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Drug-Target Interaction

Drug

show drug details
PubChem ID:4943
Structure:
Synonyms:
2, 6-Diisopropylphenol
2,6 Diisopropylphenol
2,6-bis(1-methylethyl)-phenol
2,6-Bis(1-methylethyl)phenol
2,6-Bis(Isopropyl)-phenol
2,6-bis(propan-2-yl)phenol
2,6-di(propan-2-yl)phenol
2,6-Diisopropyl phenol
2,6-Diisopropylphenol
2078-54-8
28449-97-0
4-06-00-03435 (Beilstein Handbook Reference)
50356-15-5
AB00513968
Abbott Brand of Propofol
AC-2038
AC1L1J9Y
AC1Q1OUI
AI3-26295
AIDS-123996
AIDS123996
Alpha Brand of Propofol
AM-149
Ampofol
Aquafol
Astra Brand of Propofol
AstraZeneca Brand of Propofol
BIDD:GT0436
Biomol-NT_000248
BPBio1_000950
BPBio1_000969
Braun Brand of Propofol
BRD-K82255054-001-03-5
BRN 1866484
BSPBio_000862
C07523
C12H18O
CAS-2078-54-8
CCG-204529
CCRIS 9000
CHEBI:44915
CHEMBL526
CPD-11437
CPD000059151
Curamed Brand of Propofol
D00549
D015742
D0617
D126608
D126608_ALDRICH
DB00818
DDS-04F
Diisopropylphenol
Dipravan
Diprivan
Diprivan (TN)
Diprivan Injectable emulsion
Disoprivan
Disoprofol
EINECS 218-206-6
EU-0100437
Fresenius Brand of Propofol
Fresenius Kabi Brand of Propofol
Fresofol
ghl.PD_Mitscher_leg0.558
HMS1570L04
HMS2089O21
HMS2094E17
HMS2097L04
HMS2231E16
HMS3259E03
HMS3261G16
HSDB 7123
ICI 35,868
ICI 35868
ICI-35,868
ICI-35868
ICI35,868
ICI35868
Ivofol
Jsp004266
Juste Brand of Propofol
Lopac-D126608
Lopac0_000437
LS-996
MLS001066348
MLS001335999
MLS002454360
NCGC00015389-01
NCGC00015389-02
NCGC00015389-03
NCGC00015389-04
NCGC00015389-05
NCGC00015389-06
NCGC00015389-07
NCGC00015389-08
NCGC00015389-09
NCGC00015389-10
NCGC00015389-11
NCGC00091538-01
NCGC00091538-02
NCGC00091538-03
NCGC00091538-04
NCGC00091538-05
NCGC00091538-06
nchembio.552-comp7
NSC 5105
NSC5105
Parnell Brand of Propofol
PFL
Phenol, 2, 6-bis(1-methylethyl)-
Phenol, 2,6-bis(1-methylethyl)-
Phenol, 2,6-diisopropyl-
Pisa Brand of Propofol
Prestwick0_000931
Prestwick1_000931
Prestwick2_000931
Prestwick3_000931
Propofol
Propofol (JAN/USAN/INN)
Propofol Abbott
Propofol Fresenius
Propofol IDD-D
Propofol MCT
Propofol Rovi
Propofol [USAN:BAN:INN]
Propofol [USAN:INN:BAN]
Propofol(2,6-Diisopropylphenol)
Propofol-Lipuro
propofolum
Propofolum [Latin]
Rapinovet
Recofol
Rovi Brand of Propofol
S01-0189
SAM002264610
Schering Brand of Propofol
SMR000059151
SPBio_003031
SPECTRUM1505022
ST50405911
ST5405911
UNII-YI7VU623SF
W505102_ALDRICH
ZD-0859
Zeneca Brand of Propofol
ZINC00968303
ATC-Codes:
Side-Effects:
Side-EffectFrequency
vision abnormal0.0010
cardiovascular collapse0.0010
supraventricular tachycardia0.0010
apnea0.0010
drug abuse0.0010
tachycardia nodal0.0010
hypomagnesemia0.0010
anaphylaxis0.0010
metabolic acidosis0.0010
hypertension0.00075
hypersalivation0.00066
sneezing0.00066
leukocytosis0.00066
syncope0.00066
urine retention0.00066
seizures0.00066
pruritus0.00066
premature atrial contractions0.00066
myocardial infarction0.00066
nystagmus0.00066
pain0.00066
insomnia0.00066
weakness0.00066
paresthesia0.00066
pharyngitis0.00066
phlebitis0.00066
tinnitus0.00066
tremor0.00066
ecg abnormal0.00066
neuropathy0.00066
bradycardia0.00066
hypoventilation0.00066
bigeminy0.00066
sepsis0.00066
right heart failure0.00066
myalgia0.00066
eye pain0.00066
myocardial ischemia0.00066
premature ventricular contractions0.00066
neck rigidity0.00066
chills0.00066
dry mouth0.00066
wheezing0.00066
ventricular fibrillation0.00066
hives0.00066
diaphoresis0.00066
hallucinations0.00066
asthenia0.00066
bronchospasm0.00066
flushing0.00066
bundle branch block0.00066
fever0.00066
fatigue0.00066
cough0.00066
chest pain0.00066
ear pain0.00066
dehydration0.00066
delirium0.00066
diarrhea0.00066
coagulation disorder0.00066
atrioventricular heart block0.00066
diplopia0.00066
acidosis0.00066
amblyopia0.00066
anxiety0.00066
hyperkalemia0.00066
hyperglycemia0.00066
hiccough0.00066
somnolence0.00066
hemorrhage0.00066
atrial fibrillation0.00066
cardiac arrest0.00066
arrhythmia0.00066
vomiting0.0005
rash0.0005
agitation0.0005
confusion0.0005
hypoxia0.0005
dizziness0.0005
tachycardia0.0005
kidney failure0.0005
nausea0.0005
hyperlipemia0.0005
headache0.0005
dyspnea0.0005
hypotension0.0005
ventricular tachycardia0.0005
rhabdomyolysis0.0005
pneumothorax0.0
heart block0.0
heart failure0.0
anemia0.0
hypokalemia0.0
pancreatitis0.0
respiratory arrest0.0
extremity pain0.0
hepatomegaly0.0
edema0.0
erythema0
emotional lability0
angioedema0
convulsions0
euphoria0
pulmonary edema0
thinking abnormal0

Target

show target details
Uniprot ID:CP1A1_HUMAN
Synonyms:
CYPIA1
Cytochrome P450 1A1
P450 form 6
P450-C
P450-P1
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

7772432
Human cytochrome P450 mono-oxygenase system is suppressed by propofol.. T L Chen; T H Ueng; S H Chen; P H Lee; S Z Fan; C C Liu (1995) British journal of anaesthesia display abstract
We have studied the effect of propofol on the cytochrome P450-dependent mono-oxygenase system in human liver microsomes by assaying mono-oxygenase activities toward specific cytochrome P450 isoform test substrates, aniline, 7-ethoxycoumarin, benzphetamine and benzo(a) pyrene. Propofol inhibited benzo(a)pyrene hydroxylation to a greater extent than the oxidative metabolism of the other test substrates, even at 0.05 mmol litre-1. The degrees of inhibition of benzphetamine N-demethylation and 7-ethoxy-coumarin O-de-ethylation were similar, while aniline hydroxylation was least affected by propofol. Spectral analysis showed that propofol competed with carbon monoxide for binding to the haem moiety of haemoprotein in the P450 enzyme. The variable inhibition observed may be caused by the differential binding of propofol to P450 isoforms. Propofol 0.05-1.0 mmol litre-1 exhibited a concentration-dependent inhibitory effect on human cytochrome P450 2E1, 2B1 and 1A1. These inhibitory actions of propofol on human liver microsomal enzymes in vitro suggest that potential drug interactions may exist between propofol and other drugs administered clinically.
9764927
Effects of propofol on human hepatic microsomal cytochrome P450 activities.. D McKillop; M J Wild; C J Butters; C Simcock (1998) Xenobiotica; the fate of foreign compounds in biological systems display abstract
1. The potential of propofol to inhibit the activity of major human cytochrome P450 enzymes has been examined in vitro using human liver microsomes. Propofol produced inhibition of CYP1A2 (phenacetin O-deethylation), CYP2C9 (tolbutamide 4'-hydroxylation), CYP2D6 (dextromethorphan O-demethylation) and CYP3A4 (testosterone 6beta-hydroxylation) activities with IC50 = 40, 49, 213 and 32 microM respectively. Ki for propofol against all of these enzymes with the exception of CYP2D6, where propofol showed little inhibitory activity, was 30, 30 and 19 microM respectively for CYPs 1A2, 2C9 and 3A4. 2. Furafylline, sulphaphenazole, quinidine and ketoconazole, known selective inhibitors of CYPs 1A2, 2C9, 2D6 and 3A4 respectively, were much more potent than propofol having IC50 = 0.8, 0.5, 0.2 and 0.1 microM; furafylline and sulphaphenazole yielded Ki = 0.6 and 0.7 microM respectively. 3. The therapeutic blood concentration of propofol (20 microM; 3-4 microg/ml) together with the in vitro Ki estimates for each of the major human P450 enzymes have been used to estimate the extent of cytochrome P450 inhibition, which may be produced in vivo by propofol. This in vitro-in vivo extrapolation indicates that the degree of inhibition of CYP1A2, 2C9 and 3A4 activity which could theoretically be produced in vivo by propofol is relatively low (40-51%); this is considered unlikely to have any pronounced clinical significance. 4. Although propofol has now been used in > 190 million people since its launch in 1986, there are only single reports of possible drug interactions between propofol and either alfentanil or warfarin. Consequently, it is difficult to conclude from either the published literature or the ZENECA safety database whether there is any evidence to indicate that propofol produces clinically significant drug interactions through inhibition of cytochrome P450-related drug metabolism.