Home Transmembrane Transporters Sodium Channel inhibitor - Autophagy activator Carbamazepine For research use only.

Carbamazepine

Synonyms: NSC 169864

Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.

Carbamazepine Chemical Structure

Carbamazepine Chemical Structure

CAS: 298-46-4

Selleck's Carbamazepine has been cited by 5 publications

Purity & Quality Control

Batch: Purity: 99.93%
99.93

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Biological Activity

Description Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
Features Frequently prescribed first-line drug for the treatment of partial and generalized tonic-clonic epileptic seizures.
Targets
Sodium channel [1]
131 μM
In vitro
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
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]
Animal Research Animal Models Male Wistar rats
Dosages ~100 mg/kg
Administration Injected intraperitoneally (i.p.)
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06005688 Active not recruiting Healthy Participants Pfizer|Arvinas Estrogen Receptor Inc. August 18 2023 Phase 1
NCT05860933 Recruiting Healthy Eli Lilly and Company|Loxo Oncology Inc. May 8 2023 Phase 1

Chemical lnformation & Solubility

Molecular Weight 236.27 Formula

C15H12N2O
CAS No. 298-46-4 SDF Download Carbamazepine SDF
Smiles C1=CC=C2C(=C1)C=CC3=CC=CC=C3N2C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 47 mg/mL ( (198.92 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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