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

Drug-Target Interaction

Drug

show drug details
PubChem ID:3559
Structure:
Synonyms:
.gamma.-[4-(p-Chlorphenyl)-4-hydroxpiperidino]-p-fluorbutyrophenone
1-(3-p-Fluorobenzoylpropyl)-4-p-chlorophenyl-4-hydroxypiperidine
1-Butanone, 4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-
1-Butanone, 4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-
4'-Fluoro-4-(4-(p-chlorophenyl)-4-hydroxypiperidinyl)butyrophenone
4'-Fluoro-4-(4-hydroxy-4-(4'-chlorophenyl)piperidino)butyrophenone
4'-Fluoro-4-(4-hydroxy-4-p-chlorophenylpiperidino)butyrophenone
4'-Fluoro-4-[4-hydroxy-4-(4'-chlorophenyl)piperidino]butyrophenone
4-(4-(4-Chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butanone
4-(4-(p-Chlorophenyl)-4-hydroxypiperidino)-4'-fluorobutyrophenone
4-(4-(para-chlorophenyl)-4-hydroxypiperidino)-4'-fluorobutyrophenone
4-(4-Hydroxy-4'-chloro-4-phenylpiperidino)-4'-fluorobutyrophenone
4-[4-(4-Chlorophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-1-(4-fluorophenyl)-butan-1-one
4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-o
4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
4-[4-(4-Chlorophenyl)-4-hydroxypiperidino]-4'-fluorobutyrophenone
4-[4-(p-Chlorophenyl)-4-hydroxypiperidino]-4'-fluorobutyrophenone
4-[4-(para-Chlorophenyl)-4-hydroxypiperidino]-4'-fluorobutyrophenone
5-21-02-00377 (Beilstein Handbook Reference)
52-86-8
AB00052008
AIDS-001623
AIDS001623
Aldo
Aloperidin
Aloperidol
Aloperidolo
Aloperidolo [DCIT]
Aloperidolo [Italian]
Aloperidon
Biomol-NT_000035
BPBio1_000144
BPBio1_001231
BRN 0331267
Brotopon
BSPBio_000130
BSPBio_002096
Butyrophenone, 4'-fluoro-4-(4-(p-chlorophenyl)-4-hydroxypiperidino)-
Butyrophenone, 4-(4-(p-chlorophenyl)-4-hydroxypiperidino)-4'-fluoro-
Butyrophenone, 4-[4-(p-chlorophenyl)-4-hydroxypiperidino]-4'-fluoro-
C01814
C21H23ClFNO2
CAS-52-86-8
CCRIS 1630
CHEBI:5613
CID3559
cMAP_000037
D00136
D006220
DB00502
DivK1c_000654
Dozic
Einalon S
EINECS 200-155-6
EU-0100583
Eukystol
Fortunan
Galoperidol
gamma-(4-(p-chlorophenyl)-4-hydroxpiperidino)-p-fluorbutyrophenone
gamma-(4-(p-Chlorophenyl)-4-hydroxypiperidino)-p-fluorbutyrophenone
gamma-(4-(p-Chlorophenyl)-4-hydroxypiperidino)-p-fluorobutyrophenone
H1512_SIGMA
Haldol
Haldol (TN)
HALDOL SOLUTAB
Halojust
Halol
Halopal
Haloperidol
Haloperidol (JP15/USP/INN)
Haloperidol [USAN:BAN:INN:JAN]
Haloperidol [USAN:INN:BAN:JAN]
Haloperidolum
Haloperidolum [INN-Latin]
Halopoidol
HSDB 3093
IDI1_000654
IN1474
KBio1_000654
KBio2_001341
KBio2_002390
KBio2_003909
KBio2_004958
KBio2_006477
KBio2_007526
KBio3_001316
KBio3_002869
KBioGR_000980
KBioGR_002390
KBioSS_001341
KBioSS_002395
Keselan
Lealgin compositum
Linton
Lopac-H-1512
Lopac0_000583
LS-48311
McN-JR-1625
Mixidol
MLS000028450
MLS001146904
NCGC00015500-01
NCGC00015500-02
NCGC00016234-01
NCGC00023875-02
NCGC00023875-04
NCGC00023875-05
NCGC00023875-06
NCGC00023875-07
NCGC00023875-08
NCGC00023875-09
NINDS_000654
NSC 170973
NSC 615296
NSC170973
NSC615296
Oprea1_509923
Peluces
Pernox
Prestwick0_000115
Prestwick1_000115
Prestwick2_000115
Prestwick3_000115
Prestwick_250
Probes1_000255
Probes2_000296
QTL1_000042
R 1625
R-1625
Serenace
Serenase
Serenelfi
Sernas
Sernel
SMR000058303
SPBio_001236
SPBio_002069
SPECTRUM1500325
Spectrum2_001268
Spectrum3_000448
Spectrum4_000570
Spectrum5_000788
Spectrum_000861
ST5319916
Tocris-0931
Ulcolind
Uliolind
Vesalium
WLN: T6NTJ A3VR DF& DQ DR DG
ATC-Codes:
Side-Effects:
Side-EffectFrequency
insomnia0
cerebrovascular accident0
spasm0
increased salivation0
seizures0
retinopathy0
priapism0
nausea0
breast pain0
leukopenia0
leukocytosis0
jaundice0
tachycardia0
vertigo0
increased sweating0
tardive dyskinesia0
photosensitivity0
blurred vision0
parkinson0
drug withdrawal0
cataract0
agitation0
urinary retention0
dry mouth0
vomiting0
impotence0
hypotension0
somnolence0
diarrhea0
dysphagia0
constipation0
confusion0
bronchospasm0
arrhythmia0
anxiety0
anorexia0
anemia0
alopecia0
dyskinesia0
dyspepsia0
hyponatremia0
hypoglycemia0
hypertension0
hyperglycemia0
headache0
hallucinations0
gynecomastia0
euphoria0
grand mal0
endocrine disorders0
dyspnea0
agranulocytosis0

Target

show target details
Uniprot ID:CP2D6_HUMAN
Synonyms:
CYPIID6
Cytochrome P450 2D6
Debrisoquine 4-hydroxylase
P450-DB1
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2F9Q
Structure:
2F9Q

Binding Affinities:

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

References:

10460810
10688273
11717183
1412613
15048614
9681669
Involvement of human cytochrome P450 3A4 in reduced haloperidol oxidation.. S Kudo; M Odomi (1998) European journal of clinical pharmacology display abstract
OBJECTIVE: The present study was conducted to identify in vitro the cytochrome P450(CYP) isoform involved in the metabolic conversion of reduced haloperidol to haloperidol using microsomes derived from human AHH-1 TK +/- cells expressing human cytochrome P450s. The inhibitory and/or stimulatory effects of reduced haloperidol or haloperidol on CYP2D6-catalyzed carteolol 8-hydroxylase activity were also investigated. RESULTS: The CYP isoform involved in the oxidation of reduced haloperidol to haloperidol was CYP3A4. CYP1A1, 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, and 2E1 were not involved in the oxidation. The kM value for the CYP3A4 expressed in the cells was 69.7 micromol x l(-1), and the Vmax was 4.87 pmol x min(-1) x pmol(-1) P450. Troleandomycin, a relatively selective probe for CYP3A enzymes, inhibited the CYP3A4-mediated oxidation of reduced haloperidol in a dose-dependent manner. Quinidine and sparteine competitively inhibited the oxidative reaction with a k(i) value of 24.9 and 1390 micromol x l(-1), respectively. Carteolol 8-hydroxylase activity, which is a selective reaction probe for CYP2D6 activity, was inhibited by reduced haloperidol with a k(i) value of 4.3 micromol x l(-1). Haloperidol stimulated the CYP2D6-mediated carteolol 8-hydroxylase activity with an optimum concentration of 1 micromol x l(-1), whereas higher concentrations of the compound (> 10 micromol x l(-1)) inhibited the hydroxylase activity. CONCLUSION: It was concluded that CYP3A4, not CYP2D6, is the principal isoform of cytochrome P450 involved in the metabolic conversion of reduced haloperidol to haloperidol. It was further found that reduced haloperidol is a substrate of CYP3A4 and an inhibitor of CYP2D6, and that haloperidol has both stimulatory and inhibitory effects on CYP2D6 activity.