DT-Web

DB01121 - Phenacemide


Identification
Name Phenacemide
Accession Number DB01121 (APRD00089)
Type small molecule
Description Phenacemide is used to control certain seizures in the treatment of epilepsy. This medicine acts on the central nervous system (CNS) to reduce the number and severity of seizures.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 178.1879
Groups approved
Monoisotopic Weight 178.074227574
Pharmacology
Indication Used to control certain seizures in the treatment of epilepsy.
Mechanism of action Phenacemide binds to and blocks neuronal sodium channels or voltage sensitive calcium channels. This blocks or suppresses neuronal depolarization and hypersynchronization. Hypersynchronization is what often causes seizures.
Absorption Almost completely absorbed.
Protein binding Not Available
Biotransformation Metabolized in the liver by hepatic microsomal enzymes, where it is inactivated by p-hydroxylation.
Route of elimination Not Available
Toxicity Oral, mouse: LD50 = 987 mg/kg; Oral, rabbit: LD50 = 2500 mg/kg; Oral, rat: LD50 = 1600 mg/kg
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions
  • May be taken with food if stomach upset occurs.

Targets


Sodium channel protein type 1 subunit alpha
Name Sodium channel protein type 1 subunit alpha
Gene Name SCN1A
Pharmacological action yes
Actions inhibitor
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Wong MG, Defina JA, Andrews PR: Conformational analysis of clinically active anticonvulsant drugs. J Med Chem. 1986 Apr;29(4):562-72. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.4973

Predictions


Id Partner name Gene Name Score
4512 Cytochrome P450 3A4 CYP3A4 0.0399
6030 Cytochrome P450 2B6 CYP2B6 0.0325
382 Glutamate receptor, ionotropic kainate 1 GRIK1 0.0248
592 Carbonic anhydrase 4 CA4 0.0205
6016 Cytochrome P450 2C19 CYP2C19 0.0174
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0168
357 Carbonic anhydrase 2 CA2 0.016
220 Sodium channel protein type 5 subunit alpha SCN5A 0.011
1588 Multidrug resistance protein 1 ABCB1 0.0106
587 Serum albumin ALB 0.009
233 Potassium channel subfamily K member 2 KCNK2 0.0087
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0082
6158 Solute carrier organic anion transporter family member 1C1 SLCO1C1 0.0081
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.0073
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.0073
6106 Cytochrome P450 2C18 CYP2C18 0.0073
3803 Sodium channel protein type 3 subunit alpha SCN3A 0.0071
6133 Sodium channel subunit beta-2 SCN2B 0.0069
6135 Sodium channel subunit beta-4 SCN4B 0.0069
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0069
6134 Sodium channel subunit beta-3 SCN3B 0.0069
6132 Sodium channel subunit beta-1 SCN1B 0.0069
6127 Carbonic anhydrase-related protein CA8 0.0069
6128 Carbonic anhydrase-related protein 10 CA10 0.0069
6129 Carbonic anhydrase-related protein 11 CA11 0.0069
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.0066
3802 Sodium channel protein type 2 subunit alpha SCN2A 0.0062
6130 Carbonic anhydrase 13 CA13 0.0061
6124 Carbonic anhydrase 5B, mitochondrial CA5B 0.0061
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0058
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0058
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0057
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0057
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0057
6131 Carbonic anhydrase 14 CA14 0.0056
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0056
6091 Gamma-aminobutyric acid receptor subunit theta GABRQ 0.0055
1995 Sodium channel protein type 9 subunit alpha SCN9A 0.0055
6122 Carbonic anhydrase 3 CA3 0.0053
6107 Cytochrome P450 3A7 CYP3A7 0.0053
3804 Sodium channel protein type 4 subunit alpha SCN4A 0.0052
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0052
6123 Carbonic anhydrase 5A, mitochondrial CA5A 0.0051
789 Alpha-1D adrenergic receptor ADRA1D 0.0051
6086 Gamma-aminobutyric acid receptor subunit gamma-2 GABRG2 0.0051
6090 Gamma-aminobutyric acid receptor subunit pi GABRP 0.005
6088 Gamma-aminobutyric acid receptor subunit gamma-3 GABRG3 0.005
6115 Gamma-aminobutyric acid receptor subunit rho-3 GABRR3 0.005
6092 Gamma-aminobutyric acid receptor subunit rho-2 GABRR2 0.005
4118 Cytochrome P450 3A5 CYP3A5 0.005
4100 Gamma-aminobutyric-acid receptor subunit beta-2 GABRB2 0.005
6093 Gamma-aminobutyric acid receptor subunit delta GABRD 0.005
6089 Gamma-aminobutyric acid receptor subunit epsilon GABRE 0.005
6087 Gamma-aminobutyric acid receptor subunit gamma-1 GABRG1 0.005
142 Gamma-aminobutyric-acid receptor subunit rho-1 GABRR1 0.005
4924 Cytochrome P450 2C8 CYP2C8 0.005
378 Alpha-2C adrenergic receptor ADRA2C 0.0049
629 Alpha-2B adrenergic receptor ADRA2B 0.0048
4098 Gamma-aminobutyric-acid receptor subunit beta-1 GABRB1 0.0048
4099 Gamma-aminobutyric-acid receptor subunit beta-3 GABRB3 0.0048
4205 Carbonic anhydrase 9 CA9 0.0048
3007 Carbonic anhydrase 12 CA12 0.0048
193 Beta-1 adrenergic receptor ADRB1 0.0047
4757 Cytochrome P450 2C9 CYP2C9 0.0046
632 Alpha-1B adrenergic receptor ADRA1B 0.0045
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0045
6126 Carbonic anhydrase 7 CA7 0.0045
841 Gamma-aminobutyric-acid receptor subunit alpha-6 GABRA6 0.0045
530 Gamma-aminobutyric-acid receptor subunit alpha-4 GABRA4 0.0045
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0043
318 Alpha-2A adrenergic receptor ADRA2A 0.0043
580 Gamma-aminobutyric-acid receptor subunit alpha-3 GABRA3 0.0042
523 Gamma-aminobutyric-acid receptor subunit alpha-5 GABRA5 0.0042
423 Gamma-aminobutyric-acid receptor subunit alpha-2 GABRA2 0.0042
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.0041
556 Alpha-1A adrenergic receptor ADRA1A 0.004
6020 Aldehyde oxidase AOX1 0.0037
6013 Cytochrome P450 2E1 CYP2E1 0.0035
295 Carbonic anhydrase 1 CA1 0.0034
3939 Amine oxidase [flavin-containing] B MAOB 0.0033
3941 Amine oxidase [flavin-containing] A MAOA 0.0033
4119 Cytochrome P450 2D6 CYP2D6 0.0031
↑