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Carbamazepine

pharmaceutical raw materials
Carbamazepine structure

Carbamazepine 

structure
  • CAS No:

    298-46-4

  • Formula:

    C15H12N2O

  • Chemical Name:

    Carbamazepine

  • Synonyms:

    5H-Dibenz[b,f]azepine-5-carboxamide;G 32883;Geigy 32883;Carbamazepen;Carbamazepine;5-Carbamoyl-5H-dibenz[b,f]azepine;Carbazepine;Tegretol;Tegretal;Finlepsin;Karbamazepin;Neurotol;Amizepin;Stazepine;Carbamazepin;Sirtal;Calepsin;Carbelan;Telesmin;Timonil;Epitol;Biston;NSC 169864;Neurotop;Carbatrol;Tegretol XR;CBZ;Karberol;Karbelex;Equetro;105234-21-7;121947-25-9;121985-71-5

  • Categories:

    Active Pharmaceutical Ingredients  >  Nervous System Drugs

Description

Carbamazepine, a sodium channel blocker, is an anticonvulsant drug.Target: Sodium channelCarbamazepine inhibits the binding of [3H]batrachotoxinin A 20-α-benzoate (BTX-B) to a receptor site of voltage-sensitive sodium channel with IC50 of 131 μM, to decrease the activation of sodium channel ion flux in rat brain synaptosomes. Carbamazepine does not alter basal 125I-labeled scorpion toxin binding to synaptosomes in the absence of batrachotoxin, but when batrachotoxin (1.25 μM) added, Carb

Carbamazepine Basic Attributes

236.27

236.27

206-062-7

2933990090

Characteristics

46.3

2.5

Almost white Crystals

1.3±0.1 g/cm3

190.2 °C

411°C at 760 mmHg

9℃

1.670

Practically insoluble in water;45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: soluble 29mg/mL

2-8°C

1.84X10-7 mm Hg at 25 deg C (est)

LD50 orally in mice, rats: 3750, 4025 mg/kg (Stenger, Roulet)

15.96, -3.8

Safety Information

III

6.1(b)

3249

2

42/43-22-20/21/22-39/23/24/25-23/24/25-11

37-24-22-36/37/39-36-45-36/37-16

HN8225000

Xn,T,F

To study the photostability of carbamazepine polymorphs, the pure materials on the tablet surface were evaluated without physical damage by means of Fourier-transform infrared reflection-absorption infrared spectrometry (FT-IR-RAS) and colorimetric measurement of the carbamazepine polymorphs I, II, and III, after photodegradation at 2 irradiation intensities under a near-UV fluorescent lamp. The surface of sample pellets of all crystalline forms turned gradually from white to yellow-orange upon

P261-P280-P342 + P311

H302-H317-H334

Carbamazepine Use and Manufacturing

Carbamazepine (CBZ) is a first generation anticonvulsant and mood stabilizing compound that has been used as a therapeutic in the context of neuropathic pain, epilepsy, and affective disorders. It exerts its effects by blocking voltage-gated sodium channels (IC50 = 640 μM), making fewer of these channels available to subsequently open, which leads to decreased high-frequency repetitive firing of action potentials. The estimated IC50 values for inhibition of Nav1.7-, Nav1.3-, and Nav1.8-type channels by CBZ following prolonged inactivation have been reported as 406, 900, and 138 μM, respectively. CBZ can also inhibit L-type Ca2+ channels (IC50 = 974 μM) and has been shown to potentiate GABAA receptors (IC50 >3 mM).

Computed Properties

Molecular Weight:236.27
XLogP3:2.5
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:1
Exact Mass:236.094963011
Monoisotopic Mass:236.094963011
Topological Polar Surface Area:46.3
Heavy Atom Count:18
Complexity:326
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Material

Hydrogen peroxide

Drug Function and Efficacy

Anticonvulsant, anti-epileptic, anti-neuropathic pain, anti-manic-depressive, improves the symptoms of certain mental illnesses, and treats central diabetes insipidus; possible mechanisms include use-dependent blocking of various excitable cell membrane Na channels, inhibition of T-type calcium channels, enhancement of central noradrenergic nerve activity, promotion of antidiuretic hormone (ADH) secretion, or increased sensitivity of effectors to ADH.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

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