Levocabastine - DrugBank

ID Pharmacology Interactions References Trials Economics Properties Spectra Taxonomy

Targets (2)

Targets (2)Biointeractions (1)

Identification

Name

Levocabastine

Accession Number

DB01106 (APRD01069)

Type

Small Molecule

Groups

Approved

Description

Levocabastine is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine was discovered at Janssen Pharmaceutica in 1979.

Structure

MOL SDF PDB SMILES InChI

Synonyms

Levocabastin

Levocabastina

Levocabastinum

External IDs

Not Available

Product Ingredients

Ingredient	UNII	CAS	InChI Key	Details
Levocabastine hydrochloride	124XMA6YEI	79547-78-7	OICFWWJHIMKBCD-VALQNVSPSA-N	Details

Approved Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Livostin Eye Drops	Solution / drops; Suspension	0.5 mg	Ophthalmic	Novartis	1995-12-31	2011-06-27	Canada
Livostin Sus Nas 0.5mg/ml	Spray; Suspension	0.5 mg	Nasal	Janssen Pharmaceuticals	1993-12-31	Not applicable	Canada

Approved Generic Prescription Products

Not Available

Approved Over the Counter Products

Not Available

Unapproved/Other Products

Not Available

International Brands

Name	Company
Livostin	Not Available

Brand mixtures

Not Available

Categories

UNII

H68BP06S81

CAS number

79516-68-0

Weight

Average: 420.528
Monoisotopic: 420.221306345

Chemical Formula

C₂₆H₂₉FN₂O₂

InChI Key

ZCGOMHNNNFPNMX-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[[email protected]@H]1CN(CC[[email protected]]1(C(O)=O)C1=CC=CC=C1)[[email protected]]1CC[[email protected]](CC1)(C#N)C1=CC=C(F)C=C1

Pharmacology

Indication

As 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

Allergic Rhinitis (AR)

Pharmacodynamics

Levocabastine 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 action

Levocabastine 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.

Target	Kind	Pharmacological action	Actions	Organism	UniProt ID
Histamine H1 receptor	Protein	yes	antagonist	Human	P35367	details
Neurotensin receptor type 2	Protein	yes	partial antagonist	Human	O95665	details

Absorption

After instillation in the eye, levocabastine is systemically absorbed, albeit at low levels.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

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

Route of elimination

Not Available

Half life

36 hours (after oral administration)

Clearance

Not Available

Toxicity

Adverse effects include visual disturbances, dry mouth, cough, nausea, eyelid edema and lacrimation.

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

Drug	Interaction	Drug group
2,5-Dimethoxy-4-ethylamphetamine	2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Levocabastine.	Experimental, Illicit
3,4-Methylenedioxyamphetamine	3,4-Methylenedioxyamphetamine may decrease the sedative activities of Levocabastine.	Experimental, Illicit
3,4-Methylenedioxymethamphetamine	3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Levocabastine.	Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine	4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Levocabastine.	Experimental, Illicit
7-Nitroindazole	The risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Levocabastine.	Experimental
Acepromazine	The risk or severity of adverse effects can be increased when Acepromazine is combined with Levocabastine.	Approved, Vet Approved
Aceprometazine	The risk or severity of adverse effects can be increased when Aceprometazine is combined with Levocabastine.	Approved
Adipiplon	The risk or severity of adverse effects can be increased when adipiplon is combined with Levocabastine.	Investigational
Agomelatine	The risk or severity of adverse effects can be increased when Agomelatine is combined with Levocabastine.	Approved, Investigational
Alfaxalone	The risk or severity of adverse effects can be increased when Alfaxalone is combined with Levocabastine.	Vet Approved
Alfentanil	The risk or severity of adverse effects can be increased when Alfentanil is combined with Levocabastine.	Approved, Illicit
Allopregnanolone	The risk or severity of adverse effects can be increased when Sage 547 is combined with Levocabastine.	Investigational
Alphacetylmethadol	The risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Levocabastine.	Experimental, Illicit
Alprazolam	The risk or severity of adverse effects can be increased when Alprazolam is combined with Levocabastine.	Approved, Illicit, Investigational
Amisulpride	The risk or severity of adverse effects can be increased when Amisulpride is combined with Levocabastine.	Approved, Investigational
Amitriptyline	The risk or severity of adverse effects can be increased when Amitriptyline is combined with Levocabastine.	Approved
Amobarbital	The risk or severity of adverse effects can be increased when Amobarbital is combined with Levocabastine.	Approved, Illicit
Amoxapine	The risk or severity of adverse effects can be increased when Amoxapine is combined with Levocabastine.	Approved
Amperozide	The risk or severity of adverse effects can be increased when Amperozide is combined with Levocabastine.	Experimental
Amphetamine	Amphetamine may decrease the sedative activities of Levocabastine.	Approved, Illicit
Aripiprazole	The risk or severity of adverse effects can be increased when Aripiprazole is combined with Levocabastine.	Approved, Investigational
Articaine	The risk or severity of adverse effects can be increased when Articaine is combined with Levocabastine.	Approved
Asenapine	The risk or severity of adverse effects can be increased when Asenapine is combined with Levocabastine.	Approved
Azaperone	The risk or severity of adverse effects can be increased when Azaperone is combined with Levocabastine.	Vet Approved
Azelastine	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.	Approved
Azelastine	The risk or severity of adverse effects can be increased when Azelastine is combined with Levocabastine.	Approved
Baclofen	The risk or severity of adverse effects can be increased when Baclofen is combined with Levocabastine.	Approved
Barbital	The risk or severity of adverse effects can be increased when Barbital is combined with Levocabastine.	Illicit
Benperidol	The risk or severity of adverse effects can be increased when Benperidol is combined with Levocabastine.	Investigational
Benzocaine	The risk or severity of adverse effects can be increased when Benzocaine is combined with Levocabastine.	Approved
Benzphetamine	Benzphetamine may decrease the sedative activities of Levocabastine.	Approved, Illicit
Benzyl alcohol	The risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Levocabastine.	Approved
Benzylpenicilloyl Polylysine	Levocabastine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.	Approved
Betahistine	The therapeutic efficacy of Betahistine can be decreased when used in combination with Levocabastine.	Approved
Brexpiprazole	The risk or severity of adverse effects can be increased when Brexpiprazole is combined with Levocabastine.	Approved
Brimonidine	The risk or severity of adverse effects can be increased when Brimonidine is combined with Levocabastine.	Approved
Brimonidine	Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved
Bromazepam	The risk or severity of adverse effects can be increased when Bromazepam is combined with Levocabastine.	Approved, Illicit
Brompheniramine	The risk or severity of adverse effects can be increased when Brompheniramine is combined with Levocabastine.	Approved
Brotizolam	The risk or severity of adverse effects can be increased when Brotizolam is combined with Levocabastine.	Approved, Withdrawn
Bupivacaine	The risk or severity of adverse effects can be increased when Bupivacaine is combined with Levocabastine.	Approved, Investigational
Buprenorphine	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.	Approved, Illicit, Investigational, Vet Approved
Buspirone	The risk or severity of adverse effects can be increased when Buspirone is combined with Levocabastine.	Approved, Investigational
Butabarbital	The risk or severity of adverse effects can be increased when Butabarbital is combined with Levocabastine.	Approved, Illicit
Butacaine	The risk or severity of adverse effects can be increased when Butacaine is combined with Levocabastine.	Vet Approved
Butalbital	The risk or severity of adverse effects can be increased when Butalbital is combined with Levocabastine.	Approved, Illicit
Butamben	The risk or severity of adverse effects can be increased when Butamben is combined with Levocabastine.	Approved
Butethal	The risk or severity of adverse effects can be increased when Butethal is combined with Levocabastine.	Approved, Illicit
Butorphanol	The risk or severity of adverse effects can be increased when Butorphanol is combined with Levocabastine.	Approved, Illicit, Vet Approved
Carbamazepine	The risk or severity of adverse effects can be increased when Carbamazepine is combined with Levocabastine.	Approved, Investigational
Carbinoxamine	The risk or severity of adverse effects can be increased when Carbinoxamine is combined with Levocabastine.	Approved
Carfentanil	The risk or severity of adverse effects can be increased when Carfentanil is combined with Levocabastine.	Illicit, Vet Approved
Carisoprodol	The risk or severity of adverse effects can be increased when Carisoprodol is combined with Levocabastine.	Approved
Cetirizine	The risk or severity of adverse effects can be increased when Cetirizine is combined with Levocabastine.	Approved
Chloral hydrate	The risk or severity of adverse effects can be increased when Chloral hydrate is combined with Levocabastine.	Approved, Illicit, Vet Approved
Chlordiazepoxide	The risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Levocabastine.	Approved, Illicit
Chlormezanone	The risk or severity of adverse effects can be increased when Chlormezanone is combined with Levocabastine.	Approved, Withdrawn
Chloroprocaine	The risk or severity of adverse effects can be increased when Chloroprocaine is combined with Levocabastine.	Approved
Chlorphenamine	The risk or severity of adverse effects can be increased when Chlorphenamine is combined with Levocabastine.	Approved
Chlorphentermine	Chlorphentermine may decrease the sedative activities of Levocabastine.	Illicit, Withdrawn
Chlorpromazine	The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Levocabastine.	Approved, Vet Approved
Chlorprothixene	The risk or severity of adverse effects can be increased when Chlorprothixene is combined with Levocabastine.	Approved, Withdrawn
Chlorzoxazone	The risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Levocabastine.	Approved
Cinchocaine	The risk or severity of adverse effects can be increased when Cinchocaine is combined with Levocabastine.	Approved, Vet Approved
Citalopram	The risk or severity of adverse effects can be increased when Levocabastine is combined with Citalopram.	Approved
Clemastine	The risk or severity of adverse effects can be increased when Clemastine is combined with Levocabastine.	Approved
Clidinium	The risk or severity of adverse effects can be increased when Clidinium is combined with Levocabastine.	Approved
Clobazam	The risk or severity of adverse effects can be increased when Clobazam is combined with Levocabastine.	Approved, Illicit
clomethiazole	The risk or severity of adverse effects can be increased when clomethiazole is combined with Levocabastine.	Investigational
Clomipramine	The risk or severity of adverse effects can be increased when Clomipramine is combined with Levocabastine.	Approved, Vet Approved
Clonazepam	The risk or severity of adverse effects can be increased when Clonazepam is combined with Levocabastine.	Approved, Illicit
Clonidine	The risk or severity of adverse effects can be increased when Clonidine is combined with Levocabastine.	Approved
Clorazepate	The risk or severity of adverse effects can be increased when Clorazepate is combined with Levocabastine.	Approved, Illicit
Clozapine	The risk or severity of adverse effects can be increased when Clozapine is combined with Levocabastine.	Approved
Cocaine	The risk or severity of adverse effects can be increased when Cocaine is combined with Levocabastine.	Approved, Illicit
Codeine	The risk or severity of adverse effects can be increased when Codeine is combined with Levocabastine.	Approved, Illicit
Cyclizine	The risk or severity of adverse effects can be increased when Cyclizine is combined with Levocabastine.	Approved
Cyclobenzaprine	The risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Levocabastine.	Approved
Cyproheptadine	The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Levocabastine.	Approved
Dantrolene	The risk or severity of adverse effects can be increased when Dantrolene is combined with Levocabastine.	Approved
Dapiprazole	The risk or severity of adverse effects can be increased when Dapiprazole is combined with Levocabastine.	Approved
Dapoxetine	The risk or severity of adverse effects can be increased when Levocabastine is combined with Dapoxetine.	Investigational
Deramciclane	The risk or severity of adverse effects can be increased when deramciclane is combined with Levocabastine.	Investigational
Desflurane	The risk or severity of adverse effects can be increased when Desflurane is combined with Levocabastine.	Approved
Desipramine	The risk or severity of adverse effects can be increased when Desipramine is combined with Levocabastine.	Approved
Desloratadine	The risk or severity of adverse effects can be increased when Desloratadine is combined with Levocabastine.	Approved, Investigational
Desvenlafaxine	The risk or severity of adverse effects can be increased when Levocabastine is combined with Desvenlafaxine.	Approved
Detomidine	The risk or severity of adverse effects can be increased when Detomidine is combined with Levocabastine.	Vet Approved
Dexbrompheniramine	The risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Levocabastine.	Approved
Dexmedetomidine	The risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Levocabastine.	Approved, Vet Approved
Dextroamphetamine	Dextroamphetamine may decrease the sedative activities of Levocabastine.	Approved, Illicit
Dextromoramide	The risk or severity of adverse effects can be increased when Dextromoramide is combined with Levocabastine.	Experimental, Illicit
Dextropropoxyphene	The risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Levocabastine.	Approved, Illicit, Withdrawn
Dezocine	The risk or severity of adverse effects can be increased when Dezocine is combined with Levocabastine.	Approved
Diazepam	The risk or severity of adverse effects can be increased when Diazepam is combined with Levocabastine.	Approved, Illicit, Vet Approved
Diethylpropion	Diethylpropion may decrease the sedative activities of Levocabastine.	Approved, Illicit
Difenoxin	The risk or severity of adverse effects can be increased when Difenoxin is combined with Levocabastine.	Approved, Illicit
Dihydrocodeine	The risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Levocabastine.	Approved, Illicit
Dihydroetorphine	The risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Levocabastine.	Experimental, Illicit
Dihydromorphine	The risk or severity of adverse effects can be increased when Dihydromorphine is combined with Levocabastine.	Experimental, Illicit
Dimenhydrinate	The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Levocabastine.	Approved
Diphenhydramine	The risk or severity of adverse effects can be increased when Diphenhydramine is combined with Levocabastine.	Approved
Diphenoxylate	The risk or severity of adverse effects can be increased when Diphenoxylate is combined with Levocabastine.	Approved, Illicit
Doramectin	The risk or severity of adverse effects can be increased when Doramectin is combined with Levocabastine.	Vet Approved
Doxepin	The risk or severity of adverse effects can be increased when Doxepin is combined with Levocabastine.	Approved
Doxylamine	Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved, Vet Approved
DPDPE	The risk or severity of adverse effects can be increased when DPDPE is combined with Levocabastine.	Investigational
Dronabinol	Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved, Illicit
Droperidol	Droperidol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved, Vet Approved
Drotebanol	The risk or severity of adverse effects can be increased when Drotebanol is combined with Levocabastine.	Experimental, Illicit
Duloxetine	The risk or severity of adverse effects can be increased when Levocabastine is combined with Duloxetine.	Approved
Dyclonine	The risk or severity of adverse effects can be increased when Dyclonine is combined with Levocabastine.	Approved
Ecgonine	The risk or severity of adverse effects can be increased when Ecgonine is combined with Levocabastine.	Experimental, Illicit
Ecopipam	The risk or severity of adverse effects can be increased when Ecopipam is combined with Levocabastine.	Investigational
Efavirenz	The risk or severity of adverse effects can be increased when Efavirenz is combined with Levocabastine.	Approved, Investigational
Eltanolone	The risk or severity of adverse effects can be increased when Pregnanolone is combined with Levocabastine.	Investigational
Enflurane	The risk or severity of adverse effects can be increased when Enflurane is combined with Levocabastine.	Approved, Vet Approved
Entacapone	The risk or severity of adverse effects can be increased when Entacapone is combined with Levocabastine.	Approved, Investigational
Escitalopram	The risk or severity of adverse effects can be increased when Levocabastine is combined with Escitalopram.	Approved, Investigational
Estazolam	The risk or severity of adverse effects can be increased when Estazolam is combined with Levocabastine.	Approved, Illicit
Eszopiclone	The risk or severity of adverse effects can be increased when Eszopiclone is combined with Levocabastine.	Approved
Ethanol	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.	Approved
Ethchlorvynol	The risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Levocabastine.	Approved, Illicit, Withdrawn
Ethosuximide	The risk or severity of adverse effects can be increased when Ethosuximide is combined with Levocabastine.	Approved
Ethotoin	The risk or severity of adverse effects can be increased when Ethotoin is combined with Levocabastine.	Approved
Ethyl carbamate	The risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Levocabastine.	Withdrawn
Ethyl loflazepate	The risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Levocabastine.	Approved, Illicit
Ethylmorphine	The risk or severity of adverse effects can be increased when Ethylmorphine is combined with Levocabastine.	Approved, Illicit
Etidocaine	The risk or severity of adverse effects can be increased when Etidocaine is combined with Levocabastine.	Approved
Etifoxine	The risk or severity of adverse effects can be increased when Etifoxine is combined with Levocabastine.	Withdrawn
Etizolam	The risk or severity of adverse effects can be increased when Etizolam is combined with Levocabastine.	Approved
Etomidate	The risk or severity of adverse effects can be increased when Etomidate is combined with Levocabastine.	Approved
Etoperidone	The risk or severity of adverse effects can be increased when Levocabastine is combined with Etoperidone.	Approved
Etorphine	The risk or severity of adverse effects can be increased when Etorphine is combined with Levocabastine.	Illicit, Vet Approved
Ezogabine	The risk or severity of adverse effects can be increased when Ezogabine is combined with Levocabastine.	Approved
Felbamate	The risk or severity of adverse effects can be increased when Felbamate is combined with Levocabastine.	Approved
Fencamfamine	The risk or severity of adverse effects can be increased when Fencamfamine is combined with Levocabastine.	Approved, Illicit, Withdrawn
Fentanyl	The risk or severity of adverse effects can be increased when Fentanyl is combined with Levocabastine.	Approved, Illicit, Investigational, Vet Approved
Fexofenadine	The risk or severity of adverse effects can be increased when Fexofenadine is combined with Levocabastine.	Approved
Flibanserin	The risk or severity of adverse effects can be increased when Flibanserin is combined with Levocabastine.	Approved
Fludiazepam	The risk or severity of adverse effects can be increased when Fludiazepam is combined with Levocabastine.	Approved, Illicit
Flunarizine	The risk or severity of adverse effects can be increased when Flunarizine is combined with Levocabastine.	Approved
Flunitrazepam	The risk or severity of adverse effects can be increased when Flunitrazepam is combined with Levocabastine.	Approved, Illicit
Fluoxetine	The risk or severity of adverse effects can be increased when Levocabastine is combined with Fluoxetine.	Approved, Vet Approved
Flupentixol	The risk or severity of adverse effects can be increased when Flupentixol is combined with Levocabastine.	Approved, Withdrawn
Fluphenazine	The risk or severity of adverse effects can be increased when Fluphenazine is combined with Levocabastine.	Approved
Flurazepam	The risk or severity of adverse effects can be increased when Flurazepam is combined with Levocabastine.	Approved, Illicit
Fluspirilene	The risk or severity of adverse effects can be increased when Fluspirilene is combined with Levocabastine.	Approved
Fluticasone propionate	The risk or severity of adverse effects can be increased when Fluticasone Propionate is combined with Levocabastine.	Approved
Fluvoxamine	The risk or severity of adverse effects can be increased when Fluvoxamine is combined with Levocabastine.	Approved, Investigational
Fosphenytoin	The risk or severity of adverse effects can be increased when Fosphenytoin is combined with Levocabastine.	Approved
Fospropofol	The risk or severity of adverse effects can be increased when Fospropofol is combined with Levocabastine.	Approved, Illicit
Gabapentin	The risk or severity of adverse effects can be increased when Gabapentin is combined with Levocabastine.	Approved, Investigational
Gabapentin Enacarbil	The risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Levocabastine.	Approved
Gamma Hydroxybutyric Acid	The risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Levocabastine.	Approved, Illicit
Gepirone	The risk or severity of adverse effects can be increased when Gepirone is combined with Levocabastine.	Investigational
Glutethimide	The risk or severity of adverse effects can be increased when Glutethimide is combined with Levocabastine.	Approved, Illicit
Guanfacine	The risk or severity of adverse effects can be increased when Guanfacine is combined with Levocabastine.	Approved, Investigational
Halazepam	The risk or severity of adverse effects can be increased when Halazepam is combined with Levocabastine.	Approved, Illicit, Withdrawn
Haloperidol	The risk or severity of adverse effects can be increased when Haloperidol is combined with Levocabastine.	Approved
Halothane	The risk or severity of adverse effects can be increased when Halothane is combined with Levocabastine.	Approved, Vet Approved
Heroin	The risk or severity of adverse effects can be increased when Heroin is combined with Levocabastine.	Approved, Illicit
Hexobarbital	The risk or severity of adverse effects can be increased when Hexobarbital is combined with Levocabastine.	Approved
Hyaluronidase	The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Levocabastine.	Approved, Investigational
Hydrocodone	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.	Approved, Illicit
Hydromorphone	The risk or severity of adverse effects can be increased when Hydromorphone is combined with Levocabastine.	Approved, Illicit
Hydroxyamphetamine	Hydroxyamphetamine hydrobromide may decrease the sedative activities of Levocabastine.	Approved
Hydroxyzine	Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved
Iloperidone	The risk or severity of adverse effects can be increased when Iloperidone is combined with Levocabastine.	Approved
Imipramine	The risk or severity of adverse effects can be increased when Imipramine is combined with Levocabastine.	Approved
Indalpine	The risk or severity of adverse effects can be increased when Levocabastine is combined with Indalpine.	Investigational, Withdrawn
Isoflurane	The risk or severity of adverse effects can be increased when Isoflurane is combined with Levocabastine.	Approved, Vet Approved
Ketamine	The risk or severity of adverse effects can be increased when Ketamine is combined with Levocabastine.	Approved, Vet Approved
Ketazolam	The risk or severity of adverse effects can be increased when Ketazolam is combined with Levocabastine.	Approved
Ketobemidone	The risk or severity of adverse effects can be increased when Ketobemidone is combined with Levocabastine.	Approved
Lamotrigine	The risk or severity of adverse effects can be increased when Lamotrigine is combined with Levocabastine.	Approved, Investigational
Levetiracetam	The risk or severity of adverse effects can be increased when Levetiracetam is combined with Levocabastine.	Approved, Investigational
Levobupivacaine	The risk or severity of adverse effects can be increased when Levobupivacaine is combined with Levocabastine.	Approved
Levocetirizine	The risk or severity of adverse effects can be increased when Levocetirizine is combined with Levocabastine.	Approved
Levodopa	The risk or severity of adverse effects can be increased when Levodopa is combined with Levocabastine.	Approved
Levomethadyl Acetate	The risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Levocabastine.	Approved
Levomilnacipran	The risk or severity of adverse effects can be increased when Levocabastine is combined with Levomilnacipran.	Approved
Levorphanol	The risk or severity of adverse effects can be increased when Levorphanol is combined with Levocabastine.	Approved
Lidocaine	The risk or severity of adverse effects can be increased when Lidocaine is combined with Levocabastine.	Approved, Vet Approved
Lisdexamfetamine	Lisdexamfetamine may decrease the sedative activities of Levocabastine.	Approved, Investigational
Lithium	The risk or severity of adverse effects can be increased when Lithium is combined with Levocabastine.	Approved
Lofentanil	The risk or severity of adverse effects can be increased when Lofentanil is combined with Levocabastine.	Illicit
Loratadine	The risk or severity of adverse effects can be increased when Loratadine is combined with Levocabastine.	Approved
Lorazepam	The risk or severity of adverse effects can be increased when Lorazepam is combined with Levocabastine.	Approved
Loxapine	The risk or severity of adverse effects can be increased when Loxapine is combined with Levocabastine.	Approved
Lurasidone	The risk or severity of adverse effects can be increased when Lurasidone is combined with Levocabastine.	Approved
Magnesium Sulfate	Magnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved, Vet Approved
Maprotiline	The risk or severity of adverse effects can be increased when Maprotiline is combined with Levocabastine.	Approved
Meclizine	The risk or severity of adverse effects can be increased when Meclizine is combined with Levocabastine.	Approved
Medetomidine	The risk or severity of adverse effects can be increased when Medetomidine is combined with Levocabastine.	Vet Approved
Melatonin	The risk or severity of adverse effects can be increased when Melatonin is combined with Levocabastine.	Approved, Nutraceutical, Vet Approved
Melperone	The risk or severity of adverse effects can be increased when Melperone is combined with Levocabastine.	Approved
Mephedrone	Mephedrone may decrease the sedative activities of Levocabastine.	Investigational
Mephentermine	Mephentermine may decrease the sedative activities of Levocabastine.	Approved
Mepivacaine	The risk or severity of adverse effects can be increased when Mepivacaine is combined with Levocabastine.	Approved, Vet Approved
Meprobamate	The risk or severity of adverse effects can be increased when Meprobamate is combined with Levocabastine.	Approved, Illicit
Mesoridazine	The risk or severity of adverse effects can be increased when Mesoridazine is combined with Levocabastine.	Approved
Metaxalone	The risk or severity of adverse effects can be increased when Metaxalone is combined with Levocabastine.	Approved
Methadone	The risk or severity of adverse effects can be increased when Methadone is combined with Levocabastine.	Approved
Methadyl Acetate	The risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Levocabastine.	Approved, Illicit
Methamphetamine	Methamphetamine may decrease the sedative activities of Levocabastine.	Approved, Illicit
Methapyrilene	The risk or severity of adverse effects can be increased when Methapyrilene is combined with Levocabastine.	Withdrawn
Methaqualone	The risk or severity of adverse effects can be increased when Methaqualone is combined with Levocabastine.	Illicit, Withdrawn
Methocarbamol	The risk or severity of adverse effects can be increased when Methocarbamol is combined with Levocabastine.	Approved, Vet Approved
Methohexital	The risk or severity of adverse effects can be increased when Methohexital is combined with Levocabastine.	Approved
Methotrimeprazine	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.	Approved
Methoxyflurane	The risk or severity of adverse effects can be increased when Methoxyflurane is combined with Levocabastine.	Approved, Vet Approved
Methsuximide	The risk or severity of adverse effects can be increased when Methsuximide is combined with Levocabastine.	Approved
Methylecgonine	The risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Levocabastine.	Experimental
Methylphenobarbital	The risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Levocabastine.	Approved
Metyrosine	Levocabastine may increase the sedative activities of Metyrosine.	Approved
Midazolam	The risk or severity of adverse effects can be increased when Midazolam is combined with Levocabastine.	Approved, Illicit
Milnacipran	The risk or severity of adverse effects can be increased when Levocabastine is combined with Milnacipran.	Approved
Minocycline	Minocycline may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved, Investigational
Mirtazapine	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.	Approved
MMDA	MMDA may decrease the sedative activities of Levocabastine.	Experimental, Illicit
Molindone	The risk or severity of adverse effects can be increased when Molindone is combined with Levocabastine.	Approved
Morphine	The risk or severity of adverse effects can be increased when Morphine is combined with Levocabastine.	Approved, Investigational
Nabilone	Nabilone may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved, Investigational
Nalbuphine	The risk or severity of adverse effects can be increased when Nalbuphine is combined with Levocabastine.	Approved
Nefazodone	The risk or severity of adverse effects can be increased when Levocabastine is combined with Nefazodone.	Approved, Withdrawn
Nitrazepam	The risk or severity of adverse effects can be increased when Nitrazepam is combined with Levocabastine.	Approved
Nitrous oxide	The risk or severity of adverse effects can be increased when Nitrous oxide is combined with Levocabastine.	Approved, Vet Approved
Norflurane	The risk or severity of adverse effects can be increased when 1,1,1,2 Tetrafluoroethane is combined with Levocabastine.	Investigational
Normethadone	The risk or severity of adverse effects can be increased when Normethadone is combined with Levocabastine.	Approved, Illicit
Nortriptyline	The risk or severity of adverse effects can be increased when Nortriptyline is combined with Levocabastine.	Approved
Olanzapine	The risk or severity of adverse effects can be increased when Olanzapine is combined with Levocabastine.	Approved, Investigational
Olopatadine	The risk or severity of adverse effects can be increased when Olopatadine is combined with Levocabastine.	Approved
Ondansetron	The risk or severity of adverse effects can be increased when Ondansetron is combined with Levocabastine.	Approved
Opium	The risk or severity of adverse effects can be increased when Opium is combined with Levocabastine.	Approved, Illicit
Orphenadrine	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.	Approved
Osanetant	The risk or severity of adverse effects can be increased when Osanetant is combined with Levocabastine.	Investigational
Oxazepam	The risk or severity of adverse effects can be increased when Oxazepam is combined with Levocabastine.	Approved
Oxethazaine	The risk or severity of adverse effects can be increased when Oxetacaine is combined with Levocabastine.	Investigational
Oxprenolol	The risk or severity of adverse effects can be increased when Oxprenolol is combined with Levocabastine.	Approved
Oxybuprocaine	The risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Levocabastine.	Approved
Oxycodone	The risk or severity of adverse effects can be increased when Oxycodone is combined with Levocabastine.	Approved, Illicit, Investigational
Oxymorphone	The risk or severity of adverse effects can be increased when Oxymorphone is combined with Levocabastine.	Approved, Investigational, Vet Approved
Paliperidone	The risk or severity of adverse effects can be increased when Paliperidone is combined with Levocabastine.	Approved
Paraldehyde	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.	Approved
Paroxetine	The risk or severity of adverse effects can be increased when Levocabastine is combined with Paroxetine.	Approved, Investigational
Pentazocine	The risk or severity of adverse effects can be increased when Pentazocine is combined with Levocabastine.	Approved, Vet Approved
Pentobarbital	The risk or severity of adverse effects can be increased when Pentobarbital is combined with Levocabastine.	Approved, Vet Approved
Perampanel	Perampanel may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved
Perazine	The risk or severity of adverse effects can be increased when Perazine is combined with Levocabastine.	Investigational
Perospirone	The risk or severity of adverse effects can be increased when Perospirone is combined with Levocabastine.	Approved
Perphenazine	The risk or severity of adverse effects can be increased when Perphenazine is combined with Levocabastine.	Approved
Pethidine	The risk or severity of adverse effects can be increased when Pethidine is combined with Levocabastine.	Approved
Phenobarbital	The risk or severity of adverse effects can be increased when Phenobarbital is combined with Levocabastine.	Approved
Phenoxyethanol	The risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Levocabastine.	Approved
Phentermine	Phentermine may decrease the sedative activities of Levocabastine.	Approved, Illicit
Phenytoin	The risk or severity of adverse effects can be increased when Phenytoin is combined with Levocabastine.	Approved, Vet Approved
Pimozide	The risk or severity of adverse effects can be increased when Pimozide is combined with Levocabastine.	Approved
Pipamperone	The risk or severity of adverse effects can be increased when Pipamperone is combined with Levocabastine.	Approved
Pipotiazine	The risk or severity of adverse effects can be increased when Pipotiazine is combined with Levocabastine.	Approved
Piritramide	The risk or severity of adverse effects can be increased when Piritramide is combined with Levocabastine.	Investigational
Pizotifen	The risk or severity of adverse effects can be increased when Pizotifen is combined with Levocabastine.	Approved
Pomalidomide	The risk or severity of adverse effects can be increased when Pomalidomide is combined with Levocabastine.	Approved
Pramipexole	Levocabastine may increase the sedative activities of Pramipexole.	Approved, Investigational
Pramocaine	The risk or severity of adverse effects can be increased when Pramocaine is combined with Levocabastine.	Approved
Prazepam	The risk or severity of adverse effects can be increased when Prazepam is combined with Levocabastine.	Approved, Illicit
Pregabalin	The risk or severity of adverse effects can be increased when Pregabalin is combined with Levocabastine.	Approved, Illicit, Investigational
Prilocaine	The risk or severity of adverse effects can be increased when Prilocaine is combined with Levocabastine.	Approved
Primidone	The risk or severity of adverse effects can be increased when Primidone is combined with Levocabastine.	Approved, Vet Approved
Procaine	The risk or severity of adverse effects can be increased when Procaine is combined with Levocabastine.	Approved, Investigational, Vet Approved
Prochlorperazine	The risk or severity of adverse effects can be increased when Prochlorperazine is combined with Levocabastine.	Approved, Vet Approved
Promazine	The risk or severity of adverse effects can be increased when Promazine is combined with Levocabastine.	Approved, Vet Approved
Promethazine	The risk or severity of adverse effects can be increased when Promethazine is combined with Levocabastine.	Approved
Proparacaine	The risk or severity of adverse effects can be increased when Proparacaine is combined with Levocabastine.	Approved, Vet Approved
Propofol	The risk or severity of adverse effects can be increased when Propofol is combined with Levocabastine.	Approved, Investigational, Vet Approved
Propoxycaine	The risk or severity of adverse effects can be increased when Propoxycaine is combined with Levocabastine.	Approved
Protriptyline	The risk or severity of adverse effects can be increased when Protriptyline is combined with Levocabastine.	Approved
PSD502	The risk or severity of adverse effects can be increased when PSD502 is combined with Levocabastine.	Investigational
Pseudoephedrine	Pseudoephedrine may decrease the sedative activities of Levocabastine.	Approved
Quazepam	The risk or severity of adverse effects can be increased when Quazepam is combined with Levocabastine.	Approved, Illicit
Quetiapine	The risk or severity of adverse effects can be increased when Quetiapine is combined with Levocabastine.	Approved
Raclopride	The risk or severity of adverse effects can be increased when Raclopride is combined with Levocabastine.	Investigational
Ramelteon	The risk or severity of adverse effects can be increased when Ramelteon is combined with Levocabastine.	Approved, Investigational
Remifentanil	The risk or severity of adverse effects can be increased when Remifentanil is combined with Levocabastine.	Approved
Remoxipride	The risk or severity of adverse effects can be increased when Remoxipride is combined with Levocabastine.	Approved, Withdrawn
Reserpine	The risk or severity of adverse effects can be increased when Reserpine is combined with Levocabastine.	Approved
Risperidone	The risk or severity of adverse effects can be increased when Risperidone is combined with Levocabastine.	Approved, Investigational
Ritanserin	The risk or severity of adverse effects can be increased when Ritanserin is combined with Levocabastine.	Investigational
Ritobegron	Ritobegron may decrease the sedative activities of Levocabastine.	Investigational
Romifidine	The risk or severity of adverse effects can be increased when Romifidine is combined with Levocabastine.	Vet Approved
Ropinirole	Levocabastine may increase the sedative activities of Ropinirole.	Approved, Investigational
Ropivacaine	The risk or severity of adverse effects can be increased when Ropivacaine is combined with Levocabastine.	Approved
Rotigotine	Levocabastine may increase the sedative activities of Rotigotine.	Approved
Rufinamide	The risk or severity of adverse effects can be increased when Rufinamide is combined with Levocabastine.	Approved
Scopolamine	The risk or severity of adverse effects can be increased when Scopolamine is combined with Levocabastine.	Approved
Secobarbital	The risk or severity of adverse effects can be increased when Secobarbital is combined with Levocabastine.	Approved, Vet Approved
Sepranolone	The risk or severity of adverse effects can be increased when Uc1010 is combined with Levocabastine.	Investigational
Sertindole	The risk or severity of adverse effects can be increased when Sertindole is combined with Levocabastine.	Approved, Withdrawn
Sertraline	The risk or severity of adverse effects can be increased when Levocabastine is combined with Sertraline.	Approved
Sevoflurane	The risk or severity of adverse effects can be increased when Sevoflurane is combined with Levocabastine.	Approved, Vet Approved
Sodium oxybate	Sodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved
Stiripentol	The risk or severity of adverse effects can be increased when Stiripentol is combined with Levocabastine.	Approved
Sufentanil	The risk or severity of adverse effects can be increased when Sufentanil is combined with Levocabastine.	Approved, Investigational
Sulpiride	The risk or severity of adverse effects can be increased when Sulpiride is combined with Levocabastine.	Approved
Suvorexant	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.	Approved
Tandospirone	The risk or severity of adverse effects can be increased when Tandospirone is combined with Levocabastine.	Investigational
Tapentadol	Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.	Approved
Tasimelteon	The risk or severity of adverse effects can be increased when Tasimelteon is combined with Levocabastine.	Approved
Temazepam	The risk or severity of adverse effects can be increased when Temazepam is combined with Levocabastine.	Approved
Tetrabenazine	The risk or severity of adverse effects can be increased when Tetrabenazine is combined with Levocabastine.	Approved
Tetracaine	The risk or severity of adverse effects can be increased when Tetracaine is combined with Levocabastine.	Approved, Vet Approved
Tetrodotoxin	The risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Levocabastine.	Investigational
Thalidomide	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.	Approved, Investigational, Withdrawn
Thiamylal	The risk or severity of adverse effects can be increased when Thiamylal is combined with Levocabastine.	Approved, Vet Approved
Thiopental	The risk or severity of adverse effects can be increased when Thiopental is combined with Levocabastine.	Approved, Vet Approved
Thioridazine	The risk or severity of adverse effects can be increased when Thioridazine is combined with Levocabastine.	Withdrawn
Thiothixene	The risk or severity of adverse effects can be increased when Thiothixene is combined with Levocabastine.	Approved
Tiagabine	The risk or severity of adverse effects can be increased when Tiagabine is combined with Levocabastine.	Approved
Tiapride	The risk or severity of adverse effects can be increased when Tiapride is combined with Levocabastine.	Approved, Investigational
Tiletamine	The risk or severity of adverse effects can be increased when Tiletamine is combined with Levocabastine.	Vet Approved
Tizanidine	The risk or severity of adverse effects can be increased when Tizanidine is combined with Levocabastine.	Approved
Tolcapone	The risk or severity of adverse effects can be increased when Tolcapone is combined with Levocabastine.	Approved, Withdrawn
Topiramate	The risk or severity of adverse effects can be increased when Topiramate is combined with Levocabastine.	Approved
Tramadol	The risk or severity of adverse effects can be increased when Tramadol is combined with Levocabastine.	Approved, Investigational
Trans-2-Phenylcyclopropylamine	The risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Levocabastine.	Experimental
Tranylcypromine	The risk or severity of adverse effects can be increased when Tranylcypromine is combined with Levocabastine.	Approved
Trazodone	The risk or severity of adverse effects can be increased when Trazodone is combined with Levocabastine.	Approved, Investigational
Triazolam	The risk or severity of adverse effects can be increased when Triazolam is combined with Levocabastine.	Approved
Trifluoperazine	The risk or severity of adverse effects can be increased when Trifluoperazine is combined with Levocabastine.	Approved
Triflupromazine	The risk or severity of adverse effects can be increased when Triflupromazine is combined with Levocabastine.	Approved, Vet Approved
Trimipramine	The risk or severity of adverse effects can be increased when Trimipramine is combined with Levocabastine.	Approved
Triprolidine	The risk or severity of adverse effects can be increased when Triprolidine is combined with Levocabastine.	Approved
Valproic Acid	The risk or severity of adverse effects can be increased when Valproic Acid is combined with Levocabastine.	Approved, Investigational
Venlafaxine	The risk or severity of adverse effects can be increased when Levocabastine is combined with Venlafaxine.	Approved
Vigabatrin	The risk or severity of adverse effects can be increased when Vigabatrin is combined with Levocabastine.	Approved
Vortioxetine	The risk or severity of adverse effects can be increased when Vortioxetine is combined with Levocabastine.	Approved
Xylazine	The risk or severity of adverse effects can be increased when Xylazine is combined with Levocabastine.	Vet Approved
Zaleplon	The risk or severity of adverse effects can be increased when Zaleplon is combined with Levocabastine.	Approved, Illicit, Investigational
Ziconotide	The risk or severity of adverse effects can be increased when Ziconotide is combined with Levocabastine.	Approved
Zimelidine	The risk or severity of adverse effects can be increased when Levocabastine is combined with Zimelidine.	Withdrawn
Ziprasidone	The risk or severity of adverse effects can be increased when Ziprasidone is combined with Levocabastine.	Approved
Zolazepam	The risk or severity of adverse effects can be increased when Zolazepam is combined with Levocabastine.	Vet Approved
Zolpidem	Levocabastine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.	Approved
Zonisamide	The risk or severity of adverse effects can be increased when Zonisamide is combined with Levocabastine.	Approved, Investigational
Zopiclone	The risk or severity of adverse effects can be increased when Zopiclone is combined with Levocabastine.	Approved
Zotepine	The risk or severity of adverse effects can be increased when Zotepine is combined with Levocabastine.	Approved
Zuclopenthixol	The risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Levocabastine.	Approved, Investigational

Food Interactions

Not Available

References

Synthesis Reference

Not Available

General References

Not Available

External Links

Resource	Link
KEGG Drug	D01717
ChemSpider	16736421
BindingDB	50019405
ChEBI	135679
ChEMBL	CHEMBL1615438
Therapeutic Targets Database	DAP000335
PharmGKB	PA164742988
IUPHAR	1586
Guide to Pharmacology	1586
Drug Product Database	923
RxList	http://www.rxlist.com/cgi/generic2/livostin.htm
Drugs.com	http://www.drugs.com/mtm/levocabastine-ophthalmic.html
Wikipedia	Levocabastine

ATC Codes

R01AC02 — Levocabastine

S01GX02 — Levocabastine

AHFS Codes

52:02.00

PDB Entries

Not Available

FDA label

Not Available

MSDS

Not Available

Clinical Trials

Phase	Status	Purpose	Conditions	Count
2	Completed	Treatment	Rhinitis, Allergic, Perennial and Seasonal	2
3	Completed	Treatment	Rhinitis, Allergic, Perennial	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Dosage forms

Form	Route	Strength
Solution / drops; suspension	Ophthalmic	0.5 mg
Spray; suspension	Nasal	0.5 mg

Prices

Not Available

Patents

Not Available

Properties

State

Solid

Experimental Properties

Property	Value	Source
water solubility	>0.5 mg/mL	Not Available
logP	5	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.00347 mg/mL	ALOGPS
logP	4.56	ALOGPS
logP	2.5	ChemAxon
logS	-5.1	ALOGPS
pKa (Strongest Acidic)	3.71	ChemAxon
pKa (Strongest Basic)	10.32	ChemAxon
Physiological Charge	0	ChemAxon
Hydrogen Acceptor Count	4	ChemAxon
Hydrogen Donor Count	1	ChemAxon
Polar Surface Area	64.33 Å²	ChemAxon
Rotatable Bond Count	4	ChemAxon
Refractivity	118.48 m³·mol^-1	ChemAxon
Polarizability	45.58 Å³	ChemAxon
Number of Rings	4	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	Yes	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	0.9811
Blood Brain Barrier	+	0.8388
Caco-2 permeable	+	0.5747
P-glycoprotein substrate	Substrate	0.7325
P-glycoprotein inhibitor I	Inhibitor	0.5
P-glycoprotein inhibitor II	Non-inhibitor	0.5682
Renal organic cation transporter	Non-inhibitor	0.5526
CYP450 2C9 substrate	Non-substrate	0.7708
CYP450 2D6 substrate	Non-substrate	0.6679
CYP450 3A4 substrate	Substrate	0.5153
CYP450 1A2 substrate	Non-inhibitor	0.9046
CYP450 2C9 inhibitor	Non-inhibitor	0.9071
CYP450 2D6 inhibitor	Inhibitor	0.8932
CYP450 2C19 inhibitor	Non-inhibitor	0.9026
CYP450 3A4 inhibitor	Non-inhibitor	0.8309
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.9046
Ames test	Non AMES toxic	0.7503
Carcinogenicity	Non-carcinogens	0.9196
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.9608 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9404
hERG inhibition (predictor II)	Inhibitor	0.625

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum Type	Description	Splash Key
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 10V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 20V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 40V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 10V, Negative	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 20V, Negative	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 40V, Negative	Not Available

Taxonomy

Description

This 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.

Kingdom

Organic compounds

Super Class

Organoheterocyclic compounds

Class

Piperidines

Sub Class

Phenylpiperidines

Direct Parent

Phenylpiperidines

Alternative Parents

Piperidinecarboxylic acids / Fluorobenzenes / Cyclohexylamines / Aralkylamines / Aryl fluorides / Trialkylamines / Amino acids / Nitriles / Monocarboxylic acids and derivatives / Carboxylic acids

Substituents

Phenylpiperidine / Piperidinecarboxylic acid / Cyclohexylamine / Fluorobenzene / Aralkylamine / Halobenzene / Aryl fluoride / Aryl halide / Monocyclic benzene moiety / Benzenoid

Molecular Framework

Aromatic heteromonocyclic compounds

External Descriptors

Not Available

Targets

Details

1. Histamine H1 receptor

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
Uniprot Name:: Histamine H1 receptor
Molecular Weight:: 55783.61 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
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 ]
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 ]
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 ]
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 ]
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 ]

Details

2. Neurotensin receptor type 2

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
Uniprot Name:: Neurotensin receptor type 2
Molecular Weight:: 45384.635 Da

References

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 ]
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 ]
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 ]

Drug created on June 13, 2005 07:24 / Updated on September 01, 2017 10:36

Structure for DB01106 (Levocabastine)

Targets

References

References