research use only
Cat.No.S1693
| Related Targets | CFTR CRM1 CD markers AChR Calcium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR |
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| Other Sodium Channel Inhibitors | Camostat Mesilate A-803467 cariporide Veratramine Tolperisone HCl Bulleyaconi cine A Vinpocetine Tenapanor PF-06869206 Sparteine |
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In vitro |
DMSO
: 47 mg/mL
(198.92 mM)
Ethanol : 47 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 236.27 | Formula | C15H12N2O |
Storage (From the date of receipt) | |
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| CAS No. | 298-46-4 | Download SDF | Storage of Stock Solutions |
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| Synonyms | NSC 169864 | Smiles | C1=CC=C2C(=C1)C=CC3=CC=CC=C3N2C(=O)N | ||
| Features |
Frequently prescribed first-line drug for the treatment of partial and generalized tonic-clonic epileptic seizures.
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| Targets/IC50/Ki |
Sodium channel
131 μM
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| 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. This compound 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. It does not alter basal 125I-labeled scorpion toxin binding to synaptosomes in the absence of batrachotoxin, but when batrachotoxin (1.25 μM) added, this chemical 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.
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| 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 this compound 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 this chemical (~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.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06357260 | Not yet recruiting | Trigeminal Neuralgia |
Postgraduate Institute of Dental Sciences Rohtak |
April 2024 | Not Applicable |
| NCT06348888 | Recruiting | Advanced Non-small Cell Lung Cancer|EGFR Mutation|HER2 Mutation|Healthy Volunteers |
Bayer |
April 10 2024 | Phase 1 |
| NCT06005688 | Completed | Healthy Participants |
Pfizer|Arvinas Estrogen Receptor Inc. |
August 18 2023 | Phase 1 |
| NCT05860933 | Completed | Healthy |
Eli Lilly and Company|Loxo Oncology Inc. |
May 8 2023 | Phase 1 |
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