Home
Drugs
Targets
Pathways
Ontologies
Cyp450s
Adv.search
Help/FAQ

Drug-Target Interaction

Drug

show drug details
PubChem ID:60021
Structure:
Synonyms:
(1)-Temafloxacin
1-(2,4-Difluorophenyl)-6-fluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinoline-carboxylic acid
1-(2,4-difluorophenyl)-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
1-(2,4-difluorophenyl)-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
105784-61-0
105784-61-0 (MONOHYDROCHLORIDE)
108319-06-8
3-Quinolinecarboxylic acid,
3-Quinolinecarboxylic acid, 1,4-dihydro-1-(2,4-difluorophenyl)-6-fluoro-7- (3-methyl-1-piperazinyl)-4-oxo-
3-Quinolinecarboxylic acid, 1,4-dihydro-1-(2,4-difluorophenyl)-6-fluoro-7-(3-methyl-1-piperazinyl)-4-oxo-
3-Quinolinecarboxylic acid, 1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-
A 62254
A63004
Abbott 62254
AIDS-007773
AIDS007773
BRN 4301726
C21H18F3N3O3
CCRIS 6303
DB01405
LS-141579
LS-141580
Omniflox
T 1258
Temafloxacin
Temafloxacin hydrochloride
Temafloxacin [INN:BAN]
Temafloxacina
Temafloxacina [Spanish]
Temafloxacine
Temafloxacine [French]
Temafloxacinum
Temafloxacinum [Latin]
ATC-Codes:

Target

show target details
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.