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Drug-Target Interaction

Drug

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PubChem ID:2157
Structure:
Synonyms:
(2-butyl-1-benzofuran-3-yl)(4-{[2-(diethylamino)ethyl]oxy}-3,5-diiodophenyl)methanone
(2-butyl-1-benzofuran-3-yl)-[4-(2-diethylaminoethoxy)-3,5-diiodophenyl]methanone
(2-butyl-1-benzofuran-3-yl){4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl}methanone
(2-Butyl-3-benzofuranyl)(4-(2-(diethylamino)ethoxy)-3,5-diidophenyl)methanone
(2-Butylbenzofuran-3-yl)-[4-(2-diethylaminoethoxy)-3,5-diiodo-phenyl]-methanone
1951-25-3
2-Butyl-3-(3,5-diiodo-4-(2-diethylaminoethoxy)benzoyl)benzofuran
2-Butyl-3-(3,5-diiodo-4-(beta-diethylaminoethoxy)benzoyl)benzofuran
2-Butyl-3-(4'-beta-N-diethylaminoethoxy-3',5'-diiodobenzoyl)benzofuran
2-Butyl-3-benzofuranyl 4-(2-(diethylamino)ethoxy)-3,5-diiodophenyl ketone
2-Butyl-3-benzofuranyl p-((2-diethylamino)ethoxy)-m,m-diiodophenyl ketone
2-n-Butyl-3',5'-diiodo-4'-N-diethylaminoethoxy-3-benzoylbenzofuran
5-18-02-00353 (Beilstein Handbook Reference)
AB00053422
AIDS-114337
AIDS114337
Alphapharm Brand of Amiodarone Hydrochloride
Amidorone
Amiobeta
Amiodarex
Amiodarona
Amiodarona [INN-Spanish]
Amiodarone
Amiodarone (USAN/INN)
Amiodarone Base
Amiodarone HCL
Amiodarone Hydrochloride
Amiodarone [USAN:BAN:INN]
Amiodaronum [INN-Latin]
Amiohexal
Amjodaronum
Aratac
Armstrong Brand of Amiodarone Hydrochloride
ASTA Medica Brand of Amiodarone Hydrochloride
Berenguer Infale Brand of Amiodarone Hydrochloride
Betapharm Brand of Amiodarone Hydrochloride
Bio1_000026
Bio1_000515
Bio1_001004
Bio2_000294
Bio2_000774
BPBio1_000372
Braxan
BRN 1271711
BSPBio_000338
BSPBio_001574
BSPBio_002580
C06823
C25H29I2NO3
CAS-19774-82-4
CBiol_001740
CHEBI:2663
Corbionax
Cordarex
Cordarone
D000638
D02910
DB01118
DivK1c_000079
EINECS 217-772-1
G Gam Brand of Amiodarone Hydrochloride
Hexal Brand of Amiodarone Hydrochloride
IDI1_000079
IDI1_034044
KBio1_000079
KBio2_000294
KBio2_000741
KBio2_002862
KBio2_003309
KBio2_005430
KBio2_005877
KBio3_000587
KBio3_000588
KBio3_001800
KBioGR_000294
KBioGR_001859
KBioSS_000294
KBioSS_000741
Ketone, 2-butyl-3-benzofuranyl 4-(2-(diethylamino)ethoxy)-3,5-diiodophenyl
Kordaron
L 3428
L-3428
L3428
Leurquin Brand of Amiodarone Hydrochloride
Lopac-A-8423
Lopac0_000122
LS-87088
Methanone,
Methanone, (2-butyl-3-benzofuranyl)(4-(2-(diethylamino)ethoxy)-3,5-diiodophenyl)-
Methanone, (2-butyl-3-benzofuranyl)[4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl]-
NCGC00015096-01
NCGC00015096-02
NCGC00015096-03
NCGC00024242-03
NCGC00024242-04
NCGC00024242-05
NCGC00024242-06
nchembio.79-comp9
nchembio732-comp1
NCI60_041885
NINDS_000079
Ortacrone
Pacerone
Pharma Investi Brand of Amiodarone Hydrochloride
Prestwick0_000409
Prestwick1_000409
Prestwick2_000409
Prestwick3_000409
QTL1_000008
Rytmarone
Sanofi Winthrop Brand of Amiodarone Hydrochloride
Sedacoron
Sedacorone
SKF 33134 A
SKF 33134-A
SKF 33134A
SPBio_001825
SPBio_002277
Spectrum2_001813
Spectrum3_001050
Spectrum4_001190
Spectrum5_001533
Spectrum_000261
Tachydaron
Trangorex
UNM000001215003
Wyeth Brand of Amiodarone Hydrochloride
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.