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Drug-Target Interaction

Drug

show drug details
PubChem ID:3948
Structure:
Synonyms:
(+)-1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
(+-)-1-Ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-
(+-)-1-Ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
1,4-Dihydro-6,8-difluoro-1-ethyl-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinol
1,4-Dihydro-6,8-difluoro-1-ethyl-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
1-Ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
1-ethyl-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
1-ethyl-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
114394-67-1 (MESYLATE)
3-Quinolinecarboxylic acid, 1,4-dihydro-6,8-difluoro-1-ethyl-7-(3-methyl-1-piperazinyl)-4-oxo-
3-Quinolinecarboxylic acid, 1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo- (+/-)
3-Quinolinecarboxylic acid, 1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-, (+-)-
3-Quinolinecarboxylic acid, 1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-, monohydrochloride
98079-51-7
98079-52-8
98079-52-8 (HYDROCHLORIDE)
AIDS-007749
AIDS007749
Bareon
BPBio1_000347
BRN 4210041
BSPBio_000315
BSPBio_003107
C07078
C17H19F2N3O3
CCRIS 6305
CHEBI:116278
D02318
DB00978
DivK1c_000365
DM 10 (bactericide)
DM-10
IDI1_000365
KBio1_000365
KBio2_001911
KBio2_004479
KBio2_007047
KBio3_002607
KBioGR_000636
KBioSS_001911
L2906_SIGMA
LFLX
Lomefloxacin
Lomefloxacin (USAN)
Lomefloxacin hydrochloride
Lomefloxacin [USAN:BAN:INN]
Lomefloxacine
Lomefloxacine [French]
Lomefloxacino
Lomefloxacino [Spanish]
Lomefloxacinum
Lomefloxacinum [Latin]
Lopac0_000678
LS-141570
Maxaquin
Maxaquin (hydrochloride)
NCGC00162221-01
NCGC00178293-01
NCGC00178293-02
NINDS_000365
NY 198
NY-198
NY-198 (hydrochloride)
Prestwick0_000238
Prestwick1_000238
Prestwick2_000238
Prestwick3_000238
SBB012581
SC 4711
SC 47111A
SC-4711
SC-47111 (hydrochloride)
SC-47111A
SC-47111B (mesylate)
SMP1_000287
SPBio_000851
SPBio_002236
Spectrum2_000696
Spectrum3_001494
Spectrum4_000158
Spectrum5_001246
Spectrum_001431
ST072201
TL8006033
ATC-Codes:
Side-Effects:
Side-EffectFrequency
phobia0.0010
polyuria0.0010
renal calculi0.0010
intestinal perforation0.0010
hyperpigmentation0.0010
hepatic necrosis0.0010
pulmonary edema0.0010
photophobia0.0010
stevens - johnson syndrome0.0010
exfoliative dermatitis0.0010
vasculitis0.0010
diplopia0.0010
urinary retention0.0010
cerebral thrombosis0.0010
renal failure0.0010
toxic epidermal necrolysis0.0010
hiccough0.0010
hepatitis0.0010
hallucinations0.0010
peripheral neuropathy0.0010
acidosis0.0010
agranulocytosis0.0010
albuminuria0.0010
anaphylaxis0.0010
pseudomembranous colitis0.0010
hemolytic anemia0.0010
dysphasia0.0010
tendinitis0.0010
interstitial nephritis0.0010
erythema nodosum0.0010
nystagmus0.0010
myasthenia gravis0.0010
ataxia0.0010
stridor0
rhinitis0
syncope0
tachycardia0
stomatitis0
skin ulcer0
purpura0
pulmonary embolism0
pruritus0
phlebitis0
pharyngitis0
paresthesia0
pain0
orchitis0
nightmares0
vertigo0
malaise0
myalgia0
thinking abnormal0
concentration impaired0
allergic reaction0
photosensitivity0
bradycardia0
lymphadenopathy0
manic0
increased sweating0
acne0
thrombocythemia0
eye pain0
macrocytosis0
thrombocytopenia0
tinnitus0
tremor0
urticaria0
vaginitis0
cardiomyopathy0
viral infection0
abnormal vision0
vomiting0
dry mouth0
chills0
agitation0
insomnia0
abdominal pain0
confusion0
conjunctivitis0
constipation0
convulsions0
cough0
dysphagia0
depersonalization0
diarrhea0
dizziness0
somnolence0
dyspepsia0
dyspnea0
coma0
chest pain0
cerebrovascular disorder0
anemia0
angina pectoris0
angioedema0
anorexia0
anxiety0
arrhythmia0
arthralgia0
asthenia0
back pain0
bronchospasm0
moniliasis0
vaginal moniliasis0
dysuria0
ear pain0
eczema0
hypertension0
hypoglycemia0
hypotension0
influenza0
leg cramps0
leukocytosis0
leukopenia0
menstrual disorder0
metrorrhagia0
fungal infection0
myocardial infarction0
nausea0
hyperglycemia0
hot flashes0
hematuria0
edema0
eosinophilia0
epididymitis0
epistaxis0
rash0
fatigue0
flatulence0
flushing0
gastrointestinal hemorrhage0
gout0
headache0
heart failure0
nervousness0

Target

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Uniprot ID:CP1A2_HUMAN
Synonyms:
CYPIA2
Cytochrome P450 1A2
P(3)450
P450 4
P450-P3
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2HI4
Structure:
2HI4

Binding Affinities:

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

References:

1510417
Inhibitory potency of quinolone antibacterial agents against cytochrome P450IA2 activity in vivo and in vitro.. U Fuhr; E M Anders; G Mahr; F Sörgel; A H Staib (1992) Antimicrobial agents and chemotherapy display abstract
Inhibition of cytochrome P450IA2 activity is an important adverse effect of quinolone antibacterial agents. It results in a prolonged half-life for some drugs that are coadministered with quinolones, such as theophylline. The objective of the study described here was to define the parameters for quantifying the inhibitory potencies of quinolones against cytochrome P450IA2 in vivo and in vitro and to investigate the relationship between the results of both approaches. Cytochrome P450IA2 activity in vitro was measured by using the 3-demethylation rate of caffeine (500 microM) in human liver microsomes. The inhibitory potency of a quinolone in vitro was determined by calculating the decrease in the activity of cytochrome P450IA2 caused by addition of the quinolone (500 microM) into the incubation medium. The mean values (percent reduction of activity without quinolone) were as follows: enoxacin, 74.9%; ciprofloxacin, 70.4%; nalidixic acid, 66.6%; pipemidic acid, 59.3%; norfloxacin, 55.7%; lomefloxacin, 23.4%; pefloxacin, 22.0%; amifloxacin, 21.4%; difloxacin, 21.3%; ofloxacin, 11.8%; temafloxacin, 10.0%; fleroxacin, no effect. The inhibitory potency of a quinolone in vivo was defined by a dose- and bioavailability-normalized parameter calculated from changes of the elimination half-life of theophylline and/or caffeine reported in previously published studies. Taking the pharmacokinetics of the quinolones into account, it was possible to differentiate between substances with and without clinically relevant inhibitory effects by using results of in vitro investigations. The in vitro test described here may help to qualitatively predict the relevant drug interactions between quinolones and methylxanthines that occur during therapy.