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Carbamazepine

Catalog No. T0943 CAS 298-46-4

Synonyms: NSC 169864

Carbamazepine (NSC-169864) is a tricyclic compound chemically related to tricyclic antidepressants (TCA) with anticonvulsant and analgesic properties. Carbamazepine exerts its anticonvulsant activity by reducing polysynaptic responses and blocking post-tetanic potentiation. Its analgesic activity is not understood; however, carbamazepine is commonly used to treat pain associated with trigeminal neuralgia.

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Carbamazepine, CAS 298-46-4

Pack Size	Availability	Price/USD
100 mg	In stock	$ 37.00
200 mg	In stock	$ 42.00
500 mg	In stock	$ 50.00
1 mL * 10 mM (in DMSO)	In stock	$ 42.00

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Purity: 100%

Purity: 99.88%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Carbamazepine (NSC-169864) is a tricyclic compound chemically related to tricyclic antidepressants (TCA) with anticonvulsant and analgesic properties. Carbamazepine exerts its anticonvulsant activity by reducing polysynaptic responses and blocking post-tetanic potentiation. Its analgesic activity is not understood; however, carbamazepine is commonly used to treat pain associated with trigeminal neuralgia.
Targets&IC50	Na+ channel:131 μM
In vitro	Treatment with Carbamazepine (25 mg/kg) significantly increases the levels of hippocampal dopamine, dihydroxyphenylalanine (DOPA), striatal homovanillic acid, and 3,4-dihydroxyphenylacetic acid, with these effects being dose-dependent. However, a higher dose of Carbamazepine (50 mg/kg) markedly reduces the overall hippocampal homovanillic acid and striatal DOPA and dopamine levels, while not affecting hippocampal dopamine, DOPA, and DOPAC levels, nor overall striatal DOPAC and homovanillic acid. At a dose of Carbamazepine (100 mg/kg, i.p.), there is a dose-dependent significant increase in the concentrations of neuroactive steroids in rat plasma corticosterone.
In vivo	In the presence of batrachotoxin, carbamazepine did not alter the binding of scorpion toxin (125I-labeled) to synaptosomes; however, upon the addition of 1.25 μM batrachotoxin, carbamazepine concentration dependently inhibited the enhancement of batrachotoxin-dependent scorpion toxin binding (IC50: 260 μM) via regulatory sites of the toxin alkaloid. Importantly, carbamazepine had no effect on [3H]saxitoxin binding. When acting on rat brain synaptosomes, carbamazepine impeded the binding of [3H]Batrachotoxinin A 20-α-benzoate to the voltage-sensitive sodium channel site (IC50: 131 μM), thereby reducing the ion flow activity of the sodium channels. As the dissociation rate of the ligand from the receptor-ligand complex increased, carbamazepine, despite decreasing receptor affinity, did not change the maximal binding capacity in Scatchard analyses of [3H]Batrachotoxinin A 20-α-benzoate to synaptosomes, suggesting that binding of [3H]Batrachotoxinin A 20-α-benzoate inhibits conformational changes associated with anticonvulsant effects.

Synonyms	NSC 169864
Molecular Weight	236.27
Formula	C15H12N2O
CAS No.	298-46-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 44 mg/mL (186.2 mM)

Ethanol: 15 mg/mL (63.5 mM)

References and Literature

1. Willow M, et al. Mol Pharmacol, 1982, 22(3), 627-635. 2. Okada M, et al. Epilepsy Res, 1997, 28(2), 143-153. 3. Serra M, et al. Neuropharmacology, 2000, 39(12), 2448-2456. 4. Li H, Zhou D S, Chang H, et al. Interactome Analyses implicated CAMK2A in the genetic predisposition and pharmacological mechanism of Bipolar Disorder[J]. Journal of psychiatric research. 2019. 5. . Carbamazepine promotes specific stimuli induced NLRP3 inflammasome activation and causes idiosyncratic liver injury in mice . Archives of Toxicology. 2019

Citations

1. Li H, Zhou D S, Chang H, et al. Interactome Analyses implicated CAMK2A in the genetic predisposition and pharmacological mechanism of Bipolar Disorder. Journal of Psychiatric Research. 2019

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Bioactive Compounds Library Max Autophagy Compound Library ReFRAME Related Library Pediatric Drug Library Human Metabolite Library

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Keywords

Carbamazepine 298-46-4 Autophagy Membrane transporter/Ion channel Mitophagy Sodium Channel CBZ NSC169864 inhibit Inhibitor Na channels NSC-169864 Mitochondrial Autophagy Na+ channels NSC 169864 inhibitor

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