Identification

Name
Rupatadine
Accession Number
DB11614
Type
Small Molecule
Groups
Approved
Description

Rupatadine is a dual histamine H1 receptor and platelet activating factor receptor antagonist that is used for symptomatic relief in seasonal and perennial rhinitis as well as chronic spontaneous urticaria. It was approved for marketing in Canada under the tradename Rupall and comes in tablet formulation for adult use and liquid formulation for pediatric use.

Structure
Thumb
Synonyms
Not Available
External IDs
UR-12592
Product Ingredients
IngredientUNIICASInChI Key
Rupatadine fumarateXJ6OT32M93182349-12-8JYBLCDXVHQWMSU-WLHGVMLRSA-N
Rupatadine trihydrochlorideG61C8NZY2T156611-76-6BQFOTHHRVVHLEW-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RupallTablet10 mgOralPediapharm Inc2017-01-16Not applicableCanada
RupallSolution1 mgOralPediapharm Inc2017-01-20Not applicableCanada
Categories
UNII
2AE8M83G3E
CAS number
158876-82-5
Weight
Average: 415.97
Monoisotopic: 415.1815255
Chemical Formula
C26H26ClN3
InChI Key
WUZYKBABMWJHDL-UHFFFAOYSA-N
InChI
InChI=1S/C26H26ClN3/c1-18-13-19(16-28-15-18)17-30-11-8-20(9-12-30)25-24-7-6-23(27)14-22(24)5-4-21-3-2-10-29-26(21)25/h2-3,6-7,10,13-16H,4-5,8-9,11-12,17H2,1H3
IUPAC Name
13-chloro-2-{1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene}-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3(8),4,6,11,13-hexaene
SMILES
CC1=CC(CN2CCC(CC2)=C2C3=CC=C(Cl)C=C3CCC3=C2N=CC=C3)=CN=C1

Pharmacology

Indication

For the symptomatic relief of nasal and non-nasal symptoms of seasonal allergic rhinitis and perennial allergic rhinitis in patients 2 years of age and older [FDA Label]. Also used for the symptomatic relief of chronic spontaneous urticaria in patients 2 years of age and older.

Structured Indications
Pharmacodynamics

Rupatadine is an anti allergenic and acts to reduce allergic symptoms like urticaria, rhinorrhea, sneezing and itching [FDA Label].

Mechanism of action

Rupatadine is a dual histamine H1 receptor and platelet activating (PAF) receptor antagonist [1] [FDA Label]. During allergic response mast cells undergo degranulation, releasing histamine and other substances [2]. Histamine acts on H1 receptors to produce symptoms of nasal blockage, rhinorhea, itching, and swelling. PAF is produced from phospholipids cleaved by phospholipase A2. It acts to produce vascular leakage which contributes to rhinorhea and nasal blockage. By blocking both the H1 receptor and PAF receptor, rupatidine prevents these mediators from exerting their effects and so reduces the severity of allergic symptoms.

TargetActionsOrganism
APlatelet-activating factor receptor
antagonist
Human
AHistamine H1 receptor
antagonist
Human
Absorption

Rupatidine is rapidly absorbed with a Tmax of 1 h [FDA Label]. Administration with a high fat meal increases exposure by 23% and increases Tmax to 2 h.

Volume of distribution

The apparent volume of distribution is 9799 L [FDA Label].

Protein binding

Rupatidine is 98.5-99.0% bound to human plasma proteins [FDA Label].

Metabolism

Rupatadine is metabolized by oxidation mediated primarily by CYP3A4 [FDA Label]. CYP2C9, CYP2C19, and CYP2D6 are also involved to a lesser extent. The metabolites desloratidine and hydroxylated forms of desloratidine retain some activity as H1 receptor antagonists.

Route of elimination
Not Available
Half life

The half life of elimination is 15.9 h in children 2-5 years old, 12.3 h in children 6-11 years old, 5.9 h in adults, and 8.7 h in geriatric patients [FDA Label].

Clearance

Systemic clearance is 1556.2 L/h in young adults and 798.2 L/h in geriatric patients [FDA Label].

Toxicity
Not Available
Affected organisms
Not Available
Pathways
PathwayCategory
Rupatadine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Rupatadine can be increased when it is combined with Abiraterone.Approved
AmiodaroneThe metabolism of Rupatadine can be decreased when combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Rupatadine can be increased when it is combined with Aprepitant.Approved, Investigational
ArmodafinilThe metabolism of Rupatadine can be decreased when combined with Armodafinil.Approved, Investigational
ArtemetherThe metabolism of Rupatadine can be decreased when combined with Artemether.Approved
AtazanavirThe metabolism of Rupatadine can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Rupatadine can be decreased when combined with Atomoxetine.Approved
BetaxololThe metabolism of Rupatadine can be decreased when combined with Betaxolol.Approved
BoceprevirThe metabolism of Rupatadine can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Rupatadine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Rupatadine can be decreased when it is combined with Bosentan.Approved, Investigational
BupropionThe metabolism of Rupatadine can be decreased when combined with Bupropion.Approved
CapecitabineThe metabolism of Rupatadine can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Rupatadine can be increased when combined with Carbamazepine.Approved, Investigational
CelecoxibThe metabolism of Rupatadine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Rupatadine can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Rupatadine can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChloroquineThe metabolism of Rupatadine can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe metabolism of Rupatadine can be decreased when combined with Chlorpromazine.Approved, Vet Approved
CholecalciferolThe metabolism of Rupatadine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Rupatadine can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Rupatadine can be decreased when combined with Cinacalcet.Approved
CitalopramThe metabolism of Rupatadine can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Rupatadine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Rupatadine can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Rupatadine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Rupatadine can be decreased when combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe metabolism of Rupatadine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Rupatadine can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Rupatadine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Rupatadine can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Rupatadine can be increased when it is combined with Conivaptan.Approved, Investigational
CrisaboroleThe metabolism of Rupatadine can be decreased when combined with Crisaborole.Approved
CrizotinibThe metabolism of Rupatadine can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Rupatadine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Rupatadine can be decreased when it is combined with Dabrafenib.Approved
DarifenacinThe metabolism of Rupatadine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Rupatadine can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Rupatadine can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Rupatadine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Rupatadine can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Rupatadine can be decreased when combined with Desipramine.Approved
DihydroergotamineThe metabolism of Rupatadine can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Rupatadine can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Rupatadine can be decreased when combined with Diphenhydramine.Approved
DosulepinThe metabolism of Rupatadine can be decreased when combined with Dosulepin.Approved
DoxycyclineThe metabolism of Rupatadine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Rupatadine can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Rupatadine can be decreased when combined with Duloxetine.Approved
EfavirenzThe metabolism of Rupatadine can be decreased when combined with Efavirenz.Approved, Investigational
EliglustatThe metabolism of Rupatadine can be decreased when combined with Eliglustat.Approved
EnzalutamideThe serum concentration of Rupatadine can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Rupatadine can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe metabolism of Rupatadine can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Rupatadine can be decreased when combined with Esomeprazole.Approved, Investigational
EtravirineThe metabolism of Rupatadine can be decreased when combined with Etravirine.Approved
FloxuridineThe metabolism of Rupatadine can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Rupatadine can be decreased when combined with Fluconazole.Approved
FluorouracilThe metabolism of Rupatadine can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Rupatadine can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluvastatinThe metabolism of Rupatadine can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Rupatadine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Rupatadine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Rupatadine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Rupatadine can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Rupatadine can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe metabolism of Rupatadine can be decreased when combined with Gemfibrozil.Approved
HaloperidolThe metabolism of Rupatadine can be decreased when combined with Haloperidol.Approved
ImatinibThe metabolism of Rupatadine can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Rupatadine can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Rupatadine can be decreased when combined with Indinavir.Approved
IrbesartanThe metabolism of Rupatadine can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Rupatadine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Rupatadine can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Rupatadine can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Rupatadine can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Rupatadine can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Rupatadine can be decreased when combined with Ketoconazole.Approved, Investigational
LeflunomideThe metabolism of Rupatadine can be decreased when combined with Leflunomide.Approved, Investigational
LobeglitazoneThe metabolism of Rupatadine can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe metabolism of Rupatadine can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Rupatadine can be decreased when combined with Lorcaserin.Approved
LosartanThe metabolism of Rupatadine can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Rupatadine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Rupatadine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Rupatadine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Rupatadine can be decreased when combined with Lumefantrine.Approved
ManidipineThe metabolism of Rupatadine can be decreased when combined with Manidipine.Approved, Investigational
MethadoneThe metabolism of Rupatadine can be decreased when combined with Methadone.Approved
MethotrimeprazineThe metabolism of Rupatadine can be decreased when combined with Methotrimeprazine.Approved
MetoprololThe metabolism of Rupatadine can be decreased when combined with Metoprolol.Approved, Investigational
MidostaurinThe metabolism of Rupatadine can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Rupatadine can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Rupatadine can be decreased when combined with Mirabegron.Approved
MitotaneThe serum concentration of Rupatadine can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Rupatadine can be decreased when combined with Moclobemide.Approved
ModafinilThe metabolism of Rupatadine can be decreased when combined with Modafinil.Approved, Investigational
NefazodoneThe metabolism of Rupatadine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Rupatadine can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Rupatadine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Rupatadine can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Rupatadine can be decreased when combined with Nicardipine.Approved
NilotinibThe metabolism of Rupatadine can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Rupatadine can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Rupatadine can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Rupatadine can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Rupatadine can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Rupatadine can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Rupatadine can be decreased when combined with Pantoprazole.Approved
ParoxetineThe metabolism of Rupatadine can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Rupatadine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Rupatadine can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Rupatadine can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Rupatadine can be increased when combined with Phenytoin.Approved, Vet Approved
PosaconazoleThe metabolism of Rupatadine can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Rupatadine can be increased when combined with Primidone.Approved, Vet Approved
PromazineThe metabolism of Rupatadine can be decreased when combined with Promazine.Approved, Vet Approved
PyrimethamineThe metabolism of Rupatadine can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuinidineThe metabolism of Rupatadine can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Rupatadine can be decreased when combined with Quinine.Approved
RanolazineThe metabolism of Rupatadine can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Rupatadine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Rupatadine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Rupatadine can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Rupatadine can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe metabolism of Rupatadine can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Rupatadine can be decreased when combined with Ropinirole.Approved, Investigational
SaquinavirThe metabolism of Rupatadine can be decreased when combined with Saquinavir.Approved, Investigational
SecobarbitalThe metabolism of Rupatadine can be increased when combined with Secobarbital.Approved, Vet Approved
SertralineThe metabolism of Rupatadine can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Rupatadine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Rupatadine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Rupatadine can be increased when it is combined with Simeprevir.Approved
SorafenibThe metabolism of Rupatadine can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Rupatadine can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Rupatadine can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Rupatadine can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Rupatadine can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Rupatadine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TelaprevirThe metabolism of Rupatadine can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Rupatadine can be decreased when combined with Telithromycin.Approved
TerbinafineThe metabolism of Rupatadine can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
ThioridazineThe metabolism of Rupatadine can be decreased when combined with Thioridazine.Approved, Withdrawn
TicagrelorThe metabolism of Rupatadine can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Rupatadine can be decreased when combined with Ticlopidine.Approved
TipranavirThe metabolism of Rupatadine can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Rupatadine can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Rupatadine can be decreased when combined with Tolbutamide.Approved
TopiramateThe metabolism of Rupatadine can be decreased when combined with Topiramate.Approved
TopiroxostatThe metabolism of Rupatadine can be decreased when combined with Topiroxostat.Approved, Investigational
TranylcypromineThe metabolism of Rupatadine can be decreased when combined with Tranylcypromine.Approved
TrimethoprimThe metabolism of Rupatadine can be decreased when combined with Trimethoprim.Approved, Vet Approved
Valproic AcidThe metabolism of Rupatadine can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Rupatadine can be decreased when combined with Valsartan.Approved, Investigational
VenlafaxineThe metabolism of Rupatadine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Rupatadine can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Rupatadine can be decreased when combined with Voriconazole.Approved, Investigational
ZafirlukastThe metabolism of Rupatadine can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Rupatadine can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe metabolism of Rupatadine can be decreased when combined with Zucapsaicin.Approved
Food Interactions
Not Available

References

General References
  1. Merlos M, Giral M, Balsa D, Ferrando R, Queralt M, Puigdemont A, Garcia-Rafanell J, Forn J: Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [PubMed:8996188]
  2. Alfaro V: Role of histamine and platelet-activating factor in allergic rhinitis. J Physiol Biochem. 2004 Jun;60(2):101-11. [PubMed:15457928]
External Links
PubChem Compound
133017
PubChem Substance
347828008
ChemSpider
117388
BindingDB
50036935
ChEBI
135673
ChEMBL
CHEMBL91397
PharmGKB
PA165107052
Wikipedia
Rupatadine
ATC Codes
R06AX28 — Rupatadine
AHFS Codes
  • 04:08.00 — Second Generation Antihistamines
FDA label
Download (794 KB)
MSDS
Download (56.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHuman Experimentation (Human Volunteers)1
2CompletedTreatmentCold Contact Urticaria1
2TerminatedTreatmentUrticarias1
3RecruitingTreatmentChronic Urticaria1
3TerminatedTreatmentUrticarias1
4TerminatedPreventionHealthy Volunteers1
4Unknown StatusPreventionAllergies1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
SolutionOral1 mg
TabletOral10 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)194-201FDA Label
logP0.8FDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.00544 mg/mLALOGPS
logP4.82ALOGPS
logP5.37ChemAxon
logS-4.9ALOGPS
pKa (Strongest Basic)7.19ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area29.02 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity133.83 m3·mol-1ChemAxon
Polarizability46.98 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as benzocycloheptapyridines. These are aromatic compounds containing a benzene ring and a pyridine ring fused to a seven membered carbocycle.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzocycloheptapyridines
Sub Class
Not Available
Direct Parent
Benzocycloheptapyridines
Alternative Parents
Methylpyridines / Aralkylamines / Piperidines / Benzenoids / Aryl chlorides / Heteroaromatic compounds / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organochlorides
show 1 more
Substituents
Benzocycloheptapyridine / Methylpyridine / Aralkylamine / Aryl chloride / Aryl halide / Piperidine / Benzenoid / Pyridine / Heteroaromatic compound / Tertiary aliphatic amine
show 10 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Platelet activating factor receptor activity
Specific Function
Receptor for platelet activating factor, a chemotactic phospholipid mediator that possesses potent inflammatory, smooth-muscle contractile and hypotensive activity. Seems to mediate its action via ...
Gene Name
PTAFR
Uniprot ID
P25105
Uniprot Name
Platelet-activating factor receptor
Molecular Weight
39203.075 Da
References
  1. Merlos M, Giral M, Balsa D, Ferrando R, Queralt M, Puigdemont A, Garcia-Rafanell J, Forn J: Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [PubMed:8996188]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Merlos M, Giral M, Balsa D, Ferrando R, Queralt M, Puigdemont A, Garcia-Rafanell J, Forn J: Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [PubMed:8996188]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da

Drug created on August 05, 2016 17:52 / Updated on December 11, 2017 13:02