Carbamazepine

製品コードS1693 バッチS169302

印刷

化学情報

Chemical Structure Synonyms NSC 169864 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H12N2O
分子量 236.27 CAS No. 298-46-4
Solubility (25°C)* 体外 DMSO 47 mg/mL (198.92 mM)
Ethanol 47 mg/mL (198.92 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
in vitro 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. [1]
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. [2] 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. [3]
特徴 Frequently prescribed first-line drug for the treatment of partial and generalized tonic-clonic epileptic seizures.

プロトコル(参考用のみ)

キナーゼアッセイ [3H]BTX-B binding assay
[3H]BTX-B binding is studied by incubating synaptosomes (1.10 mg/mL) for 30 minutes at 36 °C in the standard incubation medium containing 25 mM KCl and 105 mM choline chloride plus [3H]BTX-B (10 nM), tetrodotoxin (1 μM), scorpion toxin (0.3 or 2 μM), BSA (1 mg/mL), and varying concentrations of Carbamazepine. Nonspecific binding of [3H]BTX-B is determined in the presence of 0.3 mM veratridine. Binding reactions are initiated by the addition of 25 μL of the synaptosomal suspension to 175 μL of the reaction mixture. Samples are rapidly mixed and, following incubation (10 minutes), the reaction is stopped by the addition of 3 mL of ice-cold wash medium consisting of choline chloride (163 mM), 5 mM Hepes-Tris (pH 7.4), CaCl2 (1.8 mM), MgSO4 (0.8 mM), and BSA (1 mg/mL). The synaptosomes are immediately collected on glassfiber filters under vacuum and washed three times with 3 mL of wash medium. Filters containing trapped synaptosomes are suspended in liquid scintillation fluid, and 3H bound is determined in a liquid scintifiation spectrometer. The IC50 determination is calculated by log-probit analysis according to the method of Finney.
動物実験 動物モデル Male Wistar rats
投薬量 ~100 mg/kg
投与方法 Injected intraperitoneally (i.p.)

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Complement Receptor 3 Mediates HIV-1 Transcytosis across an Intact Cervical Epithelial Cell Barrier: New Insight into HIV Transmission in Women [ mBio, 2022, e0217721] PubMed: 35012346
Carbamazepine Induces Platelet Apoptosis and Thrombocytopenia Through Protein Kinase A [ Front Pharmacol, 2021, 12:749930] PubMed: 34658890
A Low Dose of Aripiprazole Has the Strongest Sensitization Effect Among 19 Repositioned Bipolar Drugs in P-gp-overexpressing Drug-resistant Cancer Cells [ Anticancer Res, 2021, 41(2):687-697] PubMed: 33517273
AMPA receptor antagonist perampanel affects glioblastoma cell growth and glutamate release in vitro. [ PLoS One, 2019, 14(2):e0211644] PubMed: 30716120
Effects of MDR1 (C3435T) Polymorphism on Resistance, Uptake, and Efflux to Antiepileptic Drugs [10.1089/dna.2018.4553 DNA Cell Biol, 2019, 10.1089/dna.2018.4553] PubMed: 30632789

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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