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Drug-Target Interaction

Drug

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PubChem ID:441325
Structure:
Synonyms:
19774-82-4
2-Butyl-3-benzofuranyl 4-[(2-diethylamino)ethoxy] 3,5-diiodophenyl ketone, hydrochloride
Amidorone
Amio-Aqueous
Amiodarone
AMIODARONE HYDROCHLORIDE
Amiodarone hydrochloride (JAN)
Ancaro
Ancaron
Ancaron (TN)
calcium channel (L type) blocker
Cordarone
Cordarone (TN)
CPD000058296
D00636
EU-0100122
L-3428
Methanone,
MLS000028520
MLS001076313
NCGC00093613-01
NCGC00093613-02
NCGC00093613-03
NCGC00093613-04
Nexterone
Prestwick_707
RJC 02270
SAM001246646
Sedacoron
Sedacorone
SMR000058296
SPECTRUM2300165
TL8001651
ATC-Codes:

Target

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Uniprot ID:CP1A2_HUMAN
Synonyms:
CYPIA2
Cytochrome P450 1A2
P(3)450
P450 4
P450-P3
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2HI4
Structure:
2HI4

Binding Affinities:

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

References:

11038157
11907638
9578183
Inhibitory effects of antiarrhythmic drugs on phenacetin O-deethylation catalysed by human CYP1A2.. K Kobayashi; M Nakajima; K Chiba; T Yamamoto; M Tani; T Ishizaki; Y Kuroiwa (1998) British journal of clinical pharmacology display abstract
AIMS: The aim of the study was to clarify whether the pharmacokinetic interaction between theophylline and mexiletine is mediated by inhibition of CYP1A2 and to assess the possible interaction potential of other antiarrhythmic drugs with drugs metabolized by CYP1A2. METHODS: The inhibitory effects of mexiletine and 10 antiarrhythmic drugs on phenacetin O-deethylation, a marker reaction of CYP1A2, were studied using human liver microsomes and cDNA-expressed CYP1A2. RESULTS: Propafenone and mexiletine inhibited phenacetin O-deethylation with IC50 values of 29 and 37 microM, respectively. Disopyramide, procainamide and pilsicainide produced negligible inhibition of phenacetin O-deethylation (IC50 >1 mM). Amiodarone, bepridil, aprindine, lignocaine, flecainide and quinidine inhibited phenacetin O-deethylation in a concentration-dependent manner, although the inhibitory effects were relatively weak with IC50 values ranging from 86 to 704 microM. Propafenone and mexiletine selectively abolished the high-affinity component of phenacetin O-deethylation in human liver microsomes. In addition, propafenone and mexiletine inhibited phenacetin O-deethylation catalysed by cDNA-expressed CYP1A2. CONCLUSIONS: These data suggest that, among the antiarrhythmic drugs studied, propafenone and mexiletine are relatively potent inhibitors of CYP1A2, which may cause a drug-drug interaction with drugs metabolized by CYP1A2.