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Drug-Target Interaction

Drug

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PubChem ID:2247
Structure:
Synonyms:
1-((4-Fluorophenyl)methyl)-N-(1-(2-(4-methoxyphenyl)ethyl)-4-piperidinyl)- 1H-benzimidazol-2-amine
1-(p-Fluorobenzyl)-2-((1-(2-(p-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole
1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidaz
1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole
1-[(4-fluorophenyl)methyl]-N-(1-{2-[4-(methyloxy)phenyl]ethyl}piperidin-4-yl)-1H-benzimidazol-2-amine
1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine
1-[(fluorophenyl)-methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
1H-Benzimidazol-2-amine, 1-((4-fluorophenyl)methyl)-N-(1-(2-(4-methoxyphenyl)eth l)-4-piperidinyl)-
1H-Benzimidazol-2-amine, 1-((4-fluorophenyl)methyl)-N-(1-(2-(4-methoxyphenyl)ethyl)-4-piperidinyl)-
1H-Benzimidazol-2-amine, 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-
1H-Benzimidazol-2-amine,1-((4-fluorophenyl)methyl)-N-(1-(2-(4-methoxyphenyl)ethyl)-4-piperdinyl)
68844-77-9
AB00052413
Alermizol
Astemison
Astemizol
Astemizol [German]
Astemizol [INN-Spanish]
Astemizole
Astemizole (JAN/USP/INN)
Astemizole [USAN:BAN:INN]
Astemizolum
Astemizolum [INN-Latin]
Benzimidazole, 1-(p-fluorobenzyl)-2-((1-(2-(p-methoxyphenyl)ethyl)piperid-4-yl)amino)-
BPBio1_000234
BRN 4830190
BSPBio_000212
BSPBio_002684
C06832
C28H31FN4O
CAS-68844-77-9
CCRIS 7595
CHEBI:2896
D00234
DB00637
DivK1c_000039
EINECS 272-441-9
Hestazol
Hestazol, Kelp, Laridal, Retolen, Wareezol, HSBD 6799, BRN 4830190
Hismanal
Hismanal (TN)
Histamen
Histaminos
HSDB 6799
IDI1_000039
KBio1_000039
KBio2_000928
KBio2_003496
KBio2_006064
KBio3_001904
KBioGR_001686
KBioSS_000928
Kelp
Laridal
LS-32978
Metodih
MJD-30
MLS000028667
MLS001148073
NCGC00016913-01
NCGC00018288-01
NCGC00022520-03
NCGC00022520-04
NCGC00022520-05
NCGC00022520-06
NCGC00022520-07
nchembio732-comp2
nchembio806-comp1
NINDS_000039
Novo-mastizol A
NSC329963
Paralergin
Prestwick0_000136
Prestwick1_000136
Prestwick2_000136
Prestwick3_000136
Prestwick_35
QTL1_000010
R 42512
R-43-512
R-43512
Retolen
SMR000058911
SPBio_001804
SPBio_002151
SPECTRUM2300094
Spectrum2_001732
Spectrum3_001072
Spectrum4_001223
Spectrum5_001239
Spectrum_000448
UPCMLD-DP024
UPCMLD-DP024:001
Wareezol
[3H]Astemizole
ATC-Codes:

Target

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Uniprot ID:CP2J2_HUMAN
Synonyms:
Arachidonic acid epoxygenase
CYPIIJ2
Cytochrome P450 2J2
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

12386130
Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole.. Shigeki Matsumoto; Tomoe Hirama; Tsutomu Matsubara; Kiyoshi Nagata; Yasushi Yamazoe (2002) Drug metabolism and disposition: the biological fate of chemicals display abstract
Orally administered astemizole is well absorbed but undergoes an extensive first-pass metabolism to O-desmethylastemizole. Desmethylastemizole is formed in the human microsomal systems of the small intestine as well as the liver, which suggests the role of cytochromes P450 (P450s) in the first-pass metabolism of astemizole. Human P450s involved in the O-demethylation of astemizole have, however, not been identified, and the involvement of twelve known drug-metabolizing P450s were denied. During the course of the P450 identification study, higher activities of the astemizole O-demethylation in the rabbit small intestine than in the liver (about 3-fold) were found. These data suggest the possible involvement of CYP2J, since P450 included in this subfamily is dominantly expressed in the small intestine of rabbits. Therefore, CYP2J2 cDNA has been isolated from the human cDNA library and expressed in COS-1 cells. A clear activity of astemizole O-demethylation was detected in recombinant CYP2J2 with K(m) = 0.65 microM and V(max) = 1129 pmol/nmol P450/min. Expression of the immunoreactive protein with CYP2J2 antibody was detected in the small intestine and liver. Expression levels of the immunoreactive protein with the CYP2J2 antibody in the small intestine were well correlated with the activities of the astemizole O-demethylation (r = 0.901, n = 5, p < 0.05). The CYP2J2 substrates, arachidonic acid and ebastine, strongly inhibited the microsomal astemizole O-demethylation in the human small intestines and recombinant CYP2J2. These results indicate the involvement of CYP2J2 in the presystemic elimination of astemizole in the human small intestine.
12851038
15762770
15861034