Catalog No.S1693 Synonyms: NSC 169864
Molecular Weight(MW): 236.27
Carbamazepine (Carbatrol) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
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|Description||Carbamazepine (Carbatrol) 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.|
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. |
|In vitro||DMSO||47 mg/mL (198.92 mM)|
|Ethanol||18 mg/mL (76.18 mM)|
|In vivo||Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03031184||Recruiting||Dementia||University of Sussex|Norwich Clinical Trials Unit|University of East Anglia|University of Cambridge|University College, London|London School of Economics and Political Science|University of Manchester|University of Newcastle Upon-Tyne|Birmingham and Solihull Mental Health NHS Foundation Trust|Alzheimers Society|The Centre for Dementia Studies, Brighton and Sussex Medical School and SPFT||January 2017||Phase 3|
|NCT02893371||Not yet recruiting||Bipolar Disorder||University of New Mexico|Patient-Centered Outcomes Research Institute|Montana State University|National Alliance on Mental Illness|CGStat LLC|Risk Benefit Statistics LLC||September 2016||--|
|NCT02912364||Recruiting||Epilepsy||Stanford University|Sunovion||July 2016||Phase 4|
|NCT02705768||Recruiting||Seizures, Focal||All India Institute of Medical Sciences, Bhubaneswar||April 2016||Phase 4|
|NCT02707965||Not yet recruiting||Epilepsy||Food and Drug Administration (FDA)|University of Maryland||March 2016||--|
|NCT02623504||Recruiting||Bipolar Disorder||Validus Pharmaceuticals||January 2016||Phase 4|
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