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Drug-Target Interaction

Drug

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PubChem ID:124087
Structure:
Synonyms:
100643-71-8
5H-Benzo(5,6)cyclohepta(1,2-b)pyridine, 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-
5H-Benzo(5,6)cyclohepta(1,2-b)pyridine,8-chloro-6,11-dihydro-11-(4-piperidinyllidene)-
8-Chloro-11-piperidin-4-ylidene-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b
8-Chloro-11-piperidin-4-ylidene-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
8-Chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo(5,6)cyclohepta(1,2-b)pyridine
Aerius
Allex
Azomyr
C121345
CHEBI:291342
Clarinex
Clarinex (TN)
Clarinex RediTabs
CPD000149358
D03693
DB00967
DCL
Denosin
Desalex
Descarboethoxyloratadine
Descarboethoxyoratidine
Desloratadine
Desloratadine (USAN/INN)
Desloratadine [USAN]
Desloratidine
Essex brand of desloratadine
KS-1048
LS-181814
MLS000559042
MLS000759406
MLS001201801
NCGC00159325-02
NCGC00159325-03
NCGC00159325-04
Neoclarityn
NSC675447
Opulis
SAM001246545
Sch 34117
Sch-34117
Schering brand of desloratadine
Schering-Plough brand of desloratadine
SMR000149358
TL8000065
ATC-Codes:
Side-Effects:
Side-EffectFrequency
headache0.06
insomnia0.046666667
dry mouth0.04592307
pharyngitis0.029454546
somnolence0.021636363
nausea0.02
fatigue0.019999998
myalgia0.019714285
dysmenorrhea0.018857142
nervousness0.014999999
dizziness0.014999999
anorexia0.01
diarrhea0
bronchitis0
seizures0
palpitations0
vomiting0
anaphylaxis0
elevated liver enzymes0
upper respiratory tract infection0
viral infection0
varicella0
infection0
emotional lability0
dyspepsia0
tachycardia0
erythema0
rash0
agitation0
fever0
otitis media0
hypersensitivity0
epistaxis0
hepatitis0
urinary tract infection0
edema0
dyspnea0
rhinorrhea0
irritability0

Target

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Uniprot ID:CP2CJ_HUMAN
Synonyms:
(R)-limonene 6-monooxygenase
(S)-limonene 6-monooxygenase
(S)-limonene 7-monooxygenase
CYPIIC17
CYPIIC19
Cytochrome P450 2C19
Mephenytoin 4-hydroxylase
P450-11A
P450-254C
EC-Numbers:1.14.13.48
1.14.13.49
1.14.13.80
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

11502723
In vitro characterization of the inhibition profile of loratadine, desloratadine, and 3-OH-desloratadine for five human cytochrome P-450 enzymes.. M E Barecki; C N Casciano; W W Johnson; R P Clement (2001) Drug metabolism and disposition: the biological fate of chemicals display abstract
The purpose of this study was to evaluate loratadine, desloratadine, and 3-OH-desloratadine as inhibitors of certain human liver cytochrome P-450 enzymes. Pooled human liver microsomes were used to determine whether loratadine, desloratadine, and 3-OH-desloratadine were inhibitors of cytochrome P-450 (CYP) 1A2, 2C9, 2C19, 2D6, and 3A4. Loratadine did not inhibit CYP1A2 or CYP3A4 at concentrations up to 3829 ng/ml, which is approximately 815-fold greater than the expected maximal human plasma concentration (4.7 +/- 2.7 ng/ml) following the recommended dose of 10 mg/day. Loratadine inhibited CYP2C19 and CYP2D6 with IC(50) values of approximately 0.76 microM [291 ng/ml; K(i) congruent with 0.61 microM (234 ng/ml)] and 8.1 microM [3100 ng/ml; K(i) congruent with 2.7 microM (1034 ng/ml)], respectively, which are approximately 62 and 660 times the expected loratadine therapeutic exposure concentration. Neither desloratadine nor 3-OH-desloratadine inhibited CYP1A2, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 greater than 25% at concentrations of 3108 or 3278 ng/ml, respectively. These results suggest that loratadine and the active metabolites desloratadine and 3-OH-desloratadine are unlikely to affect the pharmacokinetics of coadministered drugs which are metabolized by these five cytochrome P-450 enzymes.