |
| Chemical Name |
10,11-Dihydro-10-oxo-5H-dibenz[b,f]azepine-5- carboxamide |
| IUPAC Name |
5-oxo-6H-benzo[b][1]benzazepine-11-carboxamide |
| Synonym |
Trileptal |
| Melting Point |
215-216°C |
| Solubility |
Soluble in DMSO (9mg/mL). |
| Appearance |
White or Almost White Powder |
Di Resta C, Ambrosi P, Curia G, et al. Effect of carbamazepine and oxcarbazepine on wild-type and mutant neuronal nicotinic acetylcholine receptors linked to nocturnal frontal lobe epilepsy. Eur J Pharmacol. 2010 Sep 15;643(1):13-20. PMID: 20561518.
Johannessen Landmark C, Johannessen SI. Pharmacological management of epilepsy: recent advances and future prospects. Drugs. 2008;68(14):1925-39. PMID: 18778117.
Huang CW, Huang CC, Lin MW, et al. The synergistic inhibitory actions of oxcarbazepine on voltage-gated sodium and potassium currents in differentiated NG108-15 neuronal cells and model neurons. Int J Neuropsychopharmacol. 2008 Aug;11(5):597-610. PMID: 18184444.
Sitges M, Chiu LM, Guarneros A, et al. Effects of carbamazepine, phenytoin, lamotrigine, oxcarbazepine, topiramate and vinpocetine on Na+ channel-mediated release of [3H]glutamate in hippocampal nerve endings. Neuropharmacology. 2007 Feb;52(2):598-605. PMID: 17070874.
Nishimura M, Nakanishi T, Yasui A, et al. Serum calcium increases the incidence of arrhythmias during acetate hemodialysis. Am J Kidney Dis. 1992 Feb;19(2):149-55. PMID: 1739097.
