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28721-07-5

28721-07-5 structure
28721-07-5 structure
  • Name: Oxcarbazepine
  • Chemical Name: oxcarbazepine
  • CAS Number: 28721-07-5
  • Molecular Formula: C15H12N2O2
  • Molecular Weight: 252.268
  • Catalog: API Nervous system medication Antiepileptic and anticonvulsant
  • Create Date: 2018-08-05 07:57:25
  • Modify Date: 2024-01-02 07:09:59
  • Oxcarbazepine inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.Target: Sodium ChannelOxcarbazepine is an antiepileptic drug with a chemical structure similar to carbamazepine, but with different metabolism. Oxcarbazepine is rapidly reduced to 10,11-dihydro-10-hydroxy-carbazepine (monohydroxy derivative, MHD), the clinically relevant metabolite of oxcarbazepine. MHD has (S)-(+)- and the (R)-(-)-enantiomer [1]. Oxcarbazepine (oxcarb) 600 and 900 mg (2360 and 3540 mumol) was taken by 3 volunteers (2 female, 1 male; 45-67 kg; age 22-34 years) after an overnight fast. Blood, saliva and urine were collected for the next 72 h for assay of oxcarb, 10,11-dihydro-10-hydroxy-carbamazepine (OHcarb), and 10,11-dihydro-trans-10,11-dihydroxy-carbamazepine (diol). Oxcarb reached a maximum level of about 1 microgram/ml (3.93 mumol/l) within 1 h and dropped below the detection limit (0.1 microgram/ml = 0.39 mumol/l) within 3 h. The active metabolite OHcarb appeared in the blood before oxcarb and reached the higher maximum level of 7.4 microgram/ml (29 mumol/l) after 7 h [2]. Clinical indications: EpilepsyToxicity: Isolated cases of overdose with oxcarbazepine have been reported. The maximum dose taken was approximately 24,000 mg. All patients recovered with symptomatic treatment.

Name oxcarbazepine
Synonyms 10,11-Dihydro-10-oxo-5h-dibenz[b,f]azepine-5-carboxamide,Oxacarbazepine
10,11-Dihydro-10-oxo-5h-dibenz[b,f]azepine-5-carboxamide Oxacarbazepine
Oxecarb
OXCARBAMAZEPINE
Trileptal
Oxcarbapezine
Ocarbazepine
Oxetol
Aurene
Oxcarbazepine
10-Oxo-10,11-dihydro-dibenzo[b,f]azepine-5-carboxylic acid amide
10,11-Dihydro-10-oxo-5H-dibenzo[b,f]azepine-5-carboxamide
10,11-Dihydro-10-oxo-5H-dibenz(b,f)azepine-5-carboxamide
10-Oxo-10,11-dihydro-5H-dibenzo[b,f]azepine-5-carboxamide
5H-Dibenz[b,f]azepine-5-carboxamide, 10,11-dihydro-10-oxo-
EINECS 249-188-8
OXACARBAZEPINE
MFCD00865307
Description Oxcarbazepine inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.Target: Sodium ChannelOxcarbazepine is an antiepileptic drug with a chemical structure similar to carbamazepine, but with different metabolism. Oxcarbazepine is rapidly reduced to 10,11-dihydro-10-hydroxy-carbazepine (monohydroxy derivative, MHD), the clinically relevant metabolite of oxcarbazepine. MHD has (S)-(+)- and the (R)-(-)-enantiomer [1]. Oxcarbazepine (oxcarb) 600 and 900 mg (2360 and 3540 mumol) was taken by 3 volunteers (2 female, 1 male; 45-67 kg; age 22-34 years) after an overnight fast. Blood, saliva and urine were collected for the next 72 h for assay of oxcarb, 10,11-dihydro-10-hydroxy-carbamazepine (OHcarb), and 10,11-dihydro-trans-10,11-dihydroxy-carbamazepine (diol). Oxcarb reached a maximum level of about 1 microgram/ml (3.93 mumol/l) within 1 h and dropped below the detection limit (0.1 microgram/ml = 0.39 mumol/l) within 3 h. The active metabolite OHcarb appeared in the blood before oxcarb and reached the higher maximum level of 7.4 microgram/ml (29 mumol/l) after 7 h [2]. Clinical indications: EpilepsyToxicity: Isolated cases of overdose with oxcarbazepine have been reported. The maximum dose taken was approximately 24,000 mg. All patients recovered with symptomatic treatment.
Related Catalog
References

[1]. May, T.W., E. Korn-Merker, and B. Rambeck, Clinical pharmacokinetics of oxcarbazepine. Clin Pharmacokinet, 2003. 42(12): p. 1023-42.

[2]. Theisohn, M. and G. Heimann, Disposition of the antiepileptic oxcarbazepine and its metabolites in healthy volunteers. Eur J Clin Pharmacol, 1982. 22(6): p. 545-51.

Density 1.3±0.1 g/cm3
Boiling Point 457.2±55.0 °C at 760 mmHg
Melting Point 215-216°C
Molecular Formula C15H12N2O2
Molecular Weight 252.268
Flash Point 230.3±31.5 °C
Exact Mass 252.089874
PSA 63.40000
LogP 1.44
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.662
Storage condition Store at RT
Water Solubility DMSO: ~9 mg/mL

CHEMICAL IDENTIFICATION

RTECS NUMBER :
HN8445000
CHEMICAL NAME :
5H-Dibenz(b,f)azepine-5-carboxamide, 10,11-dihydro-10-oxo-
CAS REGISTRY NUMBER :
28721-07-5
LAST UPDATED :
199806
DATA ITEMS CITED :
1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
14300 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 279,1237,1996
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes Xn,F
Risk Phrases 22-36-20/21/22-11
Safety Phrases 16-36/37
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS HN8445000
HS Code 2933990090
HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%