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Drug-Target Interaction

Drug

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PubChem ID:3961
Structure:
Synonyms:
(2-butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)methanol
(2-butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-1H-imidazol-5-yl)methanol
114798-26-4
124750-99-8
1H-Imidazole-5-methanol, 2-butyl-4-chloro-1-((2'-(1H-tetrazol-5-yl)(1,1'-
1H-Imidazole-5-methanol, 2-butyl-4-chloro-1-((2'-(1H-tetrazol-5-yl)(1,1'- biphenyl)-4-yl)methyl)-
1H-Imidazole-5-methanol, 2-butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]- (9CI)
1H-imidazole-5-methanol, 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
2-Butyl-4-chloro-1-((2'-(1H-etrazol-5-yl) (1,1'-biphenyl)-4-yl)methyl)-1H-imidazole-5-methanol
2-butyl-4-chloro-1-[p-(o-1H-tetrazol-5ylphenyl)benzyl]imidazole-5-methanol
2-Butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl-1H-imidazole-5-methanol
2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]imidazole
2-n-butyl-4-chloro-5-hydroxymethyl-1-[[2'-(1H-tetrazol-5-yl)-biphenyl-4-yl]methyl]imidazole
BSPBio_002695
C07072
C22H23ClN6O
CHEBI:6541
Cozaar
DB00678
DUP 89
DuP-753
Hyzaar
KBio2_002193
KBio2_004761
KBio2_007329
KBio3_001915
KBioGR_001611
KBioSS_002193
Lortaan
Losartan
Losartan Monopotassium Salt
Losartan [INN:BAN]
LS-78746
Mixture Name
MK-954
MK954
NCGC00095125-01
NCGC00095125-02
NCGC00095125-03
Oprea1_644635
SPBio_001893
SPECTRUM1504268
Spectrum2_001677
Spectrum3_000998
Spectrum4_001126
Spectrum5_001466
Spectrum_001713
[2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol
ATC-Codes:
Side-Effects:
Side-EffectFrequency
cough0.21185417
urinary tract infection0.050666664
fatigue0.030750003
hypoglycemia0.030750003
back pain0.028250001
dizziness0.026666665
chest pain0.02575
infection0.0246
bronchitis0.024500001
vascular disease0.024500001
influenza0.024500001
diarrhea0.023545455
cellulitis0.022888891
asthenia0.022636365
anemia0.020299997
cataract0.015750002
hypotension0.013250001
sinusitis0.0126
knee pain0.012
leg pain0.012
gastritis0.012
muscular weakness0.010818183
pain0.01
weight gain0.009500001
fever0.0095
dyspepsia0.0095
diabetic neuropathy0.0095
hyperkalemia0.007928572
orthostatic hypotension0.0069999984
cramp0.0050
erythroderma0.0010
myositis0.0010
muscle pain0.0010
thrombocytopenia0.0010
hypertension0.0010
urticaria0.0010
nephropathy0.0010
vomiting0.0010
pruritus0.0010
eosinophilia0.0010
arthralgia0.0010
rhabdomyolysis0.0010
migraine0.0010
essential hypertension0.00092
hepatitis0.00092
anaphylactic reactions0.00092
angioedema0.00092
swelling0.00092
purpura0.00092
vasculitis0.00092
hypersensitivity0.0009
hyponatremia0.0009
tinnitus0
spasm0
pulmonary edema0
renal failure0
rhinitis0
shoulder pain0
tachycardia0
syncope0
sweating0
sialadenitis0
stevens - johnson syndrome0
toothache0
insomnia0
malaise0
memory impairment0
arm pain0
blurred vision0
photosensitivity0
neuropathy0
urinary frequency0
hyperuricemia0
joint swelling0
dry skin0
tremor0
erythema0
upper respiratory tract infection0
ventricular fibrillation0
agitation0
ventricular tachycardia0
vertigo0
dry mouth0
sinus bradycardia0
sleep disorder0
abdominal pain0
constipation0
decreased libido0
dermatitis0
somnolence0
dyspnea0
ecchymosis0
edema0
toxic epidermal necrolysis0
epistaxis0
erythema multiforme0
conjunctivitis0
confusion0
atrial fibrillation0
agranulocytosis0
alopecia0
aplastic anemia0
hemolytic anemia0
angina pectoris0
anorexia0
anxiety0
arrhythmia0
arthritis0
ataxia0
rash0
fibromyalgia syndrome0
flatulence0
interstitial nephritis0
nervousness0
nocturia0
palpitations0
pancreatitis0
panic disorder0
weakness0
paresthesia0
peripheral neuropathy0
pharyngitis0
nausea0
nasal congestion0
musculoskeletal pain0
flushing0
glycosuria0
gout0
headache0
hip pain0
hyperglycemia0
impotence0
jaundice0
leukopenia0
av block0
pneumonia0

Target

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Uniprot ID:CP2C9_HUMAN
Synonyms:
(R)-limonene 6-monooxygenase
(S)-limonene 6-monooxygenase
(S)-limonene 7-monooxygenase
CYPIIC9
Cytochrome P450 2C9
P-450MP
P450 MP-4/MP-8
P450 PB-1
S-mephenytoin 4-hydroxylase
EC-Numbers:1.14.13.48
1.14.13.49
1.14.13.80
Organism:Homo sapiens
Human
PDB IDs:1OG2 1OG5 1R9O
Structure:
1R9O

Binding Affinities:

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

References:

012743670
1
10877007
11408373
Role of CYP2C9 polymorphism in losartan oxidation.. Yasar U; G Tybring; M Hidestrand; M Oscarson; M Ingelman-Sundberg; M L Dahl; E Eliasson (2001) Drug metabolism and disposition: the biological fate of chemicals display abstract
Losartan, an angiotensin II receptor antagonist, is oxidized by hepatic cytochromes P450 to an active carboxylic acid metabolite, E-3174. The aim of the present investigation was to study the contribution of CYP2C9 and CYP3A4 in losartan oxidation in vitro and to evaluate the role of CYP2C9 polymorphism. Kinetic properties of different genetic CYP2C9 variants were compared both in a yeast expression system and in 25 different samples of human liver microsomes where all known genotypes of CYP2C9 were represented. Microsomes were incubated with losartan (0.05-50 microM), and the formation of E-3174 was analyzed by high-performance liquid chromatography to estimate V(max), K(m), and intrinsic clearance for all individual samples. Sulfaphenazole, a CYP2C9 inhibitor, blocked the formation of E-3174 at low losartan concentrations (25 microM). In comparison to the CYP2C9.1 variant, oxidation of losartan was significantly reduced in yeast expressing the rare CYP2C9.2 or CYP2C9.3 variants. Moreover, the rate of losartan oxidation was lower in liver microsomes from individuals hetero- or homozygous for the CYP2C9*3 allele, or homozygous for the CYP2C9*2 allele. The difference between the common and rare CYP2C9 variants was mainly explained by a lower V(max), both in yeast and human liver microsomes. In summary, these in vitro results indicate that CYP2C9 is the major human P450 isoenzyme responsible for losartan oxidation and that the CYP2C9 genotype contributes to interindividual differences in losartan oxidation and activation.
12235444
12359989
12520632
12820813
14600250
15197523
16029066