Carbamazepine(CBZ NSC 169864)

Molecular Weight (MW)	236.27
Formula	C15H12N2O
CAS No.	298-46-4
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 47 mg/mL (198.9 mM)
Water:<1 mg/mL
Ethanol: 18 mg/mL (76.2 mM)
Solubility (In vivo)	1% DMSO+30% polyethylene glycol+1% Tween 80: 5 mg/mL
Other info	Synonyms: NSC 169864; Carbamazepine, NSC 69864; NSC-169864; Tegretol, Epitol IUPAC/Chemical Name: benzo[b][1]benzazepine-11-carboxamide InChi Key: RYLOOVOCHDAWIL-UHFFFAOYSA-N InChi Code: InChI=1S/C15H12N2O/c16-15(18)12-9-10-5-1-3-7-13(10)17-14-8-4-2-6-11(12)14/h1-9,17H,(H2,16,18) SMILES Code: O=C(C1=CC2=CC=CC=C2NC3=CC=CC=C13)N

Molecular Weight (MW)

236.27

Formula

C15H12N2O

CAS No.

298-46-4

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 47 mg/mL (198.9 mM)

Water:<1 mg/mL

Ethanol: 18 mg/mL (76.2 mM)

Solubility (In vivo)

1% DMSO+30% polyethylene glycol+1% Tween 80: 5 mg/mL

Other info

Synonyms: NSC 169864; Carbamazepine, NSC 69864; NSC-169864; Tegretol, Epitol
IUPAC/Chemical Name: benzo[b][1]benzazepine-11-carboxamide
InChi Key: RYLOOVOCHDAWIL-UHFFFAOYSA-N
InChi Code: InChI=1S/C15H12N2O/c16-15(18)12-9-10-5-1-3-7-13(10)17-14-8-4-2-6-11(12)14/h1-9,17H,(H2,16,18)
SMILES Code: O=C(C1=CC2=CC=CC=C2NC3=CC=CC=C13)N

In Vitro	In vitro activity: Carbamazepine 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 reduces receptor affinity due to an increased rate of ligand dissociation from the receptor-ligand complex, without altering maximal binding capacity from the scatchard analysis of BTX-B binding to synaptosome, suggesting an indirect allosteric mechanism for anticonvulsant inhibition of BTX-B binding. Carbamazepine does not alter basal 125I-labeled scorpion toxin binding to synaptosomes in the absence of batrachotoxin, but when batrachotoxin (1.25 μM) added, Carbamazepine inhibits the batrachotoxin-dependent increase in scorpion toxin binding in a concentration-dependent manner with IC50 of 260 μM mediated at the alkaloid toxin binding site, none of which affects [3H]saxitoxin binding.
In Vivo	Carbamazepine at 25 mg/kg significantly increases extracellular levels of striatal and hippocampal dopamine (DA), 3,4-dihydroxyphenylalanine (DOPA), 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in a dose dependent manner, while Carbamazepine at 50 mg/kg significantly decreases total levels of striatal DA and DOPA as well as hippocampal HVA, but has no effect on total levels of striatal DOPAC and HVA nor on hippocampal DA, DOPA and DOPAC. Intraperitoneal administration of Carbamazepine （~100 mg/kg）to rats produces significant increases in the cerebral cortical concentrations of neuroactive steroids and neuroactive steroids in plasma in a dose and time dependent maner with DHEA formed as a result of side chain cleavage of pregnenolone not affected.
Animal model	Male Wistar rats
Formulation & Dosage	Dissolved in saline/DMSO (50/50 vol/vol); 100 mg/kg; i.p. injection
References	Mol Pharmacol. 1982 Nov;22(3):627-35; Epilepsy Res. 1997 Sep;28(2):143-53.

In Vitro

In vitro activity: Carbamazepine 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 reduces receptor affinity due to an increased rate of ligand dissociation from the receptor-ligand complex, without altering maximal binding capacity from the scatchard analysis of BTX-B binding to synaptosome, suggesting an indirect allosteric mechanism for anticonvulsant inhibition of BTX-B binding. Carbamazepine does not alter basal 125I-labeled scorpion toxin binding to synaptosomes in the absence of batrachotoxin, but when batrachotoxin (1.25 μM) added, Carbamazepine inhibits the batrachotoxin-dependent increase in scorpion toxin binding in a concentration-dependent manner with IC50 of 260 μM mediated at the alkaloid toxin binding site, none of which affects [3H]saxitoxin binding.

In Vivo

Carbamazepine at 25 mg/kg significantly increases extracellular levels of striatal and hippocampal dopamine (DA), 3,4-dihydroxyphenylalanine (DOPA), 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in a dose dependent manner, while Carbamazepine at 50 mg/kg significantly decreases total levels of striatal DA and DOPA as well as hippocampal HVA, but has no effect on total levels of striatal DOPAC and HVA nor on hippocampal DA, DOPA and DOPAC. Intraperitoneal administration of Carbamazepine （~100 mg/kg）to rats produces significant increases in the cerebral cortical concentrations of neuroactive steroids and neuroactive steroids in plasma in a dose and time dependent maner with DHEA formed as a result of side chain cleavage of pregnenolone not affected.

Animal model

Male Wistar rats

Formulation & Dosage

Dissolved in saline/DMSO (50/50 vol/vol); 100 mg/kg; i.p. injection

References

Mol Pharmacol. 1982 Nov;22(3):627-35; Epilepsy Res. 1997 Sep;28(2):143-53.

CAS NO:	298-46-4
规格:	≥98%

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议
1g	电议
5g	电议
10g	电议