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Oxcarbazepine

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This article, Oxcarbazepine, was written by RelentlessRecusant. Please do not edit this fiction without the writer's permission.

Oxcarbazepine (OCZ)
Chemical information
IUPAC Nomenclature

10-oxo-10,11-dihydro-5H-dibenzo[b,f]azepine-5-carboxamide

Chemical Formula

C15H12N2O2

Molecular Weight

252.27 g/mol

Clinical information
Clinical Usage
  • Anticonvulsant
  • Neuropathic pain
  • Mood stabilizer
Mechanism of Action

Inhibition of central nervous fast sodium (Na+) current

Route of Administration

Oral

Pharmacokinetic information
Metabolism

Hepatic metabolism

Elimination Half-Life

Moderately low

  [Source]

Oxcarbazepine (OCZ), IUPAC name 10-oxo-10,11-dihydro-5H-dibenzo[b,f]azepine-5-carboxamide, is a small-molecule chemical modulator of central nervous sodium (Na+) channels[1], likely Nav1.1 (SCN1A) and Nav1.2 (SCN2A) and is an inhibitor of the fast Na+ conductance current (INaF). It is an oxidated heterocyclic derivative of carbamazepine, a carbamoyl derivative of iminodibenzyls.[2]

It is marketed primarily as an anti-epileptic drug (AED) because of its neuromodulatory effects on the central fast Na+ current, although oxcarbazepine has a broad activity against other non-epileptic central neurological pathologies, including neuropathic pain, trigeminal neuralgia, maniac effective bipolar disorder, and alcohol withdrawal.[2]

Oxcarbazepine's activity is mediated by its main human metabolite; monohydroxy metabolite (MHD).[3]

[edit] References

  1. ↑ Rogawski and Löscher (2004). The Neurobiology of Antiepileptic Drugs. Nature Reviews Neuroscience (5): 553-564.
  2. ↑ 2.0 2.1 Rogawski and Löscher (2004). The neurobiology of antiepileptic drugs for the treatment of nonepileptic conditions. Nature Medicine (10): 685-692.
  3. ↑ Schmutz et. al (1991). Oxcarbazepine: preclinical anticonvulsant profile and putative mechanisms of action. Epilepsia (35): S47-50.


Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant)
Biological Targets
Compound Names
Receptor Tyrosine Kinases A-83-01 (TGFβ/Activin) · BPIQ-II (EGFR) · Dorsomorphin/LDN-193189 (TGFβ/BMP) · SU5402 (FGFR)
Signaling Kinases A-769662 (AMPK) · BMS-354825 (BCR-ABL, Src)· BIO-Acetoxime (GSK3) · CHIR99021 (GSK3) · GO 6976 (PKC) · IMD-0354 (IκBa) · PD184352 (MAPK) · SB203580 (MAPK) · Y-27632 (ROCK)
G Protein-Coupled Receptor (+)-WIN-55212 (CB1/CB2) · ±-Sulpride (D2) · A 841720 (mGluR1) · BP-554 (5-HT1A) · Hh-Ag1.5 (Smo) · Cyclopamine/KAAD-Cyclopamine (Smo) · SANT1 (Smo) · SB-277011 (D3)
Ion Channels BAY K8644 (Cav1.2) · Bicuculline (GABAAR) · Cymarin (Na+/H+) · G-strophanthin (Na+/H+) · L-AP4 (Na+/H+) · Oxcarbazepine (Na+) · Resiniferatoxin (TRPV1) · Sarmentogenin (Na+/H+) · Theanine (AMPAR, NMDAR)
Transporters O-1783 (DAT) · WF-23 (DAT, SERT)
Nuclear Receptor All-trans retinoic acid (RAR/RXR) · GW501516 (PPARδ) · RU-486 (Nr3c1, Nr3c3)
Protein Phosphatases Endothall (PP2A)
Polypharmacological Phosphoserine (mGluR4) · PK115-584 (Tcf4/β-catenin, PKC) · Pluripotin · Reversine
Other 2C-E (DAT) · 4-methoxyphenyl-HTI-286 (α/β-tubulin) · Compound E/DAPT (presenilin-1) · D-cysteine · D-phenylalanine · Flurbiprofen (COX) · JZL184 (MAGL) · QS11 (RAFGAP1) · RO-28-1675 (glucokinase) · Robotnikinin (Shh) · Selegiline (MAOB)
Uncharacterized Neuropathiazol
Libraries Kinase Inhibitor Library
Publications
Small molecule-mediated manipulation of the adult human induces selective and reversible control of physiological and psychological phenotype (Rubin et. al, 2590. Nature Medicine)
Source · Edit
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