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Identification
NameLevocabastine
Accession NumberDB01106  (APRD01069)
TypeSmall Molecule
GroupsApproved
DescriptionLevocabastine is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine was discovered at Janssen Pharmaceutica in 1979.
Structure
Thumb
Synonyms
Levocabastin
Levocabastina
Levocabastinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Livostin Eye DropsSolution / drops; Suspension0.5 mgOphthalmicNovartis Pharmaceuticals Canada Inc1995-12-312011-06-27Canada
Livostin Sus Nas 0.5mg/mlSpray; Suspension0.5 mgNasalJanssen Inc1993-12-31Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LivostinNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Levocabastine hydrochloride
79547-78-7
Thumb
  • InChI Key: OICFWWJHIMKBCD-VALQNVSPSA-N
  • Monoisotopic Mass: 456.1979841
  • Average Mass: 456.99
DBSALT001442
Categories
UNIIH68BP06S81
CAS number79516-68-0
WeightAverage: 420.528
Monoisotopic: 420.221306345
Chemical FormulaC26H29FN2O2
InChI KeyZCGOMHNNNFPNMX-KYTRFIICSA-N
InChI
InChI=1S/C26H29FN2O2/c1-19-17-29(16-15-26(19,24(30)31)21-5-3-2-4-6-21)23-11-13-25(18-28,14-12-23)20-7-9-22(27)10-8-20/h2-10,19,23H,11-17H2,1H3,(H,30,31)/t19-,23-,25-,26-/m1/s1
IUPAC Name
(3S,4R)-3-methyl-4-phenyl-1-[(1s,4s)-4-cyano-4-(4-fluorophenyl)cyclohexyl]piperidine-4-carboxylic acid
SMILES
C[C@@H]1CN(CC[C@]1(C(O)=O)C1=CC=CC=C1)[[email protected]]1CC[C@](CC1)(C#N)C1=CC=C(F)C=C1
Pharmacology
IndicationAs an ophthalmic for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis. Also used as a nasal spray for allergic rhinitis.
Structured Indications
PharmacodynamicsLevocabastine is a selective histamine H1-receptor antagonist exerting inhibitory effects on the release of chemical mediators from mast cells and on the chemotaxis of polymorphonuclear leukocytes and eosinophils. Both histamine and antigens induced conjunctivitis can be inhibited by levocabastine. Levocabastine can also reduce symptoms of allergic rhinitis by preventing an increase in vascular permeability of nasal mucosa.
Mechanism of actionLevocabastine is a potent, selective histamine H1-receptor antagonist. It works by competing with histamine for H1-receptor sites on effector cells. It thereby prevents, but does not reverse, responses mediated by histamine alone. Levocabastine does not block histamine release but, rather, prevents histamine binding and activity. Levocabastine also binds neurotensin 2 receptors and serves as a neurotensin agonist. This can induce some degree of analgesia.
TargetKindPharmacological actionActionsOrganismUniProt ID
Neurotensin receptor type 2Proteinyes
partial antagonist
HumanO95665 details
Histamine H1 receptorProteinyes
antagonist
HumanP35367 details
Related Articles
AbsorptionAfter instillation in the eye, levocabastine is systemically absorbed, albeit at low levels.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Mostly unchanged. 10 to 20% is metabolized to the acylglucuronide of levocabastine.

Route of eliminationNot Available
Half life36 hours (after oral administration)
ClearanceNot Available
ToxicityAdverse effects include visual disturbances, dry mouth, cough, nausea, eyelid edema and lacrimation.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,1,1,2 TetrafluoroethaneThe risk or severity of adverse effects can be increased when 1,1,1,2 Tetrafluoroethane is combined with Levocabastine.Investigational
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Levocabastine.Experimental, Illicit
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Levocabastine.Experimental, Illicit
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Levocabastine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Levocabastine.Experimental, Illicit
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Levocabastine.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Levocabastine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Levocabastine.Approved
adipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with Levocabastine.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Levocabastine.Approved, Investigational
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with Levocabastine.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Levocabastine.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Levocabastine.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Levocabastine.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Levocabastine.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Levocabastine.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Levocabastine.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Levocabastine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with Levocabastine.Experimental
AmphetamineAmphetamine may decrease the sedative activities of Levocabastine.Approved, Illicit
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Levocabastine.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with Levocabastine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Levocabastine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Azaperone is combined with Levocabastine.Vet Approved
AzelastineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Levocabastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Levocabastine.Approved
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Levocabastine.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Benperidol is combined with Levocabastine.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Levocabastine.Approved
BenzphetamineBenzphetamine may decrease the sedative activities of Levocabastine.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Levocabastine.Approved
Benzylpenicilloyl PolylysineLevocabastine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Levocabastine.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Brexpiprazole is combined with Levocabastine.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Levocabastine.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Levocabastine.Approved, Illicit
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Levocabastine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with Levocabastine.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Levocabastine.Approved, Investigational
BuprenorphineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Levocabastine.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Levocabastine.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Butacaine is combined with Levocabastine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with Levocabastine.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Butamben is combined with Levocabastine.Approved
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Levocabastine.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Levocabastine.Approved, Illicit, Vet Approved
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Levocabastine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with Levocabastine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Levocabastine.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Carisoprodol is combined with Levocabastine.Approved
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Levocabastine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Levocabastine.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Levocabastine.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Levocabastine.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Levocabastine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Levocabastine.Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Levocabastine.Illicit, Withdrawn
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Levocabastine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Levocabastine.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Levocabastine.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Levocabastine.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Levocabastine is combined with Citalopram.Approved
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Levocabastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Clidinium is combined with Levocabastine.Approved
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with Levocabastine.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with Levocabastine.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Levocabastine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Clonazepam is combined with Levocabastine.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Levocabastine.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Levocabastine.Approved, Illicit
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Levocabastine.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Levocabastine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Levocabastine.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Levocabastine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Levocabastine.Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Levocabastine.Approved
DantroleneThe risk or severity of adverse effects can be increased when Dantrolene is combined with Levocabastine.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Levocabastine.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Dapoxetine.Investigational
deramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with Levocabastine.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Levocabastine.Approved
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Levocabastine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Levocabastine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Detomidine is combined with Levocabastine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Levocabastine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Levocabastine.Approved, Vet Approved
DextroamphetamineDextroamphetamine may decrease the sedative activities of Levocabastine.Approved, Illicit
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Levocabastine.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Levocabastine.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Levocabastine.Approved
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Levocabastine.Approved, Illicit, Vet Approved
DiethylpropionDiethylpropion may decrease the sedative activities of Levocabastine.Approved, Illicit
DifenoxinThe risk or severity of adverse effects can be increased when Difenoxin is combined with Levocabastine.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Levocabastine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Levocabastine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Levocabastine.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Levocabastine.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Levocabastine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Levocabastine.Approved, Illicit
DoramectinThe risk or severity of adverse effects can be increased when Doramectin is combined with Levocabastine.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Levocabastine.Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Levocabastine.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Levocabastine.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Levocabastine.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Levocabastine.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Levocabastine.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Ecopipam is combined with Levocabastine.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Efavirenz is combined with Levocabastine.Approved, Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Levocabastine.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Entacapone is combined with Levocabastine.Approved, Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Levocabastine is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Levocabastine.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Levocabastine.Approved
EthanolLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Levocabastine.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with Levocabastine.Approved
EthotoinThe risk or severity of adverse effects can be increased when Ethotoin is combined with Levocabastine.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Levocabastine.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Levocabastine.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Levocabastine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with Levocabastine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with Levocabastine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with Levocabastine.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Levocabastine.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Levocabastine is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Levocabastine.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Ezogabine is combined with Levocabastine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Felbamate is combined with Levocabastine.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Levocabastine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Levocabastine.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with Levocabastine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Flibanserin is combined with Levocabastine.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Levocabastine.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Flunarizine is combined with Levocabastine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Levocabastine.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Levocabastine.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Levocabastine.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Levocabastine.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Levocabastine.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fluticasone Propionate is combined with Levocabastine.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Levocabastine.Approved, Investigational
FosphenytoinThe risk or severity of adverse effects can be increased when Fosphenytoin is combined with Levocabastine.Approved
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Levocabastine.Approved, Illicit
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Levocabastine.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Levocabastine.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Levocabastine.Approved, Illicit
GepironeThe risk or severity of adverse effects can be increased when Gepirone is combined with Levocabastine.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Levocabastine.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Levocabastine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Levocabastine.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Levocabastine.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Levocabastine.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Levocabastine.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Levocabastine.Approved
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Levocabastine.Approved, Investigational
HydrocodoneLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Levocabastine.Approved, Illicit
Hydroxyamphetamine hydrobromideHydroxyamphetamine hydrobromide may decrease the sedative activities of Levocabastine.Approved
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Iloperidone is combined with Levocabastine.Approved
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Levocabastine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Indalpine.Investigational, Withdrawn
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Levocabastine.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Levocabastine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Levocabastine.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Levocabastine.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Levocabastine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Levetiracetam is combined with Levocabastine.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Levocetirizine is combined with Levocabastine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Levodopa is combined with Levocabastine.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Levocabastine.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Levocabastine is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Levocabastine.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Levocabastine.Approved, Vet Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Levocabastine.Approved, Investigational
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Levocabastine.Approved
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Levocabastine.Illicit
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Levocabastine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Levocabastine.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Levocabastine.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Lu AA21004 is combined with Levocabastine.Investigational
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Levocabastine.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Levocabastine.Approved
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Levocabastine.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Medetomidine is combined with Levocabastine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Levocabastine.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with Levocabastine.Approved
MephedroneMephedrone may decrease the sedative activities of Levocabastine.Investigational
MephentermineMephentermine may decrease the sedative activities of Levocabastine.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Levocabastine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Levocabastine.Approved, Illicit
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Levocabastine.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Metaxalone is combined with Levocabastine.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Levocabastine.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Levocabastine.Approved, Illicit
MethamphetamineMethamphetamine may decrease the sedative activities of Levocabastine.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Levocabastine.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Levocabastine.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Methocarbamol is combined with Levocabastine.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Levocabastine.Approved
MethotrimeprazineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Levocabastine.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Methsuximide is combined with Levocabastine.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Levocabastine.Approved
MetyrosineLevocabastine may increase the sedative activities of Metyrosine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Levocabastine.Approved, Illicit
MilnacipranThe risk or severity of adverse effects can be increased when Levocabastine is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved, Investigational
MirtazapineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MMDAMMDA may decrease the sedative activities of Levocabastine.Experimental, Illicit
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Levocabastine.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Levocabastine.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Levocabastine.Approved
NefazodoneThe risk or severity of adverse effects can be increased when Levocabastine is combined with Nefazodone.Approved, Withdrawn
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Levocabastine.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Levocabastine.Approved, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Levocabastine.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Levocabastine.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Levocabastine.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Levocabastine.Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Levocabastine.Approved
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Levocabastine.Approved, Illicit
OrphenadrineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Levocabastine.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Levocabastine.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Oxetacaine is combined with Levocabastine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Levocabastine.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Levocabastine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Levocabastine.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Levocabastine.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Levocabastine.Approved
ParaldehydeLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Paroxetine.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Levocabastine.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Levocabastine.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved
PerazineThe risk or severity of adverse effects can be increased when Perazine is combined with Levocabastine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with Levocabastine.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Levocabastine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Levocabastine.Approved
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Levocabastine.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Levocabastine.Approved
PhenterminePhentermine may decrease the sedative activities of Levocabastine.Approved, Illicit
PhenytoinThe risk or severity of adverse effects can be increased when Phenytoin is combined with Levocabastine.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Levocabastine.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Levocabastine.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Pipotiazine is combined with Levocabastine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Piritramide is combined with Levocabastine.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Pizotifen is combined with Levocabastine.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Pomalidomide is combined with Levocabastine.Approved
PramipexoleLevocabastine may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with Levocabastine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Levocabastine.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Levocabastine.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Pregnanolone is combined with Levocabastine.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Levocabastine.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Levocabastine.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Levocabastine.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Levocabastine.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Levocabastine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Levocabastine.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Levocabastine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Levocabastine.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with Levocabastine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Levocabastine.Approved
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with Levocabastine.Investigational
PseudoephedrinePseudoephedrine may decrease the sedative activities of Levocabastine.Approved
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Levocabastine.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Levocabastine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Raclopride is combined with Levocabastine.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Ramelteon is combined with Levocabastine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Levocabastine.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Levocabastine.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Levocabastine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Levocabastine.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Ritanserin is combined with Levocabastine.Investigational
RitobegronRitobegron may decrease the sedative activities of Levocabastine.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Romifidine is combined with Levocabastine.Vet Approved
RopiniroleLevocabastine may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Levocabastine.Approved
RotigotineLevocabastine may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Levocabastine.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Levocabastine.Experimental
Sage 547The risk or severity of adverse effects can be increased when Sage 547 is combined with Levocabastine.Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Levocabastine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Levocabastine.Approved, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Levocabastine.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Levocabastine.Approved, Vet Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved
StiripentolThe risk or severity of adverse effects can be increased when Stiripentol is combined with Levocabastine.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Levocabastine.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Levocabastine.Approved
SuvorexantLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Tandospirone is combined with Levocabastine.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Levocabastine.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Levocabastine.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Levocabastine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with Levocabastine.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Levocabastine.Investigational
ThalidomideLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Levocabastine.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Levocabastine.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Levocabastine.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Levocabastine.Approved
TiagabineThe risk or severity of adverse effects can be increased when Tiagabine is combined with Levocabastine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Tiapride is combined with Levocabastine.Investigational
TiletamineThe risk or severity of adverse effects can be increased when Tiletamine is combined with Levocabastine.Vet Approved
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Levocabastine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with Levocabastine.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Levocabastine.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Levocabastine.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Levocabastine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Levocabastine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Levocabastine.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Levocabastine.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Levocabastine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Levocabastine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Levocabastine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Levocabastine.Approved
Uc1010The risk or severity of adverse effects can be increased when Uc1010 is combined with Levocabastine.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Levocabastine.Approved, Investigational
VenlafaxineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Venlafaxine.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Vigabatrin is combined with Levocabastine.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Levocabastine.Approved
XylazineThe risk or severity of adverse effects can be increased when Xylazine is combined with Levocabastine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Levocabastine.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Ziconotide is combined with Levocabastine.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Zimelidine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Levocabastine.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Zolazepam is combined with Levocabastine.Vet Approved
ZolpidemLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with Levocabastine.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Levocabastine.Approved
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with Levocabastine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Levocabastine.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesR01AC02S01GX02
AHFS Codes
  • 52:02.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9811
Blood Brain Barrier+0.8388
Caco-2 permeable+0.5747
P-glycoprotein substrateSubstrate0.7325
P-glycoprotein inhibitor IInhibitor0.5
P-glycoprotein inhibitor IINon-inhibitor0.5682
Renal organic cation transporterNon-inhibitor0.5526
CYP450 2C9 substrateNon-substrate0.7708
CYP450 2D6 substrateNon-substrate0.6679
CYP450 3A4 substrateSubstrate0.5153
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9046
Ames testNon AMES toxic0.7503
CarcinogenicityNon-carcinogens0.9196
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.9608 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9404
hERG inhibition (predictor II)Inhibitor0.625
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Solution / drops; suspensionOphthalmic0.5 mg
Spray; suspensionNasal0.5 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility>0.5 mg/mLNot Available
logP5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00347 mg/mLALOGPS
logP4.56ALOGPS
logP2.5ChemAxon
logS-5.1ALOGPS
pKa (Strongest Acidic)3.71ChemAxon
pKa (Strongest Basic)10.32ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area64.33 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity118.48 m3·mol-1ChemAxon
Polarizability45.58 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPiperidines
Sub ClassPhenylpiperidines
Direct ParentPhenylpiperidines
Alternative Parents
Substituents
  • Phenylpiperidine
  • Piperidinecarboxylic acid
  • Cyclohexylamine
  • Fluorobenzene
  • Aralkylamine
  • Halobenzene
  • Aryl fluoride
  • Aryl halide
  • Monocyclic benzene moiety
  • Benzenoid
  • Amino acid or derivatives
  • Amino acid
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid derivative
  • Carboxylic acid
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carbonitrile
  • Nitrile
  • Organooxygen compound
  • Hydrocarbon derivative
  • Organic nitrogen compound
  • Amine
  • Carbonyl group
  • Organic oxygen compound
  • Cyanide
  • Organic oxide
  • Organohalogen compound
  • Organofluoride
  • Organonitrogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
partial antagonist
General Function:
G-protein coupled receptor activity
Specific Function:
Receptor for the tridecapeptide neurotensin. It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name:
NTSR2
Uniprot ID:
O95665
Molecular Weight:
45384.635 Da
References
  1. Richard F, Barroso S, Martinez J, Labbe-Jullie C, Kitabgi P: Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2. Mol Pharmacol. 2001 Dec;60(6):1392-8. [PubMed:11723247 ]
  2. Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D: Molecular cloning of a levocabastine-sensitive neurotensin binding site. FEBS Lett. 1996 May 20;386(2-3):91-4. [PubMed:8647296 ]
  3. Botto JM, Guillemare E, Vincent JP, Mazella J: Effects of SR 48692 on neurotensin-induced calcium-activated chloride currents in the Xenopus oocyte expression system: agonist-like activity on the levocabastine-sensitive neurotensin receptor and absence of antagonist effect on the levocabastine insensitive neurotensin receptor. Neurosci Lett. 1997 Feb 28;223(3):193-6. [PubMed:9080465 ]
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 catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
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. Sugimoto Y, Iba Y, Ishizawa K, Suzuki G, Kamei C: Effects of levocabastine on lipid mediator release from guinea pig lung fragments. Acta Med Okayama. 1999 Dec;53(6):271-4. [PubMed:10631382 ]
  3. Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D: Molecular cloning of a levocabastine-sensitive neurotensin binding site. FEBS Lett. 1996 May 20;386(2-3):91-4. [PubMed:8647296 ]
  4. Yamada M, Yamada M, Lombet A, Forgez P, Rostene W: Distinct functional characteristics of levocabastine sensitive rat neurotensin NT2 receptor expressed in Chinese hamster ovary cells. Life Sci. 1998;62(23):PL 375-80. [PubMed:9627096 ]
  5. Betancur C, Canton M, Burgos A, Labeeuw B, Gully D, Rostene W, Pelaprat D: Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain. Eur J Pharmacol. 1998 Feb 5;343(1):67-77. [PubMed:9551716 ]
  6. Akiyoshi M, Shigeoka T, Torii S, Maki E, Enomoto S, Takahashi H, Hirano F: [Pharmacological and clinical properties of levocabastine hydrochloride (eye drop and nasal spray), a selective H1 antagonist]. Nihon Yakurigaku Zasshi. 2002 Mar;119(3):175-84. [PubMed:11915520 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23