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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:CP2D6_HUMAN
Synonyms:
CYPIID6
Cytochrome P450 2D6
Debrisoquine 4-hydroxylase
P450-DB1
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2F9Q
Structure:
2F9Q

Binding Affinities:

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

References:

010597902
11259984
Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine.. S Matsumoto; Y Yamazoe (2001) British journal of clinical pharmacology display abstract
AIMS: The aims of the present study were to investigate the metabolism of astemizole in human liver microsomes, to assess possible pharmacokinetic drug-interactions with astemizole and to compare its metabolism with terfenadine, a typical H1 receptor antagonist known to be metabolized predominantly by CYP3A4. METHODS: Astemizole or terfenadine were incubated with human liver microsomes or recombinant cytochromes P450 in the absence or presence of chemical inhibitors and antibodies. RESULTS: Troleandomycin, a CYP3A4 inhibitor, markedly reduced the oxidation of terfenadine (26% of controls) in human liver microsomes, but showed only a marginal inhibition on the oxidation of astemizole (81% of controls). Three metabolites of astemizole were detected in a liver microsomal system, i.e. desmethylastemizole (DES-AST), 6-hydroxyastemizole (6OH-AST) and norastemizole (NOR-AST) at the ratio of 7.4 : 2.8 : 1. Experiments with recombinant P450s and antibodies indicate a negligible role for CYP3A4 on the main metabolic route of astemizole, i.e. formation of DES-AST, although CYP3A4 may mediate the relatively minor metabolic routes to 6OH-AST and NOR-AST. Recombinant CYP2D6 catalysed the formation of 6OH-AST and DES-AST. Studies with human liver microsomes, however, suggest a major role for a mono P450 in DES-AST formation. CONCLUSIONS: In contrast to terfenadine, a minor role for CYP3A4 and involvement of multiple P450 isozymes are suggested in the metabolism of astemizole. These differences in P450 isozymes involved in the metabolism of astemizole and terfenadine may associate with distinct pharmacokinetic influences observed with coadministration of drugs metabolized by CYP3A4.