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Drug-Target Interaction

Drug

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PubChem ID:5212
Structure:
Synonyms:
1-((3-(4,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo(4,3-d)pyrimidin-5-y
1-((3-(4,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo(4,3-d)pyrimidin-5-yl)-4-ethoxyphenyl)sulfonyl)-4-methylpiperazine
1-((3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo(4,3-d)pyrimidin-5-yl)-4-ethoxyphenyl)sulfonyl)-4-methylpiperazine citrate
139755-83-2
171599-83-0
1udt
1xos
2h42
5-[2-ethoxy-5-(4-methylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-4H-pyrazolo[5,4-e]pyrimidin-7-one
5-{2-(ethyloxy)-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl}-1-methyl-3-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
Ambap1012
BAS 04213629
BSPBio_003424
C07259
C22H30N6O4S
CHEBI:9139
DB00203
DivK1c_006894
HSDB 7305
KBio1_001838
KBio2_002035
KBio2_004603
KBio2_007171
KBio3_002927
KBioGR_001052
KBioSS_002035
KS-1112
LS-111655
MLS001240224
MLS001304737
NCGC00095099-01
NCGC00095099-02
NCGC00159496-02
Piperazine, 1-((3-(4,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo(4,3-d)pyrimidin-5-yl)-4-ethoxyphenyl)sulfonyl)-4-methyl-
Sildenafil
SILDENAFIL CITRATE
Sildenafil [INN:BAN]
SMR000752512
SPBio_001775
SpecPlus_000798
SPECTRUM1504099
Spectrum2_001648
Spectrum3_001892
Spectrum4_000586
Spectrum5_001508
Spectrum_001555
UK 92480-10
UK-92,480-10
VIA
VIAGRA
ATC-Codes:
Side-Effects:
Side-EffectFrequency
headache0.11199999
flushing0.064
dyspepsia0.05
nasal congestion0.031999998
blurred vision0.03
urinary tract infection0.025999999
diarrhea0.022
dizziness0.015999999
rash0.015999999
abnormal vision0.011363637
coronary artery disease0.0010
swelling0.0010
hematuria0.0010
diabetes0.0010
vascular disease0.0010
hemorrhage0.0010
diplopia0.0010
hypertension0.0010
vitreous detachment0.0010
vomiting0.0010
hyperlipidemia0.0010
epistaxis0.0010
edema0.0010
neuropathy0.0010
loss of vision0.0010
arrhythmia0.0010
myocardial infarction0.0010
intracerebral hemorrhages0.0010
anxiety0.0010
priapism0.0010
transient ischemic attack0.0010
seizure0.0010
hearing loss0.0010
erythema0
upper respiratory tract infection0
sexual dysfunction0
paresthesia0
urticaria0
urinary incontinence0
pharyngitis0
syncope0
renal failure0
tremor0
skin ulcer0
shock0
stomatitis0
sweating0
synovitis0
tachycardia0
tenosynovitis0
pruritus0
shoulder pain0
rhinitis0
tinnitus0
retinal hemorrhage0
tooth disorder0
sinusitis0
varicose vein0
vertigo0
myalgia0
hypoxia0
global amnesia0
rectal hemorrhage0
dry eyes0
transient global amnesia0
photosensitivity0
ecg abnormal0
urinary frequency0
lung cancer0
skin carcinoma0
acne0
hyperuricemia0
cardiomyopathy0
insomnia0
malaise0
vascular anomaly0
weight gain0
dry mouth0
cerebral thrombosis0
chills0
agitation0
photophobia0
peripheral edema0
cataract0
lower respiratory infection0
mouth ulceration0
migraine0
myocardial ischemia0
liver function tests abnormal0
bone pain0
eye pain0
allergic reaction0
abdominal pain0
cough0
cystitis0
deafness0
dysphagia0
dermatitis0
exfoliative dermatitis0
contact dermatitis0
somnolence0
dyspnea0
ear pain0
abdominal distention0
endocrine disorders0
eructation0
esophagitis0
fever0
constipation0
conjunctivitis0
colitis0
anemia0
angina pectoris0
anorexia0
arthralgia0
arthritis0
asthenia0
asthma0
ataxia0
av block0
back pain0
balanitis0
bronchitis0
cellulitis0
cerebrovascular disorder0
chest pain0
flatulence0
furunculosis0
gastritis0
postural hypotension0
infection0
influenza0
arthrosis0
lacrimation disorder0
laryngitis0
leukopenia0
mediastinal disorders0
nail disorder0
nausea0
nervousness0
neuralgia0
nocturia0
pain0
pain in limb0
hypotension0
hypokalemia0
breast enlargement0
gastroenteritis0
gastroesophageal reflux0
gingivitis0
glossitis0
gout0
cardiac arrest0
heart disease0
heart failure0
hemoptysis0
hernia0
herpes simplex0
hyperesthesia0
hyperglycemia0
hypernatremia0
hyperthyroidism0
palpitations0

Target

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Uniprot ID:CP2CB_RAT
Synonyms:
CYPIIC11
Cytochrome P450 2C11
P-450(M-1)
P450-UT-A
P450H
UT-2
EC-Numbers:1.14.14.1
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

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

References:

12019191
In vitro biotransformation of sildenafil (Viagra) in the male rat: the role of CYP2C11.. Jill S Warrington; Lisa L Von Moltke; Richard I Shader; David J Greenblatt (2002) Drug metabolism and disposition: the biological fate of chemicals display abstract
To assess the suitability of the male rat model for human studies on sildenafil metabolism, we examined the biotransformation of sildenafil in male rat liver microsomes and identified the role of specific cytochrome P450s (P450) using inhibitory antibodies and cDNA-expressed P450s. Rates of formation of the major circulating metabolite of sildenafil, UK-103,320, were 11-fold greater in the male rat than in human liver microsomes at 36 microM sildenafil, whereas substrate concentration corresponding to 50% V(max) (K(m) values) were 2.9-fold lower in the male rat. Although sildenafil is largely metabolized by CYP3A isoforms in humans, coincubation of rat liver microsomes with immunoinhibitory antibodies (CYP1A1/2, 2B1/2, 2C11, 2E1, and 3A1/2) revealed that metabolite formation was inhibited only by an antirat CYP2C11 antibody. Incubation of sildenafil with a cDNA-expressed CYP2C11 produced 10-fold higher levels of UK-103,320 than other P450s (CYP1A1, 1A2, 2B1, 2C6, 2C12, 2C13, 2E1, 3A1, and 3A2). Thus CYP2C11 contributes in a major way to the metabolism of sildenafil in the male rat. P450 isoforms mediating sildenafil biotransformation differ substantially between humans and the male rat, thereby limiting the applicability of this species as a model for sildenafil metabolism and drug interactions in humans.