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 |
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. |