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Drug-Target Interaction

Drug

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PubChem ID:38945
Structure:
Synonyms:
(-)-2-Amino-N-(2,6-dimethylphenyl)propanamide
(S)-Tocainide
2',6'-Propionoxylidide, 2-amino-
2-Amino-2',6'-propionoxylidide
2-AMINO-N-(2,6-DIMETHYLPHENYL)PROPANAMIDE
2-Amino-N-(2,6-dimethylphenyl)propionamid
35891-93-1
35891-93-1 (mono-hydrochloride)
41708-72-9
53984-26-2
53984-75-1
76213-25-7
AB00514717
AC-16017
AC1L20PS
AC1Q5LWE
Alanyl-2,6-xylidide
Ambap41708-72-9
Astra W 36095
BPBio1_001335
BRD-A92670106-003-03-9
BRN 2416564
BSPBio_001213
C07142
C11H16N2O
CCG-100842
CHEBI:9611
CHEMBL1762
CPD000466388
D06172
DB01056
EINECS 255-505-0
HMS2051G06
HMS2232D16
LS-125003
MLS000759525
MLS001423966
N-(2,6-dimethylphenyl)alaninamide
NCGC00162129-01
NCGC00162129-02
NCGC00162129-03
Prestwick0_001027
Prestwick1_001027
Prestwick2_001027
Prestwick3_001027
Propanamide, 2-amino-N-(2,6-dimethylphenyl)-
Propanamide, 2-amino-N-(2,6-dimethylphenyl)-, (-)-
Propanamide, 2-amino-N-(2,6-dimethylphenyl)-, (S)-
SAM001246759
SMR000466388
SPBio_003074
Taquidil
Tocainida
Tocainida [INN-Spanish]
Tocainide
Tocainide (USAN/INN)
Tocainide Hydrochloride
Tocainide [USAN:BAN:INN]
Tocainidum
Tocainidum [INN-Latin]
Tonocard
UNII-27DXO59SAN
W-36095
ATC-Codes:

Target

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Uniprot ID:CP1A1_HUMAN
Synonyms:
CYPIA1
Cytochrome P450 1A1
P450 form 6
P450-C
P450-P1
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

8689940
Relative potency of mexiletine, lidocaine, and tocainide as inhibitors of rat liver CYP1A1 activity.. X Wei; C M Loi; E J Jarvi; R E Vestal (1995) Drug metabolism and disposition: the biological fate of chemicals display abstract
Mexiletine and tocainide are lidocaine congeners that share similar chemical structures. Clinical studies suggest that the in vivo inhibitory effect of mexiletine on the CYP1A family of isoforms is substantially greater than that of tocainide. We investigated the inhibitory property of mexiletine, lidocaine, and tocainide on the in vitro activity of the cytochrome P4501A1 (CYP1A1) isozyme in the rat. Hepatic microsomes were prepared from rat livers induced with 3-methylcholanthrene. The rate of ethoxyresorufin-O-dealkylation (EROD) was used as an index of CYP1A1 activity. Vmax and KM of the reactions were determined from Lineweaver-Burk plots. The Ki values for the inhibitors were derived from Dixon plots. Results showed that mexiletine is a competitive inhibitor, lidocaine is a mixed inhibitor, and tocainide is a noncompetitive inhibitor of EROD. The Ki values for mexiletine and tocainide were 0.30 +/- 0.02 mM and 12.4 +/- 0.7 mM, respectively. Two Ki values for lidocaine were determined. They were 0.65 +/- 0.07 mM and 4.1 +/- 1.3 mM, respectively. The relative inhibitory potency of these agents on rat CYP1A1 activity is mexiletine > lidocaine > tocainide. This difference in potency, which is most likely attributable to the change in the chemical composition in the aliphatic chain among the compounds, suggests that these compounds may be useful probes for studying the mechanism of the interaction with the active site of CYP1A1.