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Drug-Target Interaction

Drug

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PubChem ID:3001055
Structure:
Synonyms:
(E)-N-[2-[[5-(dimethylaminomethyl)furan-2-yl]methylsulfanyl]ethyl]-N'-methyl-2-nitroethene-1,1-diamine
(E)-N-{2-[({5-[(dimethylamino)methyl]-2-furyl}methyl)sulfanyl]ethyl}-N'-methyl-2-nitroethene-1,1-diamine
1,1-Ethenediamine,
1,1-Ethenediamine, N-(2-(((5-((dimethylamino)methyl)-2-furanyl)methyl)thio)ethyl)-N'-methyl-2-nitro-
1,1-Ethenediamine, N-[2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl]-N'-methyl-2-nitro-, (E)-
66357-35-5
66357-59-3
Achedos
Acidex
AH-19065
AIDS-032971
AIDS032971
Atural
Axoban
Biotidin
C13H22N4O3S
CAS-66357-59-3
CHEBI:8776
Coralen
Curan
D00422
DB00863
Duractin
EINECS 266-332-5
Ezopta
Gastrial
Gastrosedol
HSDB 3925
IDI1_000440
Istomar
Logast
Lopac-R-101
Lopac0_001073
LS-67645
Mauran
Microtid
N (2-(((5-((Dimethylamino)methyl)-2-furanyl)methyl)thio)ethyl)-N'-methyl-2-nitro-1,1-ethenediamine
N-(2-((5-((Dimethylamino)methyl)furfuryl)thio)ethyl)-N'-methyl-2-nitro-1,1-ethenediamine
NCGC00015876-01
NCGC00015876-02
NCGC00018108-01
NCGC00024387-02
NCGC00094913-01
NCGC00094913-02
NCGC00094913-03
NCGC00094913-04
NCGC00094913-05
Prestwick2_000201
Ptinolin
Quantor
Quicran
Radinat
Randin
Ranidine
Ranin
Raniogas
Ranisen
Raniter
Ranitidin
Ranitidina
Ranitidina [INN-Spanish]
RANITIDINE
Ranitidine (TN)
Ranitidine (USAN/INN)
Ranitidine Base
Ranitidine HCL
Ranitidine hydrochloride
Ranitidine [USAN:BAN:INN]
Ranitidinum
Ranitidinum [INN-Latin]
Ranitiget
Rantacid
Rantidine
Rantidine HCL
Ratic
Raticina
RND
Sampep
SBB006527
Sostril
SPECTRUM1501151
Spectrum5_001189
Taural
Tocris-1967
Ul-Pep
Ulceranin
Urantac
Verlost
Vesyca
Vizerul
Weichilin
Weidos
Xanidine
Zantab
ZANTAC
Zantadin
Zantic
ATC-Codes:

Target

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Uniprot ID:Q38LG2_HUMAN
Synonyms:
Cytochrome P450 2D6
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

10223772
Comparative in vitro and in vivo inhibition of cytochrome P450 CYP1A2, CYP2D6, and CYP3A by H2-receptor antagonists.. C Martínez; C Albet; J A Agúndez; E Herrero; J A Carrillo; M Márquez; J Benítez; J A Ortiz (1999) Clinical pharmacology and therapeutics display abstract
The isozymes CYP1A2, CYP2D6, and CYP3A4/5 are involved in the majority of all cytochrome P450-mediated drug biotransformations. In this study we investigated the inhibition profiles of CYP1A2 (substrate: caffeine) CYP2D6 (substrate: dextromethorphan), and CYP3A4/5 (substrate: dextrorphan) by cimetidine, ranitidine, and the novel H2-receptor antagonist ebrotidine in human liver microsomes. The inhibitory effect of the drugs on the enzymes activities were as follows: CYP1A2: cimetidine >> ranitidine = ebrotidine; CYP2D6: cimetidine >>> ranitidine = ebrotidine; CYP3A4/5: ebrotidine > cimetidine >>> ranitidine. The inhibition of CYP3A4/5 enzyme activity by ebrotidine was competitive. To test whether the inhibitory effect of ebrotidine in CYP3A activity was also found in vivo, we analyzed the biodisposition of midazolam in 8 healthy volunteers. Midazolam biodisposition was significantly reduced when administered together with cimetidine (P < .05), whereas no significant inhibition was observed with ebrotidine or ranitidine compared with placebo. Psychomotor performance analysis revealed no significant effect of the observed reduction on midazolam biodisposition. We concluded that patients who are receiving treatment with drugs metabolized through CYP3A may experience enhanced drug effects as a result of pharmacokinetic interaction when treated concomitantly with cimetidine. In contrast, the effect of ranitidine or ebrotidine on CYP3A activity in vivo seems to have little clinical significance.