Identification

Name
Cinnarizine
Accession Number
DB00568  (APRD00332)
Type
Small Molecule
Groups
Approved, Investigational
Description

Cinnarizine is an anti-histaminic drug which is mainly used for the control of vomiting due to motion sickness. Cinnarizine was first synthesized by Janssen Pharmaceutica in 1955.

It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus. The disparity of signal processing between inner ear motion receptors and the visual senses is abolished, so that the confusion of brain whether the individual is moving or standing is reduced. Vomiting in motion sickness is actually a physiological compensatory mechanism of the brain to keep the individual from moving so that it can adjust to the signal perception.

Cinnarizine could be also viewed as a nootropic drug because of its vasorelaxating abilities (due to calcium channel blockage), which happen mostly in brain. It is also effectively combined with other nootropics, primarily piracetam; in such combination each drug potentiate the other in boosting brain oxygen supply.

Structure
Thumb
Synonyms
  • 1-(Diphenylmethyl)-4-(3-phenyl-2-propenyl)piperazine
  • 1-Benzhydryl-4-cinnamylpiperazin
  • 1-Cinnamyl-4-(diphenylmethyl)piperazine
  • Cinarizina
  • Cinnarizine
  • Cinnarizinum
External IDs
5-23-01-00233 / 516 MD / 516-MD / BRN 0626121 / R 1575 / R 516 / UNII-3DI2E1X18L
Product Ingredients
IngredientUNIICASInChI Key
Cinnarizine hydrochloride5AKM4OA6VO25332-14-3LYXJDKBTSDYXQV-RSGUCCNWSA-N
International/Other Brands
Cinazyn (Italchimici) / Cinnageron (Streuli Pharma) / Folcodal (Ivax) / Sepan (Janssen-Cilag) / Stugeron (Janssen) / Stugeron Forte (Janssen) / Toliman (Scharper)
Categories
UNII
3DI2E1X18L
CAS number
298-57-7
Weight
Average: 368.5139
Monoisotopic: 368.225248906
Chemical Formula
C26H28N2
InChI Key
DERZBLKQOCDDDZ-JLHYYAGUSA-N
InChI
InChI=1S/C26H28N2/c1-4-11-23(12-5-1)13-10-18-27-19-21-28(22-20-27)26(24-14-6-2-7-15-24)25-16-8-3-9-17-25/h1-17,26H,18-22H2/b13-10+
IUPAC Name
1-(diphenylmethyl)-4-(3-phenylprop-2-en-1-yl)piperazine
SMILES
C(C=CC1=CC=CC=C1)N1CCN(CC1)C(C1=CC=CC=C1)C1=CC=CC=C1

Pharmacology

Indication

For the treatment of vertigo/meniere's disease, nausea and vomiting, motion sickness and also useful for vestibular symptoms of other origins.

Pharmacodynamics

Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system.

Mechanism of action

Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking L-type and T-type voltage gated calcium channels. Cinnarizine has also been implicated in binding to dopamine D2 receptors, histamine H1 receptors, and muscarinic acetylcholine receptors.

TargetActionsOrganism
AHistamine H1 receptor
antagonist
Human
AVoltage-dependent L-type calcium channel subunit alpha-1C
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1D
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1F
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1S
inhibitor
Human
AVoltage-dependent T-type calcium channel subunit alpha-1G
inhibitor
Human
AVoltage-dependent T-type calcium channel subunit alpha-1H
inhibitor
Human
AVoltage-dependent T-type calcium channel subunit alpha-1I
inhibitor
Human
ND(2) dopamine receptor
other/unknown
Human
UD(1) dopamine receptor
binder
Human
UMuscarinic acetylcholine receptor
binder
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Cinnarizine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2-HYDROXY-1,4-NAPHTHOQUINONEThe therapeutic efficacy of 2-HYDROXY-1,4-NAPHTHOQUINONE can be increased when used in combination with Cinnarizine.Experimental
2-mercaptobenzothiazoleThe therapeutic efficacy of 2-mercaptobenzothiazole can be increased when used in combination with Cinnarizine.Vet Approved
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Cinnarizine.Experimental, Illicit
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Cinnarizine.Experimental
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Cinnarizine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Cinnarizine.Experimental, Illicit
AbirateroneThe serum concentration of Cinnarizine can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of hypotension can be increased when Acepromazine is combined with Cinnarizine.Approved, Vet Approved
Acetyl sulfisoxazoleThe metabolism of Cinnarizine can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AlfuzosinThe risk or severity of hypotension can be increased when Alfuzosin is combined with Cinnarizine.Approved, Investigational
AmiodaroneThe metabolism of Cinnarizine can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe risk or severity of hypotension can be increased when Amitriptyline is combined with Cinnarizine.Approved
AmobarbitalThe metabolism of Cinnarizine can be increased when combined with Amobarbital.Approved, Illicit
AmorolfineThe therapeutic efficacy of Amorolfine can be increased when used in combination with Cinnarizine.Approved, Investigational
AmoxapineThe risk or severity of hypotension can be increased when Amoxapine is combined with Cinnarizine.Approved
AmphetamineAmphetamine may decrease the sedative activities of Cinnarizine.Approved, Illicit, Investigational
Amphotericin BThe therapeutic efficacy of Amphotericin B can be increased when used in combination with Cinnarizine.Approved, Investigational
AnidulafunginThe therapeutic efficacy of Anidulafungin can be increased when used in combination with Cinnarizine.Approved, Investigational
ApalutamideThe serum concentration of Cinnarizine can be decreased when it is combined with Apalutamide.Approved, Investigational
AprepitantThe metabolism of Cinnarizine can be increased when combined with Aprepitant.Approved, Investigational
AripiprazoleThe risk or severity of hypotension can be increased when Aripiprazole is combined with Cinnarizine.Approved, Investigational
ArotinololThe risk or severity of hypotension, conduction block, and bradycardia can be increased when Arotinolol is combined with Cinnarizine.Investigational
ArtemetherThe metabolism of Cinnarizine can be decreased when combined with Artemether.Approved
AsenapineThe risk or severity of hypotension can be increased when Asenapine is combined with Cinnarizine.Approved
AtomoxetineThe metabolism of Cinnarizine can be decreased when combined with Atomoxetine.Approved
AzithromycinThe metabolism of Cinnarizine can be decreased when combined with Azithromycin.Approved
Bafilomycin A1The therapeutic efficacy of Bafilomycin A1 can be increased when used in combination with Cinnarizine.Experimental
BarbexacloneThe metabolism of Cinnarizine can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Cinnarizine can be increased when combined with Barbital.Illicit
Benzoic AcidThe therapeutic efficacy of Benzoic Acid can be increased when used in combination with Cinnarizine.Approved, Investigational
BenzphetamineBenzphetamine may decrease the sedative activities of Cinnarizine.Approved, Illicit
Benzylpenicilloyl PolylysineCinnarizine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Cinnarizine.Approved, Investigational
BetaxololThe metabolism of Cinnarizine can be decreased when combined with Betaxolol.Approved, Investigational
BevantololThe risk or severity of hypotension can be increased when Bevantolol is combined with Cinnarizine.Approved
BifonazoleThe therapeutic efficacy of Bifonazole can be increased when used in combination with Cinnarizine.Approved, Investigational
BortezomibThe metabolism of Cinnarizine can be decreased when combined with Bortezomib.Approved, Investigational
Brefeldin AThe therapeutic efficacy of Brefeldin A can be increased when used in combination with Cinnarizine.Experimental
BrexpiprazoleThe risk or severity of hypotension can be increased when Brexpiprazole is combined with Cinnarizine.Approved, Investigational
BucindololThe risk or severity of hypotension can be increased when Bucindolol is combined with Cinnarizine.Investigational
BunazosinThe risk or severity of hypotension can be increased when Bunazosin is combined with Cinnarizine.Investigational
BupropionThe metabolism of Cinnarizine can be decreased when combined with Bupropion.Approved
ButenafineThe therapeutic efficacy of Butenafine can be increased when used in combination with Cinnarizine.Approved
ButoconazoleThe therapeutic efficacy of Butoconazole can be increased when used in combination with Cinnarizine.Approved
CaffeineThe metabolism of Cinnarizine can be decreased when combined with Caffeine.Approved
Calcium AcetateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium Acetate.Approved, Investigational
Calcium CarbonateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium Carbonate.Approved, Investigational
Calcium ChlorideThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium Chloride.Approved
Calcium CitrateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium Citrate.Approved
Calcium glubionateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium glubionate.Approved
Calcium GluceptateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium Gluceptate.Approved
Calcium gluconateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium gluconate.Approved, Vet Approved
Calcium lactateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium lactate.Approved, Investigational, Vet Approved
Calcium lactate gluconateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium lactate gluconate.Experimental
Calcium levulinateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium levulinate.Approved, Experimental
Calcium pangamateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium pangamate.Experimental
Calcium PhosphateThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Calcium Phosphate.Approved
CandicidinThe therapeutic efficacy of Candicidin can be increased when used in combination with Cinnarizine.Withdrawn
CapecitabineThe metabolism of Cinnarizine can be decreased when combined with Capecitabine.Approved, Investigational
Capric acidThe therapeutic efficacy of Capric acid can be increased when used in combination with Cinnarizine.Experimental
CarbamazepineThe metabolism of Cinnarizine can be increased when combined with Carbamazepine.Approved, Investigational
CarvedilolThe risk or severity of hypotension can be increased when Carvedilol is combined with Cinnarizine.Approved, Investigational
CaseinThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Casein.Approved
CaspofunginThe therapeutic efficacy of Caspofungin can be increased when used in combination with Cinnarizine.Approved
CelecoxibThe metabolism of Cinnarizine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Cinnarizine can be increased when it is combined with Ceritinib.Approved
CeruleninThe therapeutic efficacy of Cerulenin can be increased when used in combination with Cinnarizine.Approved
ChloroquineThe metabolism of Cinnarizine can be decreased when combined with Chloroquine.Approved, Investigational, Vet Approved
ChloroxineThe therapeutic efficacy of Chloroxine can be increased when used in combination with Cinnarizine.Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Cinnarizine.Illicit, Withdrawn
ChlorpromazineThe metabolism of Cinnarizine can be decreased when combined with Chlorpromazine.Approved, Investigational, Vet Approved
CholecalciferolThe metabolism of Cinnarizine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CiclopiroxThe therapeutic efficacy of Ciclopirox can be increased when used in combination with Cinnarizine.Approved, Investigational
CimetidineThe serum concentration of Cinnarizine can be increased when it is combined with Cimetidine.Approved, Investigational
CinacalcetThe metabolism of Cinnarizine can be decreased when combined with Cinacalcet.Approved
CitalopramThe metabolism of Cinnarizine can be decreased when combined with Citalopram.Approved
ClemastineThe metabolism of Cinnarizine can be decreased when combined with Clemastine.Approved, Investigational
ClobazamThe metabolism of Cinnarizine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Cinnarizine can be decreased when combined with Clomipramine.Approved, Investigational, Vet Approved
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Cinnarizine.Approved
ClotrimazoleThe metabolism of Cinnarizine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Cinnarizine can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Cinnarizine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Cinnarizine can be decreased when combined with Cocaine.Approved, Illicit
CordycepinThe therapeutic efficacy of Cordycepin can be increased when used in combination with Cinnarizine.Investigational
CrisaboroleThe metabolism of Cinnarizine can be decreased when combined with Crisaborole.Approved, Investigational
CrizotinibThe metabolism of Cinnarizine can be decreased when combined with Crizotinib.Approved
CurcuminThe metabolism of Cinnarizine can be decreased when combined with Curcumin.Approved, Investigational
CyclosporineThe metabolism of Cinnarizine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Cinnarizine can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Cinnarizine can be decreased when it is combined with Dabrafenib.Approved, Investigational
DapiprazoleThe risk or severity of hypotension can be increased when Dapiprazole is combined with Cinnarizine.Approved
DarifenacinThe metabolism of Cinnarizine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Cinnarizine can be increased when it is combined with Darunavir.Approved
DeferasiroxThe serum concentration of Cinnarizine can be increased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Cinnarizine can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Cinnarizine can be decreased when combined with Desipramine.Approved, Investigational
DextroamphetamineDextroamphetamine may decrease the sedative activities of Cinnarizine.Approved, Illicit
DichloropheneThe therapeutic efficacy of Dichlorophene can be increased when used in combination with Cinnarizine.Vet Approved
DiethylpropionDiethylpropion may decrease the sedative activities of Cinnarizine.Approved, Illicit
DiphenhydramineThe metabolism of Cinnarizine can be decreased when combined with Diphenhydramine.Approved, Investigational
DosulepinThe metabolism of Cinnarizine can be decreased when combined with Dosulepin.Approved
DoxazosinThe risk or severity of hypotension can be increased when Doxazosin is combined with Cinnarizine.Approved
DoxepinThe risk or severity of hypotension can be increased when Doxepin is combined with Cinnarizine.Approved, Investigational
DoxorubicinThe metabolism of Cinnarizine can be decreased when combined with Doxorubicin.Approved, Investigational
DronedaroneThe metabolism of Cinnarizine can be decreased when combined with Dronedarone.Approved
DroperidolThe risk or severity of hypotension can be increased when Droperidol is combined with Cinnarizine.Approved, Vet Approved
DuloxetineThe metabolism of Cinnarizine can be decreased when combined with Duloxetine.Approved
EconazoleThe therapeutic efficacy of Econazole can be increased when used in combination with Cinnarizine.Approved
EfavirenzThe serum concentration of Cinnarizine can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe therapeutic efficacy of Efinaconazole can be increased when used in combination with Cinnarizine.Approved
EliglustatThe metabolism of Cinnarizine can be decreased when combined with Eliglustat.Approved
EpinephrineThe risk or severity of hypotension can be increased when Epinephrine is combined with Cinnarizine.Approved, Vet Approved
EscitalopramThe risk or severity of hypotension can be increased when Escitalopram is combined with Cinnarizine.Approved, Investigational
EtravirineThe metabolism of Cinnarizine can be decreased when combined with Etravirine.Approved
FenticonazoleThe therapeutic efficacy of Fenticonazole can be increased when used in combination with Cinnarizine.Experimental
FloxuridineThe metabolism of Cinnarizine can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Cinnarizine can be decreased when combined with Fluconazole.Approved, Investigational
FlucytosineThe therapeutic efficacy of Flucytosine can be increased when used in combination with Cinnarizine.Approved, Investigational
FluorouracilThe metabolism of Cinnarizine can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Cinnarizine can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of hypotension can be increased when Flupentixol is combined with Cinnarizine.Approved, Investigational, Withdrawn
FlutrimazoleThe therapeutic efficacy of Flutrimazole can be increased when used in combination with Cinnarizine.Experimental
FluvastatinThe metabolism of Cinnarizine can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Cinnarizine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosphenytoinThe metabolism of Cinnarizine can be increased when combined with Fosphenytoin.Approved, Investigational
GemfibrozilThe metabolism of Cinnarizine can be decreased when combined with Gemfibrozil.Approved
GepefrineGepefrine may decrease the sedative activities of Cinnarizine.Experimental
GlyphosateThe therapeutic efficacy of Glyphosate can be increased when used in combination with Cinnarizine.Experimental
GriseofulvinThe therapeutic efficacy of Griseofulvin can be increased when used in combination with Cinnarizine.Approved, Investigational, Vet Approved
HachimycinThe therapeutic efficacy of Hachimycin can be increased when used in combination with Cinnarizine.Experimental
HaloperidolThe metabolism of Cinnarizine can be decreased when combined with Haloperidol.Approved
HaloproginThe therapeutic efficacy of Haloprogin can be increased when used in combination with Cinnarizine.Approved, Withdrawn
HexetidineThe therapeutic efficacy of Hexetidine can be increased when used in combination with Cinnarizine.Approved, Investigational
HexobarbitalThe metabolism of Cinnarizine can be increased when combined with Hexobarbital.Approved
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Cinnarizine.Approved, Investigational
HydroxyamphetamineHydroxyamphetamine may decrease the sedative activities of Cinnarizine.Approved
IloperidoneThe risk or severity of hypotension can be increased when Iloperidone is combined with Cinnarizine.Approved
ImipramineThe metabolism of Cinnarizine can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Cinnarizine can be decreased when combined with Indinavir.Approved
IndoraminThe risk or severity of hypotension can be increased when Indoramin is combined with Cinnarizine.Withdrawn
Iofetamine I-123Iofetamine I-123 may decrease the sedative activities of Cinnarizine.Approved
IrbesartanThe metabolism of Cinnarizine can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoleThe serum concentration of Cinnarizine can be decreased when it is combined with Isavuconazole.Approved, Investigational
IsoconazoleThe therapeutic efficacy of Isoconazole can be increased when used in combination with Cinnarizine.Approved
IsoniazidThe metabolism of Cinnarizine can be decreased when combined with Isoniazid.Approved, Investigational
ItraconazoleThe therapeutic efficacy of Itraconazole can be increased when used in combination with Cinnarizine.Approved, Investigational
KetoconazoleThe metabolism of Cinnarizine can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolThe risk or severity of hypotension can be increased when Labetalol is combined with Cinnarizine.Approved
LeflunomideThe metabolism of Cinnarizine can be decreased when combined with Leflunomide.Approved, Investigational
LidocaineThe metabolism of Cinnarizine can be decreased when combined with Lidocaine.Approved, Vet Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Cinnarizine.Approved, Investigational
LobeglitazoneThe metabolism of Cinnarizine can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe metabolism of Cinnarizine can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Cinnarizine can be decreased when combined with Lorcaserin.Approved
LosartanThe metabolism of Cinnarizine can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Cinnarizine can be decreased when combined with Lovastatin.Approved, Investigational
LumacaftorThe serum concentration of Cinnarizine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Cinnarizine can be decreased when combined with Lumefantrine.Approved
Magnesium hydroxideThe risk or severity of hypotension and neuromuscular blockade can be increased when Cinnarizine is combined with Magnesium hydroxide.Approved, Investigational
Magnesium oxideThe risk or severity of hypotension and neuromuscular blockade can be increased when Cinnarizine is combined with Magnesium oxide.Approved
Magnesium salicylateThe risk or severity of hypotension and neuromuscular blockade can be increased when Cinnarizine is combined with Magnesium salicylate.Approved
Magnesium sulfateThe risk or severity of hypotension and neuromuscular blockade can be increased when Cinnarizine is combined with Magnesium sulfate.Approved, Investigational, Vet Approved
ManidipineThe metabolism of Cinnarizine can be decreased when combined with Manidipine.Approved, Investigational
MepartricinThe therapeutic efficacy of Mepartricin can be increased when used in combination with Cinnarizine.Experimental
MephedroneMephedrone may decrease the sedative activities of Cinnarizine.Investigational
MephentermineMephentermine may decrease the sedative activities of Cinnarizine.Approved
MethadoneThe metabolism of Cinnarizine can be decreased when combined with Methadone.Approved
MethamphetamineMethamphetamine may decrease the sedative activities of Cinnarizine.Approved, Illicit
MethohexitalThe metabolism of Cinnarizine can be increased when combined with Methohexital.Approved
MethotrimeprazineThe metabolism of Cinnarizine can be decreased when combined with Methotrimeprazine.Approved, Investigational
MethoxyphenamineMethoxyphenamine may decrease the sedative activities of Cinnarizine.Experimental
MethylphenobarbitalThe metabolism of Cinnarizine can be increased when combined with Methylphenobarbital.Approved
MetoprololThe metabolism of Cinnarizine can be decreased when combined with Metoprolol.Approved, Investigational
MevastatinThe therapeutic efficacy of Mevastatin can be increased when used in combination with Cinnarizine.Experimental
MexiletineThe metabolism of Cinnarizine can be decreased when combined with Mexiletine.Approved, Investigational
MicafunginThe therapeutic efficacy of Micafungin can be increased when used in combination with Cinnarizine.Approved, Investigational
MiconazoleThe therapeutic efficacy of Miconazole can be increased when used in combination with Cinnarizine.Approved, Investigational, Vet Approved
MidomafetamineMidomafetamine may decrease the sedative activities of Cinnarizine.Experimental, Illicit, Investigational
MidostaurinThe metabolism of Cinnarizine can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Cinnarizine can be increased when it is combined with Mifepristone.Approved, Investigational
MiltefosineThe therapeutic efficacy of Miltefosine can be increased when used in combination with Cinnarizine.Approved, Investigational
MirabegronThe metabolism of Cinnarizine can be decreased when combined with Mirabegron.Approved
MMDAMMDA may decrease the sedative activities of Cinnarizine.Experimental, Illicit
MonensinThe therapeutic efficacy of Monensin can be increased when used in combination with Cinnarizine.Vet Approved
MyxothiazolThe therapeutic efficacy of Myxothiazol can be increased when used in combination with Cinnarizine.Experimental
NabiloneThe metabolism of Cinnarizine can be decreased when combined with Nabilone.Approved, Investigational
NafcillinThe therapeutic efficacy of Cinnarizine can be decreased when used in combination with Nafcillin.Approved, Investigational
NaftifineThe therapeutic efficacy of Naftifine can be increased when used in combination with Cinnarizine.Approved
NatamycinThe therapeutic efficacy of Natamycin can be increased when used in combination with Cinnarizine.Approved
NefazodoneThe risk or severity of hypotension can be increased when Nefazodone is combined with Cinnarizine.Approved, Withdrawn
NevirapineThe metabolism of Cinnarizine can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Cinnarizine can be decreased when combined with Nicardipine.Approved, Investigational
NicergolineThe risk or severity of hypotension can be increased when Nicergoline is combined with Cinnarizine.Approved, Investigational
NicotineThe metabolism of Cinnarizine can be decreased when combined with Nicotine.Approved
NifuratelThe therapeutic efficacy of Nifuratel can be increased when used in combination with Cinnarizine.Experimental
NiguldipineThe risk or severity of hypotension can be increased when Niguldipine is combined with Cinnarizine.Experimental
Nikkomycin ZThe therapeutic efficacy of Nikkomycin Z can be increased when used in combination with Cinnarizine.Investigational
NilotinibThe metabolism of Cinnarizine can be decreased when combined with Nilotinib.Approved, Investigational
NitroprussideCinnarizine may increase the hypotensive activities of Nitroprusside.Approved, Investigational
NitroxolineThe therapeutic efficacy of Nitroxoline can be increased when used in combination with Cinnarizine.Approved
NortriptylineThe risk or severity of hypotension can be increased when Nortriptyline is combined with Cinnarizine.Approved
NystatinThe therapeutic efficacy of Nystatin can be increased when used in combination with Cinnarizine.Approved, Vet Approved
OlanzapineThe risk or severity of hypotension can be increased when Olanzapine is combined with Cinnarizine.Approved, Investigational
OmeprazoleThe metabolism of Cinnarizine can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OmoconazoleThe therapeutic efficacy of Omoconazole can be increased when used in combination with Cinnarizine.Experimental
OsimertinibThe serum concentration of Cinnarizine can be decreased when it is combined with Osimertinib.Approved
OxiconazoleThe therapeutic efficacy of Oxiconazole can be increased when used in combination with Cinnarizine.Approved
PafuramidineThe therapeutic efficacy of Pafuramidine can be increased when used in combination with Cinnarizine.Investigational
PaliperidoneThe risk or severity of hypotension can be increased when Paliperidone is combined with Cinnarizine.Approved
PanobinostatThe serum concentration of Cinnarizine can be increased when it is combined with Panobinostat.Approved, Investigational
ParoxetineThe metabolism of Cinnarizine can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Cinnarizine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidineThe therapeutic efficacy of Pentamidine can be increased when used in combination with Cinnarizine.Approved, Investigational
PentobarbitalThe metabolism of Cinnarizine can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PhenobarbitalThe metabolism of Cinnarizine can be increased when combined with Phenobarbital.Approved, Investigational
PhenoxybenzamineThe risk or severity of hypotension can be increased when Phenoxybenzamine is combined with Cinnarizine.Approved
PhenterminePhentermine may decrease the sedative activities of Cinnarizine.Approved, Illicit
PhentolamineThe risk or severity of hypotension can be increased when Phentolamine is combined with Cinnarizine.Approved
PhenytoinThe metabolism of Cinnarizine can be increased when combined with Phenytoin.Approved, Vet Approved
PitolisantThe serum concentration of Cinnarizine can be decreased when it is combined with Pitolisant.Approved, Investigational
PizotifenThe risk or severity of hypotension can be increased when Pizotifen is combined with Cinnarizine.Approved
PosaconazoleThe therapeutic efficacy of Posaconazole can be increased when used in combination with Cinnarizine.Approved, Investigational, Vet Approved
PrazosinThe risk or severity of hypotension can be increased when Prazosin is combined with Cinnarizine.Approved
PrimidoneThe metabolism of Cinnarizine can be increased when combined with Primidone.Approved, Vet Approved
PromazineThe metabolism of Cinnarizine can be decreased when combined with Promazine.Approved, Vet Approved
PropericiazineThe risk or severity of hypotension can be increased when Propericiazine is combined with Cinnarizine.Approved, Investigational
PropiomazineThe risk or severity of hypotension can be increased when Propiomazine is combined with Cinnarizine.Approved
PropiverineThe risk or severity of hypotension can be increased when Propiverine is combined with Cinnarizine.Approved, Investigational
PseudoephedrinePseudoephedrine may decrease the sedative activities of Cinnarizine.Approved
PyrimethamineThe metabolism of Cinnarizine can be decreased when combined with Pyrimethamine.Approved, Investigational, Vet Approved
PyrrolnitrinThe therapeutic efficacy of Pyrrolnitrin can be increased when used in combination with Cinnarizine.Experimental
QuazepamThe serum concentration of Cinnarizine can be increased when it is combined with Quazepam.Approved, Illicit
QuetiapineThe risk or severity of hypotension can be increased when Quetiapine is combined with Cinnarizine.Approved
QuinidineThe metabolism of Cinnarizine can be decreased when combined with Quinidine.Approved, Investigational
QuinineThe metabolism of Cinnarizine can be decreased when combined with Quinine.Approved
RacepinephrineThe risk or severity of hypotension can be increased when Racepinephrine is combined with Cinnarizine.Approved
RadicicolThe therapeutic efficacy of Radicicol can be increased when used in combination with Cinnarizine.Experimental
RanolazineThe metabolism of Cinnarizine can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe risk or severity of hypotension can be increased when Rifabutin is combined with Cinnarizine.Approved, Investigational
RifampicinThe metabolism of Cinnarizine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Cinnarizine can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe risk or severity of hypotension can be increased when Rifaximin is combined with Cinnarizine.Approved, Investigational
RisperidoneThe risk or severity of hypotension can be increased when Risperidone is combined with Cinnarizine.Approved, Investigational
RitobegronRitobegron may decrease the sedative activities of Cinnarizine.Investigational
RitonavirThe metabolism of Cinnarizine can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe metabolism of Cinnarizine can be decreased when combined with Rolapitant.Approved, Investigational
RopiniroleThe metabolism of Cinnarizine can be decreased when combined with Ropinirole.Approved, Investigational
RucaparibThe metabolism of Cinnarizine can be decreased when combined with Rucaparib.Approved, Investigational
Salicylhydroxamic AcidThe therapeutic efficacy of Salicylhydroxamic Acid can be increased when used in combination with Cinnarizine.Experimental
Salicylic acidThe therapeutic efficacy of Salicylic acid can be increased when used in combination with Cinnarizine.Approved, Investigational, Vet Approved
SecobarbitalThe metabolism of Cinnarizine can be increased when combined with Secobarbital.Approved, Vet Approved
SertaconazoleThe therapeutic efficacy of Sertaconazole can be increased when used in combination with Cinnarizine.Approved, Investigational
SertralineThe metabolism of Cinnarizine can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Cinnarizine can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe risk or severity of hypotension can be increased when Silodosin is combined with Cinnarizine.Approved
SimeprevirThe metabolism of Cinnarizine can be decreased when combined with Simeprevir.Approved
SinefunginThe therapeutic efficacy of Sinefungin can be increased when used in combination with Cinnarizine.Experimental
SirolimusThe therapeutic efficacy of Sirolimus can be increased when used in combination with Cinnarizine.Approved, Investigational
SorafenibThe metabolism of Cinnarizine can be decreased when combined with Sorafenib.Approved, Investigational
StiripentolThe metabolism of Cinnarizine can be decreased when combined with Stiripentol.Approved
SulconazoleThe therapeutic efficacy of Sulconazole can be increased when used in combination with Cinnarizine.Approved
SulfadiazineThe metabolism of Cinnarizine can be decreased when combined with Sulfadiazine.Approved, Investigational, Vet Approved
SulfamethoxazoleThe metabolism of Cinnarizine can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Cinnarizine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TamsulosinThe risk or severity of hypotension can be increased when Tamsulosin is combined with Cinnarizine.Approved, Investigational
TavaboroleThe therapeutic efficacy of Tavaborole can be increased when used in combination with Cinnarizine.Approved, Investigational
Tenofovir disoproxilThe metabolism of Cinnarizine can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerazosinThe risk or severity of hypotension can be increased when Terazosin is combined with Cinnarizine.Approved
TerbinafineThe metabolism of Cinnarizine can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerconazoleThe therapeutic efficacy of Terconazole can be increased when used in combination with Cinnarizine.Approved
TeriflunomideThe serum concentration of Cinnarizine can be decreased when it is combined with Teriflunomide.Approved
TheophyllineThe metabolism of Cinnarizine can be decreased when combined with Theophylline.Approved
ThiamylalThe metabolism of Cinnarizine can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Cinnarizine can be increased when combined with Thiopental.Approved, Vet Approved
ThioproperazineThe risk or severity of hypotension can be increased when Thioproperazine is combined with Cinnarizine.Approved
ThioridazineThe metabolism of Cinnarizine can be decreased when combined with Thioridazine.Approved, Withdrawn
ThiotepaThe metabolism of Cinnarizine can be decreased when combined with Thiotepa.Approved, Investigational
ThymolThe therapeutic efficacy of Thymol can be increased when used in combination with Cinnarizine.Approved
TicagrelorThe metabolism of Cinnarizine can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Cinnarizine can be decreased when combined with Ticlopidine.Approved
TioconazoleThe therapeutic efficacy of Tioconazole can be increased when used in combination with Cinnarizine.Approved
TipranavirThe metabolism of Cinnarizine can be decreased when combined with Tipranavir.Approved, Investigational
TolazolineThe risk or severity of hypotension can be increased when Tolazoline is combined with Cinnarizine.Approved, Vet Approved
TolbutamideThe metabolism of Cinnarizine can be decreased when combined with Tolbutamide.Approved, Investigational
TolciclateThe therapeutic efficacy of Tolciclate can be increased when used in combination with Cinnarizine.Experimental
TolnaftateThe therapeutic efficacy of Tolnaftate can be increased when used in combination with Cinnarizine.Approved, Investigational, Vet Approved
TopiroxostatThe metabolism of Cinnarizine can be decreased when combined with Topiroxostat.Approved, Investigational
TranylcypromineThe metabolism of Cinnarizine can be decreased when combined with Tranylcypromine.Approved, Investigational
TrazodoneThe risk or severity of hypotension can be increased when Trazodone is combined with Cinnarizine.Approved, Investigational
TrifluoperazineThe risk or severity of hypotension can be increased when Trifluoperazine is combined with Cinnarizine.Approved, Investigational
TrimazosinThe risk or severity of hypotension can be increased when Trimazosin is combined with Cinnarizine.Experimental
TrimethoprimThe metabolism of Cinnarizine can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimetrexateThe therapeutic efficacy of Trimetrexate can be increased when used in combination with Cinnarizine.Approved, Investigational
TrimipramineThe risk or severity of hypotension can be increased when Trimipramine is combined with Cinnarizine.Approved
UrapidilThe risk or severity of hypotension can be increased when Urapidil is combined with Cinnarizine.Investigational
Valproic AcidThe metabolism of Cinnarizine can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Cinnarizine can be decreased when combined with Valsartan.Approved, Investigational
VemurafenibThe serum concentration of Cinnarizine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Cinnarizine can be decreased when combined with Venlafaxine.Approved
VerapamilThe risk or severity of hypotension can be increased when Verapamil is combined with Cinnarizine.Approved
VoriconazoleThe metabolism of Cinnarizine can be decreased when combined with Voriconazole.Approved, Investigational
WortmanninThe therapeutic efficacy of Wortmannin can be increased when used in combination with Cinnarizine.Experimental
ZafirlukastThe metabolism of Cinnarizine can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Cinnarizine can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe metabolism of Cinnarizine can be decreased when combined with Zucapsaicin.Approved, Investigational
ZuclopenthixolThe risk or severity of hypotension can be increased when Zuclopenthixol is combined with Cinnarizine.Approved, Investigational
Food Interactions
Not Available

References

Synthesis Reference

Janssen, P.A.J.; U.S. Patent 2,882,271; April 14, 1959; assigned to Laboratoria Pharmaceutica Dr. C. Janssen, Belgium.

General References
Not Available
External Links
KEGG Drug
D01295
PubChem Compound
2761
PubChem Substance
46506769
ChemSpider
1264793
BindingDB
50017657
ChEBI
31403
ChEMBL
CHEMBL43064
Therapeutic Targets Database
DAP000325
PharmGKB
PA164749342
Wikipedia
Cinnarizine
ATC Codes
N07CA52 — Cinnarizine, combinationsN07CA02 — Cinnarizine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentMethamphetamine-induced Psychosis1
Not AvailableUnknown StatusPreventionSimulator Sickness1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility750 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP5.77BIOBYTE (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.00172 mg/mLALOGPS
logP5.19ALOGPS
logP5.88ChemAxon
logS-5.3ALOGPS
pKa (Strongest Basic)8.4ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area6.48 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity119.86 m3·mol-1ChemAxon
Polarizability43.96 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9506
Blood Brain Barrier+0.977
Caco-2 permeable+0.6409
P-glycoprotein substrateSubstrate0.7107
P-glycoprotein inhibitor IInhibitor0.7461
P-glycoprotein inhibitor IINon-inhibitor0.8398
Renal organic cation transporterInhibitor0.7902
CYP450 2C9 substrateNon-substrate0.8549
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.7558
CYP450 1A2 substrateInhibitor0.7732
CYP450 2C9 inhibitorNon-inhibitor0.9488
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.9346
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5
Ames testNon AMES toxic0.9279
CarcinogenicityNon-carcinogens0.9496
BiodegradationNot ready biodegradable0.9968
Rat acute toxicity2.0618 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.5724
hERG inhibition (predictor II)Non-inhibitor0.524
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
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 diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Styrenes / N-alkylpiperazines / Aralkylamines / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Diphenylmethane / Styrene / Aralkylamine / N-alkylpiperazine / 1,4-diazinane / Piperazine / Tertiary amine / Tertiary aliphatic amine / Azacycle / Organoheterocyclic compound
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available

Targets

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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Paton DM, Webster DR: Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin Pharmacokinet. 1985 Nov-Dec;10(6):477-97. [PubMed:2866055]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1C
Uniprot ID
Q13936
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1C
Molecular Weight
248974.1 Da
References
  1. Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [PubMed:3530295]
  2. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity involved sa node cell action potential
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1D
Uniprot ID
Q01668
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1D
Molecular Weight
245138.75 Da
References
  1. Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [PubMed:3530295]
  2. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1F
Uniprot ID
O60840
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1F
Molecular Weight
220675.9 Da
References
  1. Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [PubMed:3530295]
  2. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1S
Uniprot ID
Q13698
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1S
Molecular Weight
212348.1 Da
References
  1. Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [PubMed:3530295]
  2. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Scaffold protein binding
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1G
Uniprot ID
O43497
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1G
Molecular Weight
262468.62 Da
References
  1. Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [PubMed:3530295]
  2. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Scaffold protein binding
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1H
Uniprot ID
O95180
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1H
Molecular Weight
259160.2 Da
References
  1. Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [PubMed:3530295]
  2. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1I
Uniprot ID
Q9P0X4
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1I
Molecular Weight
245100.8 Da
References
  1. Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [PubMed:3530295]
  2. Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [PubMed:1281221]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Other/unknown
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Brucke T, Wober C, Podreka I, Wober-Bingol C, Asenbaum S, Aull S, Wenger S, Ilieva D, Harasko-van der Meer C, Wessely P, et al.: D2 receptor blockade by flunarizine and cinnarizine explains extrapyramidal side effects. A SPECT study. J Cereb Blood Flow Metab. 1995 May;15(3):513-8. [PubMed:7714010]
  2. Kuzuhara S: [Drug-induced parkinsonism]. Nihon Rinsho. 1997 Jan;55(1):112-7. [PubMed:9014432]
  3. doi:10.1007/s00415-006-3004-8 [Link]
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.

Components:
References
  1. Nasu R, Matsuo H, Takanaga H, Ohtani H, Sawada Y: Quantitative prediction of catalepsy induced by amoxapine, cinnarizine and cyclophosphamide in mice. Biopharm Drug Dispos. 2000 May;21(4):129-38. [PubMed:11180191]
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...

Components:
References
  1. Nasu R, Matsuo H, Takanaga H, Ohtani H, Sawada Y: Quantitative prediction of catalepsy induced by amoxapine, cinnarizine and cyclophosphamide in mice. Biopharm Drug Dispos. 2000 May;21(4):129-38. [PubMed:11180191]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
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
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d 24-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
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on June 13, 2005 07:24 / Updated on June 02, 2018 09:48