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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:CP3A4_HUMAN
Synonyms:
Albendazole monooxygenase
Albendazole sulfoxidase
CYPIIIA3
CYPIIIA4
Cytochrome P450 3A3
Cytochrome P450 3A4
HLp
NF-25
Nifedipine oxidase
P450-PCN1
Quinine 3-monooxygenase
Taurochenodeoxycholate 6-alpha-hydroxylase
EC-Numbers:1.14.13.32
1.14.13.67
1.14.13.97
Organism:Homo sapiens
Human
PDB IDs:1TQN 1W0E 1W0F 1W0G 2J0D 2V0M
Structure:
2V0M

Binding Affinities:

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

References:

10546851
11298070
12058245
12497749
Interaction between sildenafil and calcineurin inhibitors in renal transplant recipients with erectile dysfunction. F Cofán; R Gutiérrez; P Beardo; J M Campistol; F Oppenheimer; J Alcover (2002) Nefrología : publicación oficial de la Sociedad Española Nefrologia display abstract
AIM: Hepatic metabolism of sildenafil uses the same metabolic pathway as the calcineurin inhibitors (cyclosporine/tacrolimus), through the CYP3A4 isoenzyme. The aim of this pilot study was to evaluate the potential interaction between sildenafil therapy and circulating levels of cyclosporine and tacrolimus in a group of steady-state renal transplant recipients with erectile dysfunction. MATERIAL AND METHODS: A prospective pilot study of sildenafil interactions was carried out in 9 stable male renal transplant recipients with severe erectile dysfunction (mean age 50 +/- 8 years, range 38-64). All patients were receiving therapy with calcineurin inhibitors (5 with cyclosporine and 4 with tacrolimus). Erectile dysfunction was evaluated by clinical history, physical examination, International Index of Erectile Function (IIEF) questionnaire and the nocturnal penile tumescence test (RigiScan). Each patient received a first dose of 50 mg of sildenafil, one hour before sexual activity and a second dose at 72 hours of 50 or 100 mg according to the clinical response to the first dose. We evaluated the efficacy and safety of sildenafil and the evolution of cyclosporine-tacrolimus levels. Cyclosporine and tacrolimus trough whole blood concentrations were determined in basal conditions (before starting sildenafil) and on days 1, 4 and 7 after sildenafil therapy. RESULTS: Eighty-nine percent of patients (n = 8) required a complete 100 mg dose of sildenafil. There was a positive clinical response in two-thirds of cases (6 patients). In 5 patients (55%) sildenafil administration produced a complete response, in one patient the response was incomplete, and in the remaining 3 cases (33%) no clinical response was observed. Associated side effects included self-limited tachycardia in one patient and mild visual disturbances in another. Cyclosporine and tacrolimus levels remained stable in all patients. There were no significant differences in circulating levels of cyclosporine (basal 120 +/- 47; day 1: 116 +/- 55; day 4: 123 +/- 56 and day 7: 121 +/- 56 ng/ml p = NS) or tacrolimus (basal 11.6 +/- 1.3; day 1: 11.9 +/- 1.3; day 4: 11.1 +/- 1.0 and day 7: 11.8 +/- 0.9 ng/ml p = NS) over the study period. CONCLUSIONS: Sildenafil therapy is safe and effective for the treatment of erectile dysfunction in renal transplant recipients. Recommended therapeutic doses of sildenafil did not modify cyclosporine and tacrolimus trough blood levels.
9916601