MEPHENYTOIN


Trade Names	MESANTOIN
Synonyms	Mephenytoin Mesantoin Methoin NSC-34652
Status
Molecule Category	Free-form
ATC	N03AB04
UNII	R420KW629U
EPA CompTox	DTXSID9023257


Active Pharmaceutical Ingredients Bioactive chemicals	Exact Similarity SubStructure	Threshold (%) >= 70


InChI Key	GMHKMTDVRCWUDX-UHFFFAOYSA-N
Smiles	CCC1(c2ccccc2)NC(=O)N(C)C1=O
InChI	InChI=1S/C12H14N2O2/c1-3-12(9-7-5-4-6-8-9)10(15)14(2)11(16)13-12/h4-8H,3H2,1-2H3,(H,13,16)

Mechanism of Action	Action	Reference
Sodium channel alpha subunit blocker	BLOCKER	PubMed PubMed DailyMed


Protein: Sodium channel alpha subunit Description: Sodium channel protein type 1 subunit alpha Organism : Homo sapiens P35498 ENSG00000144285










Protein: Sodium channel alpha subunit Description: Sodium channel protein type 4 subunit alpha Organism : Homo sapiens P35499 ENSG00000007314











Protein: Sodium channel alpha subunit Description: Sodium channel protein type 5 subunit alpha Organism : Homo sapiens Q14524 ENSG00000183873








Protein: Sodium channel alpha subunit Description: Sodium channel protein type 9 subunit alpha Organism : Homo sapiens Q15858 ENSG00000169432







Protein: Sodium channel alpha subunit Description: Sodium channel protein type 2 subunit alpha Organism : Homo sapiens Q99250 ENSG00000136531










Protein: Sodium channel alpha subunit Description: Sodium channel protein type 3 subunit alpha Organism : Homo sapiens Q9NY46 ENSG00000153253









Protein: Sodium channel alpha subunit Description: Sodium channel protein type 11 subunit alpha Organism : Homo sapiens Q9UI33 ENSG00000168356







Protein: Sodium channel alpha subunit Description: Sodium channel protein type 8 subunit alpha Organism : Homo sapiens Q9UQD0 ENSG00000196876











Protein: Sodium channel alpha subunit Description: Sodium channel protein type 10 subunit alpha Organism : Homo sapiens Q9Y5Y9 ENSG00000185313

Targets	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2C Cytochrome P450 2C19	-	-	-	-	97
Transporter Electrochemical transporter SLC superfamily of solute carriers SLC21/SLCO family of organic anion transporting polypeptides	-	-	-	-

Assay Description	Organism	Bioactivity
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting	Homo sapiens	-5.7 %
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting	Homo sapiens	-0.6 %
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting	Homo sapiens	32.9 %
Inhibition of human CYP2C19 at 10 uM	Homo sapiens	96.83 %

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