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Drug-Target Interaction

Drug

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PubChem ID:3957
Structure:
Synonyms:
1-Piperidenecarboxylic acid, 4-(8-chloro-5,6-duhydro-11H-benzo [5,6]cyclohepta[1,2-b]-pyridin-11-ylidene)-, ethyl ester
1-Piperidinecarboxylic acid,
1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-, ethyl ester
1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-, ethyl ester
1-piperidinecarboxylic acid,4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-,ethyl ester
4-(8-Chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-1-piperidinecarboxylic Acid Ethyl Ester
4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester
4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene-1-piperidinecarboxylic acid ethyl ester
79794-75-5
Aerotina
Alarin
Alavert
Alerpriv
Allertidin
Anhissen
Bedix Loratadina
Biloina
Bonalerg
BSPBio_002300
C22H23ClN2O2
Children's Claritin
Civeran
Claratyne
Claratyne Cold
Claratyne Decongestant
Clarinase
Clarinase Reperabs
Claritin
Claritin (TN)
Claritin D
Claritin reditab
CLARITIN REDITABS
CLARITIN-D
CLARITIN-D 24 HOUR
Claritine
Clarityn
Clarityne
Clarityne Dy Repetabs
Clarityne-D
Clarium
CPD000058255
D00364
D017336
DB00455
DivK1c_000792
Ethyl 4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-ylidene)-1-piperidinecarboxylate
ethyl 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidine-1-carboxylate
EU-0100680
Fristamin
Histaloran
HSDB 3578
IDI1_000792
KBio1_000792
KBio2_001976
KBio2_004544
KBio2_007112
KBio3_001520
KBioGR_000693
KBioSS_001976
KS-1079
L9664_SIGMA
Lergy
Lertamine
Lesidas
Lisino
Lopac-L-9664
Lopac0_000680
Loracert
Loradex
Loradif
Loranox
Lorantis
Lorastine
Loratadina [Spanish]
LORATADINE
Loratadine (JAN/USAN/INN)
Loratadine Wyeth Brand
Loratadine [USAN:BAN:INN]
Loratadinum [Latin]
Loratidine
Loratyne
Loraver
Lorfast
Loritine
Lowadina
LS-114660
Mixture Name
MLS000069647
MLS000758260
MLS001148466
NCGC00015619-01
NCGC00015619-02
NCGC00023125-02
NCGC00023125-04
NCGC00023125-05
NCGC00023125-06
NCGC00023125-07
NCI60_041473
NINDS_000792
NSC721075
Nularef
Oprea1_027965
Optimin
Polaratyne
Pylor
Restamine
Rhinase
Rinomex
SAM001246987
Sanelor
Sch 29851
Sch-29851
Sch29851
Sensibit
Sinhistan Dy
SMR000058255
Sohotin
SPBio_001548
SPECTRUM1503712
Spectrum2_001584
Spectrum3_000740
Spectrum4_000177
Spectrum5_001650
Spectrum_001496
Tadine
Talorat Dy
TL8005389
Tocris-1944
Velodan
Versal
Wyeth Brand of Loratadine
Zeos
ZINC00537931
ATC-Codes:
Side-Effects:
Side-EffectFrequency
dry mouth0.068333335
headache0.06
insomnia0.05
somnolence0.04
pharyngitis0.035
fatigue0.027142854
dizziness0.024999999
nausea0.024999999
nervousness0.023333333
coughing0.02
dysmenorrhea0.015
anorexia0.014999998
palpitations0.0010
alopecia0.0010
tachycardia0.0010
anaphylaxis0.0010
vomiting0
rash0
dyspepsia0
diarrhea0
gastritis0
abdominal pain0

Target

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Uniprot ID:Q38LG2_HUMAN
Synonyms:
Cytochrome P450 2D6
EC-Numbers:1.14.14.1
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.