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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyCinchocaine
Identification
- Name
- Cinchocaine
- Accession Number
- DB00527 (APRD00915)
- Type
- Small Molecule
- Groups
- Approved, Vet approved
- Description
A local anesthetic of the amide type now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local anesthetics and its parenteral use is restricted to spinal anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1006)
- Structure
Structure for DB00527 (Cinchocaine)
- Synonyms
- 2-Butoxy-N-(2-(diethylamino)ethyl)cinchoninamide
- 2-Butoxy-N-(alpha-diethylaminoethyl)cinchoninamide
- 2-Butoxy-N-(beta-diethylaminoethyl)cinchoninamide
- 2-Butoxy-N-[2-(diethylamino)ethyl]-4-quinolinecarboxamide
- 2-Butoxy-quinoline-4-carboxylic acid (2-diethylamino-ethyl)-amide
- 2-Butoxyquinoline-4-carboxylic acid diethylaminoethylamide
- 2-N-Butoxy-N-(2-diethylaminoethyl)cinchoninamide
- alpha-Butyloxycinchonic acid-gamma-diethylethylenediamine
- alpha-Butyloxycinchoninic acid diethylethylenediamide
- CINCHOCAINE
- Cinchocainum
- Cincocainio
- Dibucaine
- Dibucaine base
- N-(2-(Diethylamino)ethyl)-2-butoxycinchoninamide
- Product Ingredients
Ingredient UNII CAS InChI Key Cinchocaine hydrochloride Z97702A5DG 61-12-1 IVHBBMHQKZBJEU-UHFFFAOYSA-N Dibucaine hydrochloride Not Available Not Available Not applicable - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End CVS Hemorrhoidal Topical Analgesic Ointment 10 mg/g Topical CVS Health 2014-01-17 Not applicable US 
Dibucaine Cream 10 mg/g Topical CVS Health 2010-07-16 Not applicable US Dibucaine Ointment 1 g/100g Topical E. Fougera & CO., A division of Fougera Pharmaceuticals Inc. 1968-01-01 Not applicable US Dibucaine Ointment 1 g/100g Topical Perrigo New York Inc. 2011-06-20 Not applicable US Dibucaine Ointment .28 g/28g Topical Geritrex Llc 2014-01-06 Not applicable US Nupercainal Ointment 1 g/100g Topical Dr Reddy's Laboratories 2013-07-01 Not applicable US Nupercainal Anesthetic Ointment 1% Ointment 1 % Rectal; Topical Glaxosmithkline Inc 1944-12-31 Not applicable Canada 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Nupercainal Antiseptic Cream Cinchocaine (0.5 %) + Domiphen bromide (0.05 %) Cream Topical Glaxosmithkline Inc 1967-12-31 Not applicable Canada Proctol Ointment Dibucaine hydrochloride (0.5 %) + Esculin (1 %) + Framycetin sulfate (1 %) + Hydrocortisone (0.5 %) Ointment Rectal Odan Laboratories Ltd 2003-08-06 Not applicable Canada Proctol Suppositories Dibucaine hydrochloride (5 mg) + Esculin (10 mg) + Framycetin sulfate (10 mg) + Hydrocortisone (5 mg) Suppository Rectal Odan Laboratories Ltd 2004-03-15 Not applicable Canada Proctosedyl Ointment Dibucaine hydrochloride (5 mg) + Esculin (10 mg) + Framycetin sulfate (10 mg) + Hydrocortisone (5 mg) Ointment Rectal Hoechst Roussel Canada Inc. 1971-12-31 2006-07-28 Canada Proctosedyl Ointment Dibucaine hydrochloride (0.5 %) + Esculin (1 %) + Framycetin sulfate (1 %) + Hydrocortisone (0.5 %) Ointment Rectal Aptalis Pharma Canada Ulc 2003-04-01 Not applicable Canada Proctosedyl Ointment Dibucaine hydrochloride (5 mg) + Esculin (10 mg) + Framycetin sulfate (10 mg) + Hydrocortisone (5 mg) Ointment Rectal Roussel Canada Inc. 1959-12-31 1997-08-05 Canada Proctosedyl Sup Dibucaine hydrochloride (5 mg) + Esculin (10 mg) + Framycetin sulfate (10 mg) + Hydrocortisone (5 mg) Suppository Rectal Roussel Canada Inc. 1959-12-31 1996-09-09 Canada Proctosedyl Suppositories Dibucaine hydrochloride (5 mg) + Esculin (10 mg) + Framycetin sulfate (10 mg) + Hydrocortisone (5 mg) Suppository Rectal Hoechst Roussel Canada Inc. 1959-12-31 1999-08-11 Canada Proctosedyl Suppositories Dibucaine hydrochloride (5 mg) + Esculin (10 mg) + Framycetin sulfate (10 mg) + Hydrocortisone (5 mg) Suppository Rectal Aptalis Pharma Canada Ulc 1997-01-23 Not applicable Canada Proctosone Ont Dibucaine hydrochloride (.5 %) + Esculin (1 %) + Hydrocortisone acetate (.5 %) + Neomycin sulfate (1 %) Ointment Rectal Technilab Pharma Inc. 1981-12-31 2004-08-03 Canada - International/Other Brands
- Cincain / Nupercaine / Sovcaine
- Categories
- Agents for Treatment of Hemorrhoids and Anal Fissures for Topical Use
- Amides
- Analgesics and Anesthetics
- Anesthetics
- Anesthetics for Topical Use
- Anesthetics, Local
- Antipruritics and Local Anesthetics
- Antipruritics, Incl. Antihistamines, Anesthetics, Etc.
- Cardiovascular System
- Central Nervous System Agents
- Dermatologicals
- Nervous System
- Ophthalmologicals
- Otologicals
- Peripheral Nervous System Agents
- Quinolines
- Sensory Organs
- Sensory System Agents
- Vasoprotectives
- UNII
- L6JW2TJG99
- CAS number
- 85-79-0
- Weight
- Average: 343.4632
Monoisotopic: 343.225977187 - Chemical Formula
- C20H29N3O2
- InChI Key
- PUFQVTATUTYEAL-UHFFFAOYSA-N
- InChI
- InChI=1S/C20H29N3O2/c1-4-7-14-25-19-15-17(16-10-8-9-11-18(16)22-19)20(24)21-12-13-23(5-2)6-3/h8-11,15H,4-7,12-14H2,1-3H3,(H,21,24)
- IUPAC Name
- 2-butoxy-N-[2-(diethylamino)ethyl]quinoline-4-carboxamide
- SMILES
- CCCCOC1=NC2=CC=CC=C2C(=C1)C(=O)NCCN(CC)CC
Pharmacology
- Indication
For production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
- Associated Conditions
- Pharmacodynamics
Dibucaine is an amide-type local anesthetic, similar to lidocaine.
- Mechanism of action
Local anesthetics block both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions through sodium channel inhibition. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.
Target Actions Organism ASodium channel protein type 10 subunit alpha inhibitorHuman ASodium channel protein type 5 subunit alpha inhibitorHuman UCalmodulin inhibitorHuman - Absorption
In general, ionized forms (salts) of local anesthetics are not readily absorbed through intact skin. However, both nonionized (bases) and ionized forms of local anesthetics are readily absorbed through traumatized or abraded skin into the systemic circulation.
- Volume of distribution
- Not Available
- Protein binding
- Not Available
- Metabolism
Primarily hepatic.
- Route of elimination
- Not Available
- Half life
- Not Available
- Clearance
- Not Available
- Toxicity
Subcutaneous LD50 in rat is 27 mg/kg. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
- Affected organisms
- Humans and other mammals
- Pathways
Pathway Category Dibucaine Action Pathway Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group 7-Nitroindazole The risk or severity of adverse effects can be increased when Cinchocaine is combined with 7-Nitroindazole. Experimental Acepromazine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Acepromazine. Approved, Vet Approved Aceprometazine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Aceprometazine. Approved Adipiplon The risk or severity of adverse effects can be increased when Cinchocaine is combined with Adipiplon. Investigational Agomelatine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Agomelatine. Approved, Investigational Alaproclate The risk or severity of adverse effects can be increased when Cinchocaine is combined with Alaproclate. Experimental Alfaxalone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Alfaxalone. Vet Approved Alfentanil The risk or severity of adverse effects can be increased when Alfentanil is combined with Cinchocaine. Approved, Illicit Allopregnanolone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Allopregnanolone. Investigational Alphacetylmethadol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Alphacetylmethadol. Experimental, Illicit Alphaprodine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Alphaprodine. Illicit Alprazolam The risk or severity of adverse effects can be increased when Alprazolam is combined with Cinchocaine. Approved, Illicit, Investigational Amisulpride The risk or severity of adverse effects can be increased when Cinchocaine is combined with Amisulpride. Approved, Investigational Amitriptyline The risk or severity of adverse effects can be increased when Amitriptyline is combined with Cinchocaine. Approved Amobarbital The risk or severity of adverse effects can be increased when Amobarbital is combined with Cinchocaine. Approved, Illicit Amoxapine The risk or severity of adverse effects can be increased when Amoxapine is combined with Cinchocaine. Approved Amperozide The risk or severity of adverse effects can be increased when Cinchocaine is combined with Amperozide. Experimental Aripiprazole The risk or severity of adverse effects can be increased when Aripiprazole is combined with Cinchocaine. Approved, Investigational Articaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Articaine. Approved Asenapine The risk or severity of adverse effects can be increased when Asenapine is combined with Cinchocaine. Approved Azaperone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Azaperone. Investigational, Vet Approved Azelastine Cinchocaine may increase the central nervous system depressant (CNS depressant) activities of Azelastine. Approved Baclofen The risk or severity of adverse effects can be increased when Baclofen is combined with Cinchocaine. Approved Barbital The risk or severity of adverse effects can be increased when Cinchocaine is combined with Barbital. Illicit Benperidol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Benperidol. Approved, Investigational Brexpiprazole The risk or severity of adverse effects can be increased when Brexpiprazole is combined with Cinchocaine. Approved, Investigational Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Cinchocaine. Approved Bromazepam The risk or severity of adverse effects can be increased when Bromazepam is combined with Cinchocaine. Approved, Illicit, Investigational Bromisoval The risk or severity of adverse effects can be increased when Cinchocaine is combined with Bromisoval. Experimental Bromperidol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Bromperidol. Approved, Investigational Brotizolam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Brotizolam. Approved, Investigational, Withdrawn Bupivacaine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Cinchocaine. Approved, Investigational Buprenorphine Cinchocaine 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 Cinchocaine. Approved, Investigational Butabarbital The risk or severity of adverse effects can be increased when Butabarbital is combined with Cinchocaine. Approved, Illicit Butacaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Butacaine. Vet Approved Butalbital The risk or severity of adverse effects can be increased when Butalbital is combined with Cinchocaine. Approved, Illicit Butamben The risk or severity of adverse effects can be increased when Cinchocaine is combined with Butamben. Approved, Withdrawn Butethal The risk or severity of adverse effects can be increased when Cinchocaine is combined with Butethal. Approved, Illicit Butorphanol The risk or severity of adverse effects can be increased when Butorphanol is combined with Cinchocaine. Approved, Illicit, Vet Approved Canertinib The risk or severity of adverse effects can be increased when Cinchocaine is combined with Canertinib. Investigational Carbinoxamine The risk or severity of adverse effects can be increased when Carbinoxamine is combined with Cinchocaine. Approved Carfentanil The risk or severity of adverse effects can be increased when Cinchocaine is combined with Carfentanil. Illicit, Investigational, Vet Approved Carisoprodol The risk or severity of adverse effects can be increased when Carisoprodol is combined with Cinchocaine. Approved Chloral hydrate The risk or severity of adverse effects can be increased when Cinchocaine is combined with Chloral hydrate. Approved, Illicit, Investigational, Vet Approved Chlordiazepoxide The risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Cinchocaine. Approved, Illicit, Investigational Chlormezanone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Chlormezanone. Approved, Investigational, Withdrawn Chloroprocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Chloroprocaine. Approved Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Cinchocaine. Approved, Investigational, Vet Approved Chlorprothixene The risk or severity of adverse effects can be increased when Cinchocaine is combined with Chlorprothixene. Approved, Investigational, Withdrawn Chlorzoxazone The risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Cinchocaine. Approved Citalopram The risk or severity of adverse effects can be increased when Cinchocaine is combined with Citalopram. Approved Clidinium The risk or severity of adverse effects can be increased when Clidinium is combined with Cinchocaine. Approved Clobazam The risk or severity of adverse effects can be increased when Clobazam is combined with Cinchocaine. Approved, Illicit clomethiazole The risk or severity of adverse effects can be increased when Cinchocaine is combined with clomethiazole. Investigational Clomipramine The risk or severity of adverse effects can be increased when Clomipramine is combined with Cinchocaine. Approved, Investigational, Vet Approved Clonazepam The risk or severity of adverse effects can be increased when Clonazepam is combined with Cinchocaine. Approved, Illicit Clonidine The risk or severity of adverse effects can be increased when Clonidine is combined with Cinchocaine. Approved Clopenthixol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Clopenthixol. Experimental Clorazepate The risk or severity of adverse effects can be increased when Clorazepate is combined with Cinchocaine. Approved, Illicit Clothiapine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Clothiapine. Experimental Clozapine The risk or severity of adverse effects can be increased when Clozapine is combined with Cinchocaine. Approved Cocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Cocaine. Approved, Illicit Cyclizine The risk or severity of adverse effects can be increased when Cyclizine is combined with Cinchocaine. Approved Cyclopropane The risk or severity of adverse effects can be increased when Cinchocaine is combined with Cyclopropane. Experimental Cyproheptadine The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Cinchocaine. Approved Dantrolene The risk or severity of adverse effects can be increased when Dantrolene is combined with Cinchocaine. Approved, Investigational Dapiprazole The risk or severity of adverse effects can be increased when Dapiprazole is combined with Cinchocaine. Approved Dapoxetine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Dapoxetine. Investigational Deramciclane The risk or severity of adverse effects can be increased when Cinchocaine is combined with Deramciclane. Investigational Desflurane The risk or severity of adverse effects can be increased when Desflurane is combined with Cinchocaine. Approved Desipramine The risk or severity of adverse effects can be increased when Desipramine is combined with Cinchocaine. Approved, Investigational Desloratadine The risk or severity of adverse effects can be increased when Desloratadine is combined with Cinchocaine. Approved, Investigational Detomidine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Detomidine. Vet Approved Dexmedetomidine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Dexmedetomidine. Approved, Vet Approved Dextromoramide The risk or severity of adverse effects can be increased when Cinchocaine is combined with Dextromoramide. Experimental, Illicit Dextropropoxyphene The risk or severity of adverse effects can be increased when Cinchocaine is combined with Dextropropoxyphene. Approved, Illicit, Investigational, Withdrawn Dezocine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Dezocine. Approved, Investigational Diazepam The risk or severity of adverse effects can be increased when Diazepam is combined with Cinchocaine. Approved, Illicit, Investigational, Vet Approved Diethyl ether The risk or severity of adverse effects can be increased when Cinchocaine is combined with Diethyl ether. Experimental Difenoxin The risk or severity of adverse effects can be increased when Difenoxin is combined with Cinchocaine. Approved, Illicit Dihydrocodeine The risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Cinchocaine. Approved, Illicit Dihydroetorphine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Dihydroetorphine. Experimental, Illicit Dihydromorphine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Dihydromorphine. Experimental, Illicit Diphenoxylate The risk or severity of adverse effects can be increased when Diphenoxylate is combined with Cinchocaine. Approved, Illicit Dixyrazine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Dixyrazine. Experimental Doramectin The risk or severity of adverse effects can be increased when Cinchocaine is combined with Doramectin. Vet Approved Doxepin The risk or severity of adverse effects can be increased when Doxepin is combined with Cinchocaine. Approved, Investigational DPDPE The risk or severity of adverse effects can be increased when Cinchocaine is combined with DPDPE. Experimental Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Cinchocaine. Approved, Illicit Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Cinchocaine. Approved, Vet Approved Drotebanol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Drotebanol. Experimental, Illicit Duloxetine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Duloxetine. Approved Dyclonine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Dyclonine. Approved Ecgonine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Ecgonine. Experimental, Illicit Ecopipam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Ecopipam. Investigational Efavirenz The risk or severity of adverse effects can be increased when Efavirenz is combined with Cinchocaine. Approved, Investigational Eltanolone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Eltanolone. Investigational Enflurane The risk or severity of adverse effects can be increased when Enflurane is combined with Cinchocaine. Approved, Investigational, Vet Approved Entacapone The risk or severity of adverse effects can be increased when Entacapone is combined with Cinchocaine. Approved, Investigational Escitalopram The risk or severity of adverse effects can be increased when Cinchocaine is combined with Escitalopram. Approved, Investigational Estazolam The risk or severity of adverse effects can be increased when Estazolam is combined with Cinchocaine. Approved, Illicit Eszopiclone The risk or severity of adverse effects can be increased when Eszopiclone is combined with Cinchocaine. Approved, Investigational Ethchlorvynol The risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Cinchocaine. Approved, Illicit, Withdrawn Ethotoin The risk or severity of adverse effects can be increased when Ethotoin is combined with Cinchocaine. Approved Ethyl carbamate The risk or severity of adverse effects can be increased when Cinchocaine is combined with Ethyl carbamate. Withdrawn Ethyl chloride The risk or severity of adverse effects can be increased when Cinchocaine is combined with Ethyl chloride. Approved, Experimental, Investigational Ethyl loflazepate The risk or severity of adverse effects can be increased when Cinchocaine is combined with Ethyl loflazepate. Approved, Illicit Ethylmorphine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Ethylmorphine. Approved, Illicit Etidocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Etidocaine. Approved Etifoxine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Etifoxine. Investigational, Withdrawn Etizolam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Etizolam. Approved Etoperidone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Etoperidone. Withdrawn Etorphine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Etorphine. Illicit, Vet Approved Ezogabine The risk or severity of adverse effects can be increased when Ezogabine is combined with Cinchocaine. Approved, Investigational Felbamate The risk or severity of adverse effects can be increased when Felbamate is combined with Cinchocaine. Approved Fencamfamine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Fencamfamine. Approved, Illicit, Withdrawn Fexofenadine The risk or severity of adverse effects can be increased when Fexofenadine is combined with Cinchocaine. Approved, Investigational Flibanserin The risk or severity of adverse effects can be increased when Flibanserin is combined with Cinchocaine. Approved, Investigational Fluanisone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Fluanisone. Experimental Fludiazepam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Fludiazepam. Approved, Illicit Flunitrazepam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Flunitrazepam. Approved, Illicit Flupentixol The risk or severity of adverse effects can be increased when Flupentixol is combined with Cinchocaine. Approved, Investigational, Withdrawn Fluphenazine The risk or severity of adverse effects can be increased when Fluphenazine is combined with Cinchocaine. Approved Flurazepam The risk or severity of adverse effects can be increased when Flurazepam is combined with Cinchocaine. Approved, Illicit, Investigational Fosphenytoin The risk or severity of adverse effects can be increased when Fosphenytoin is combined with Cinchocaine. Approved, Investigational Fospropofol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Fospropofol. Approved, Illicit, Investigational Gabapentin Enacarbil The risk or severity of adverse effects can be increased when Gabapentin Enacarbil is combined with Cinchocaine. Approved, Investigational Gamma Hydroxybutyric Acid The risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Cinchocaine. Approved, Illicit, Investigational Gepirone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Gepirone. Investigational Glutethimide The risk or severity of adverse effects can be increased when Cinchocaine is combined with Glutethimide. Approved, Illicit Halazepam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Halazepam. Approved, Illicit, Withdrawn Haloperidol The risk or severity of adverse effects can be increased when Haloperidol is combined with Cinchocaine. Approved Halothane The risk or severity of adverse effects can be increased when Cinchocaine is combined with Halothane. Approved, Vet Approved Heroin The risk or severity of adverse effects can be increased when Cinchocaine is combined with Heroin. Approved, Illicit, Investigational Hexobarbital The risk or severity of adverse effects can be increased when Cinchocaine is combined with Hexobarbital. Approved Hyaluronidase The risk or severity of adverse effects can be increased when Hyaluronidase is combined with Cinchocaine. Approved, Investigational Hydromorphone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Cinchocaine. Approved, Illicit Iloperidone The risk or severity of adverse effects can be increased when Iloperidone is combined with Cinchocaine. Approved Imipramine The risk or severity of adverse effects can be increased when Imipramine is combined with Cinchocaine. Approved Indalpine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Indalpine. Investigational, Withdrawn Indiplon The risk or severity of adverse effects can be increased when Cinchocaine is combined with Indiplon. Investigational Isoflurane The risk or severity of adverse effects can be increased when Isoflurane is combined with Cinchocaine. Approved, Vet Approved Ketamine The risk or severity of adverse effects can be increased when Ketamine is combined with Cinchocaine. Approved, Vet Approved Ketazolam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Ketazolam. Approved Ketobemidone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Ketobemidone. Approved, Investigational Levobupivacaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Levobupivacaine. Approved, Investigational Levocabastine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Levocabastine. Approved, Investigational Levocetirizine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Cinchocaine. Approved Levomethadyl Acetate The risk or severity of adverse effects can be increased when Cinchocaine is combined with Levomethadyl Acetate. Approved, Investigational Levomilnacipran The risk or severity of adverse effects can be increased when Cinchocaine is combined with Levomilnacipran. Approved, Investigational Levorphanol The risk or severity of adverse effects can be increased when Levorphanol is combined with Cinchocaine. Approved Lithium cation The risk or severity of adverse effects can be increased when Cinchocaine is combined with Lithium. Experimental Lofentanil The risk or severity of adverse effects can be increased when Cinchocaine is combined with Lofentanil. Illicit Lofexidine The therapeutic efficacy of Cinchocaine can be increased when used in combination with Lofexidine. Approved, Investigational Loprazolam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Loprazolam. Experimental Lorazepam The risk or severity of adverse effects can be increased when Lorazepam is combined with Cinchocaine. Approved Lormetazepam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Lormetazepam. Approved Loxapine The risk or severity of adverse effects can be increased when Loxapine is combined with Cinchocaine. Approved Lurasidone The risk or severity of adverse effects can be increased when Lurasidone is combined with Cinchocaine. Approved, Investigational Maprotiline The risk or severity of adverse effects can be increased when Maprotiline is combined with Cinchocaine. Approved, Investigational Mebicar The risk or severity of adverse effects can be increased when Cinchocaine is combined with Mebicar. Experimental Medazepam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Medazepam. Experimental Medetomidine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Medetomidine. Vet Approved Melatonin The risk or severity of adverse effects can be increased when Cinchocaine is combined with Melatonin. Approved, Nutraceutical, Vet Approved Melperone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Melperone. Approved, Investigational Mepivacaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Mepivacaine. Approved, Vet Approved Meprobamate The risk or severity of adverse effects can be increased when Meprobamate is combined with Cinchocaine. Approved, Illicit Meptazinol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Meptazinol. Experimental Mesoridazine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Mesoridazine. Approved, Investigational Metaxalone The risk or severity of adverse effects can be increased when Metaxalone is combined with Cinchocaine. Approved Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Cinchocaine. Approved Methadyl Acetate The risk or severity of adverse effects can be increased when Cinchocaine is combined with Methadyl Acetate. Approved, Illicit Methapyrilene The risk or severity of adverse effects can be increased when Cinchocaine is combined with Methapyrilene. Withdrawn Methaqualone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Methaqualone. Illicit, Withdrawn Methocarbamol The risk or severity of adverse effects can be increased when Methocarbamol is combined with Cinchocaine. Approved, Vet Approved Methohexital The risk or severity of adverse effects can be increased when Methohexital is combined with Cinchocaine. Approved Methotrimeprazine Cinchocaine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine. Approved, Investigational Methoxyflurane The risk or severity of adverse effects can be increased when Cinchocaine is combined with Methoxyflurane. Approved, Investigational, Vet Approved Methylecgonine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Methylecgonine. Experimental Methylphenobarbital The risk or severity of adverse effects can be increased when Cinchocaine is combined with Methylphenobarbital. Approved Metyrosine Cinchocaine may increase the sedative activities of Metyrosine. Approved Midazolam The risk or severity of adverse effects can be increased when Midazolam is combined with Cinchocaine. Approved, Illicit Milnacipran The risk or severity of adverse effects can be increased when Cinchocaine is combined with Milnacipran. Approved, Investigational Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Cinchocaine. Approved, Investigational Mirtazapine Cinchocaine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine. Approved Molindone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Molindone. Approved Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Cinchocaine. Approved, Investigational Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Cinchocaine. Approved, Investigational Nalbuphine The risk or severity of adverse effects can be increased when Nalbuphine is combined with Cinchocaine. Approved Nefazodone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Nefazodone. Approved, Withdrawn Nitrazepam The risk or severity of adverse effects can be increased when Nitrazepam is combined with Cinchocaine. Approved Nitrous oxide The risk or severity of adverse effects can be increased when Nitrous oxide is combined with Cinchocaine. Approved, Vet Approved Nordazepam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Nordazepam. Approved Norflurane The risk or severity of adverse effects can be increased when Cinchocaine is combined with Norflurane. Approved, Investigational Normethadone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Normethadone. Approved, Illicit Nortriptyline The risk or severity of adverse effects can be increased when Nortriptyline is combined with Cinchocaine. Approved Olanzapine The risk or severity of adverse effects can be increased when Olanzapine is combined with Cinchocaine. Approved, Investigational Olopatadine The risk or severity of adverse effects can be increased when Olopatadine is combined with Cinchocaine. Approved Opium The risk or severity of adverse effects can be increased when Cinchocaine is combined with Opium. Approved, Illicit Orphenadrine Cinchocaine 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 Cinchocaine is combined with Osanetant. Investigational Oxazepam The risk or severity of adverse effects can be increased when Oxazepam is combined with Cinchocaine. Approved Oxprenolol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Oxprenolol. Approved Oxybuprocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Oxybuprocaine. Approved, Investigational Paliperidone The risk or severity of adverse effects can be increased when Paliperidone is combined with Cinchocaine. Approved Paraldehyde Cinchocaine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde. Approved, Investigational Pentazocine The risk or severity of adverse effects can be increased when Pentazocine is combined with Cinchocaine. Approved, Vet Approved Pentobarbital The risk or severity of adverse effects can be increased when Pentobarbital is combined with Cinchocaine. Approved, Investigational, Vet Approved Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Cinchocaine. Approved Perazine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Perazine. Approved, Investigational Perospirone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Perospirone. Approved Perphenazine The risk or severity of adverse effects can be increased when Perphenazine is combined with Cinchocaine. Approved Pethidine The risk or severity of adverse effects can be increased when Pethidine is combined with Cinchocaine. Approved Phenazocine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Phenazocine. Experimental Phenibut The risk or severity of adverse effects can be increased when Cinchocaine is combined with Phenibut. Experimental Phenoperidine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Phenoperidine. Experimental Phenoxyethanol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Phenoxyethanol. Approved Phenytoin The risk or severity of adverse effects can be increased when Phenytoin is combined with Cinchocaine. Approved, Vet Approved Pimozide The risk or severity of adverse effects can be increased when Pimozide is combined with Cinchocaine. Approved Pipamperone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Pipamperone. Approved, Investigational Pipotiazine The risk or severity of adverse effects can be increased when Pipotiazine is combined with Cinchocaine. Approved, Investigational Piritramide The risk or severity of adverse effects can be increased when Cinchocaine is combined with Piritramide. Approved, Investigational Pizotifen The risk or severity of adverse effects can be increased when Pizotifen is combined with Cinchocaine. Approved Pomalidomide The risk or severity of adverse effects can be increased when Pomalidomide is combined with Cinchocaine. Approved Prazepam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Prazepam. Approved, Illicit Prilocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Prilocaine. Approved Primidone The risk or severity of adverse effects can be increased when Primidone is combined with Cinchocaine. Approved, Vet Approved Procaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Procaine. Approved, Investigational, Vet Approved Promazine The risk or severity of adverse effects can be increased when Promazine is combined with Cinchocaine. Approved, Vet Approved Propanidid The risk or severity of adverse effects can be increased when Cinchocaine is combined with Propanidid. Experimental Proparacaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Proparacaine. Approved, Vet Approved Propofol The risk or severity of adverse effects can be increased when Propofol is combined with Cinchocaine. Approved, Investigational, Vet Approved Propoxycaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Propoxycaine. Approved Protriptyline The risk or severity of adverse effects can be increased when Protriptyline is combined with Cinchocaine. Approved Proxibarbal The risk or severity of adverse effects can be increased when Cinchocaine is combined with Proxibarbal. Experimental PSD502 The risk or severity of adverse effects can be increased when Cinchocaine is combined with PSD502. Investigational Quazepam The risk or severity of adverse effects can be increased when Quazepam is combined with Cinchocaine. Approved, Illicit Quinisocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Quinisocaine. Experimental Raclopride The risk or severity of adverse effects can be increased when Cinchocaine is combined with Raclopride. Investigational Ramelteon The risk or severity of adverse effects can be increased when Ramelteon is combined with Cinchocaine. Approved, Investigational Remifentanil The risk or severity of adverse effects can be increased when Remifentanil is combined with Cinchocaine. Approved Remoxipride The risk or severity of adverse effects can be increased when Remoxipride is combined with Cinchocaine. Approved, Withdrawn Reserpine The risk or severity of adverse effects can be increased when Reserpine is combined with Cinchocaine. Approved, Investigational Risperidone The risk or severity of adverse effects can be increased when Risperidone is combined with Cinchocaine. Approved, Investigational Ritanserin The risk or severity of adverse effects can be increased when Cinchocaine is combined with Ritanserin. Investigational Romifidine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Romifidine. Vet Approved Ropivacaine The risk or severity of adverse effects can be increased when Ropivacaine is combined with Cinchocaine. Approved Rotigotine Cinchocaine may increase the sedative activities of Rotigotine. Approved Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Cinchocaine. Approved Secobarbital The risk or severity of adverse effects can be increased when Secobarbital is combined with Cinchocaine. Approved, Vet Approved Sepranolone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Sepranolone. Investigational Sertindole The risk or severity of adverse effects can be increased when Cinchocaine is combined with Sertindole. Approved, Investigational, Withdrawn Sertraline The risk or severity of adverse effects can be increased when Cinchocaine is combined with Sertraline. Approved Sevoflurane The risk or severity of adverse effects can be increased when Sevoflurane is combined with Cinchocaine. Approved, Vet Approved Sodium oxybate Sodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Cinchocaine. Approved Stiripentol The risk or severity of adverse effects can be increased when Stiripentol is combined with Cinchocaine. Approved Sufentanil The risk or severity of adverse effects can be increased when Sufentanil is combined with Cinchocaine. Approved, Investigational Sulpiride The risk or severity of adverse effects can be increased when Sulpiride is combined with Cinchocaine. Approved, Investigational Sultopride The risk or severity of adverse effects can be increased when Cinchocaine is combined with Sultopride. Experimental Suvorexant Cinchocaine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant. Approved, Investigational Tandospirone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Tandospirone. Investigational Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Cinchocaine. Approved Tasimelteon The risk or severity of adverse effects can be increased when Tasimelteon is combined with Cinchocaine. Approved, Investigational Technetium Tc-99m tilmanocept Cinchocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Approved, Investigational Temazepam The risk or severity of adverse effects can be increased when Temazepam is combined with Cinchocaine. Approved, Investigational Tetrabenazine The risk or severity of adverse effects can be increased when Tetrabenazine is combined with Cinchocaine. Approved, Investigational Tetracaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Tetracaine. Approved, Vet Approved Tetrodotoxin The risk or severity of adverse effects can be increased when Cinchocaine is combined with Tetrodotoxin. Investigational Thalidomide Cinchocaine 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 Cinchocaine is combined with Thiamylal. Approved, Vet Approved Thiopental The risk or severity of adverse effects can be increased when Cinchocaine is combined with Thiopental. Approved, Vet Approved Thioridazine The risk or severity of adverse effects can be increased when Thioridazine is combined with Cinchocaine. Approved, Withdrawn Thiothixene The risk or severity of adverse effects can be increased when Thiothixene is combined with Cinchocaine. Approved Tiagabine The risk or severity of adverse effects can be increased when Tiagabine is combined with Cinchocaine. Approved, Investigational Tiapride The risk or severity of adverse effects can be increased when Cinchocaine is combined with Tiapride. Approved, Investigational Tiletamine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Tiletamine. Vet Approved Tilidine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Tilidine. Experimental Tizanidine The risk or severity of adverse effects can be increased when Tizanidine is combined with Cinchocaine. Approved, Investigational Tolcapone The risk or severity of adverse effects can be increased when Tolcapone is combined with Cinchocaine. Approved, Withdrawn Tranylcypromine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Tranylcypromine. Approved, Investigational Trazodone The risk or severity of adverse effects can be increased when Cinchocaine is combined with Trazodone. Approved, Investigational Triazolam The risk or severity of adverse effects can be increased when Triazolam is combined with Cinchocaine. Approved, Investigational Tricaine methanesulfonate The risk or severity of adverse effects can be increased when Cinchocaine is combined with Tricaine methanesulfonate. Vet Approved Trichloroethylene The risk or severity of adverse effects can be increased when Cinchocaine is combined with Trichloroethylene. Approved Trifluoperazine The risk or severity of adverse effects can be increased when Trifluoperazine is combined with Cinchocaine. Approved, Investigational Trifluperidol The risk or severity of adverse effects can be increased when Cinchocaine is combined with Trifluperidol. Experimental Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Cinchocaine. Approved, Vet Approved Trimipramine The risk or severity of adverse effects can be increased when Trimipramine is combined with Cinchocaine. Approved Triprolidine The risk or severity of adverse effects can be increased when Triprolidine is combined with Cinchocaine. Approved Veralipride The risk or severity of adverse effects can be increased when Cinchocaine is combined with Veralipride. Experimental Vigabatrin The risk or severity of adverse effects can be increased when Vigabatrin is combined with Cinchocaine. Approved Vinyl ether The risk or severity of adverse effects can be increased when Cinchocaine is combined with Vinyl ether. Experimental Vortioxetine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Vortioxetine. Approved, Investigational Xenon The risk or severity of adverse effects can be increased when Cinchocaine is combined with Xenon. Experimental Xylazine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Xylazine. Vet Approved Zaleplon The risk or severity of adverse effects can be increased when Zaleplon is combined with Cinchocaine. Approved, Illicit, Investigational Zimelidine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Zimelidine. Withdrawn Ziprasidone The risk or severity of adverse effects can be increased when Ziprasidone is combined with Cinchocaine. Approved Zolazepam The risk or severity of adverse effects can be increased when Cinchocaine is combined with Zolazepam. Vet Approved Zopiclone The risk or severity of adverse effects can be increased when Zopiclone is combined with Cinchocaine. Approved Zotepine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Zotepine. Approved, Investigational, Withdrawn Zuclopenthixol The risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Cinchocaine. Approved, Investigational - Food Interactions
- Not Available
References
- Synthesis Reference
- US1825623
- General References
- Abdel-Ghani NT, Youssef AF, Awady MA: Cinchocaine hydrochloride determination by atomic absorption spectrometry and spectrophotometry. Farmaco. 2005 May;60(5):419-24. [PubMed:15910814]
- Souto-Padron T, Lima AP, Ribeiro Rde O: Effects of dibucaine on the endocytic/exocytic pathways in Trypanosoma cruzi. Parasitol Res. 2006 Sep;99(4):317-20. Epub 2006 Apr 13. [PubMed:16612626]
- Nounou MM, El-Khordagui LK, Khalafallah N: Effect of various formulation variables on the encapsulation and stability of dibucaine base in multilamellar vesicles. Acta Pol Pharm. 2005 Sep-Oct;62(5):369-79. [PubMed:16459486]
- External Links
- Human Metabolome Database
- HMDB0014668
- KEGG Drug
- D00733
- KEGG Compound
- C07879
- PubChem Compound
- 3025
- PubChem Substance
- 46506734
- ChemSpider
- 2917
- BindingDB
- 48532
- ChEBI
- 247956
- ChEMBL
- CHEMBL1086
- Therapeutic Targets Database
- DAP000507
- PharmGKB
- PA449286
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Dibucaine
- ATC Codes
- S02DA04 — CinchocaineN01BB06 — CinchocaineS01HA06 — CinchocaineD04AB02 — Cinchocaine
- D04AB — Anesthetics for topical use
- D04A — ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
- D04 — ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
- D — DERMATOLOGICALS
- AHFS Codes
- 84:08.00 — Antipruritics and Local Anesthetics
- MSDS
- Download (73.8 KB)
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Novartis pharmaceuticals corp
- Packagers
- Medisca Inc.
- Novartis AG
- Perrigo Co.
- Dosage forms
Form Route Strength Ointment Topical 10 mg/g Cream Topical 10 mg/g Ointment Topical .28 g/28g Ointment Topical 1 g/100g Ointment Rectal; Topical 1 % Cream Topical Ointment Rectal Suppository Rectal - Prices
Unit description Cost Unit Dibucaine hcl powder 4.74USD g Nupercainal 1% ointment 0.15USD g Dibucaine 1% ointment 0.12USD g DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 99-101 °C (HCl salt) Not Available water solubility 42 mg/L (at 21 °C) BEILSTEIN logP 4.40 HANSCH,C ET AL. (1995) logS -3.7 ADME Research, USCD pKa 8.85 SANGSTER (1994) - Predicted Properties
Property Value Source Water Solubility 0.0389 mg/mL ALOGPS logP 3.79 ALOGPS logP 3.7 ChemAxon logS -4 ALOGPS pKa (Strongest Acidic) 14.57 ChemAxon pKa (Strongest Basic) 9.04 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 4 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 54.46 Å2 ChemAxon Rotatable Bond Count 10 ChemAxon Refractivity 102.12 m3·mol-1 ChemAxon Polarizability 40.78 Å3 ChemAxon Number of Rings 2 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 + 0.9968 Blood Brain Barrier + 0.9876 Caco-2 permeable + 0.5187 P-glycoprotein substrate Substrate 0.8702 P-glycoprotein inhibitor I Inhibitor 0.7536 P-glycoprotein inhibitor II Non-inhibitor 0.8862 Renal organic cation transporter Non-inhibitor 0.6349 CYP450 2C9 substrate Non-substrate 0.8297 CYP450 2D6 substrate Non-substrate 0.6415 CYP450 3A4 substrate Substrate 0.6842 CYP450 1A2 substrate Inhibitor 0.9107 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Inhibitor 0.8932 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6424 Ames test AMES toxic 0.6038 Carcinogenicity Non-carcinogens 0.8128 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6763 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8924 hERG inhibition (predictor II) Inhibitor 0.6851
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as quinolones and derivatives. These are compounds containing a quinoline moiety which bears a ketone group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Quinolines and derivatives
- Sub Class
- Quinolones and derivatives
- Direct Parent
- Quinolones and derivatives
- Alternative Parents
- Alkyl aryl ethers / Pyridines and derivatives / Benzenoids / Heteroaromatic compounds / Trialkylamines / Propargyl-type 1,3-dipolar organic compounds / Carboximidic acids / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Quinolone / Alkyl aryl ether / Pyridine / Benzenoid / Heteroaromatic compound / Tertiary amine / Tertiary aliphatic amine / Carboximidic acid / Carboximidic acid derivative / Ether
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- tertiary amino compound, aromatic ether, monocarboxylic acid amide (CHEBI:247956)
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated sodium channel activity
- Specific Function
- Tetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference acro...
- Gene Name
- SCN10A
- Uniprot ID
- Q9Y5Y9
- Uniprot Name
- Sodium channel protein type 10 subunit alpha
- Molecular Weight
- 220623.605 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
- Louro SR, Anteneodo C, Wajnberg E: Carboxyl groups at the membrane interface as molecular targets for local anesthetics. Biophys Chem. 1998 Aug 4;74(1):35-43. [PubMed:9742684]
- Ryan SE, Demers CN, Chew JP, Baenziger JE: Structural effects of neutral and anionic lipids on the nicotinic acetylcholine receptor. An infrared difference spectroscopy study. J Biol Chem. 1996 Oct 4;271(40):24590-7. [PubMed:8798723]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Voltage-gated sodium channel activity involved in sa node cell action potential
- Specific Function
- This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the pr...
- Gene Name
- SCN5A
- Uniprot ID
- Q14524
- Uniprot Name
- Sodium channel protein type 5 subunit alpha
- Molecular Weight
- 226937.475 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
- Oka M, Itoh Y, Fujita T: Halothane attenuates the cerebroprotective action of several Na+ and Ca2+ channel blockers via reversal of their ion channel blockade. Eur J Pharmacol. 2002 Oct 4;452(2):175-81. [PubMed:12354567]
- Louro SR, Anteneodo C, Wajnberg E: Carboxyl groups at the membrane interface as molecular targets for local anesthetics. Biophys Chem. 1998 Aug 4;74(1):35-43. [PubMed:9742684]
- Ryan SE, Demers CN, Chew JP, Baenziger JE: Structural effects of neutral and anionic lipids on the nicotinic acetylcholine receptor. An infrared difference spectroscopy study. J Biol Chem. 1996 Oct 4;271(40):24590-7. [PubMed:8798723]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Titin binding
- Specific Function
- Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number...
- Gene Name
- CALM1
- Uniprot ID
- P0DP23
- Uniprot Name
- Calmodulin
- Molecular Weight
- 16837.47 Da
References
- Muto Y, Kudo S, Nozawa Y: Effects of local anesthetics on calmodulin-dependent guanylate cyclase in the plasma membrane of Tetrahymena pyriformis. Biochem Pharmacol. 1983 Dec 1;32(23):3559-63. [PubMed:6140014]
- Volpi M, Sha'afi RI, Epstein PM, Andrenyak DM, Feinstein MB: Local anesthetics, mepacrine, and propranolol are antagonists of calmodulin. Proc Natl Acad Sci U S A. 1981 Feb;78(2):795-9. [PubMed:6262771]
- Liu SH, Fu WM, Lin-Shiau SY: Studies on the inhibition by chlorpromazine of myotonia induced by ion channel modulators in mouse skeletal muscle. Eur J Pharmacol. 1993 Jan 26;231(1):23-30. [PubMed:7680317]
- Sambandam T, Gunasekaran M: Purification and properties of calmodulin from Phymatotrichum omnivorum. Microbios. 1993;73(294):61-74. [PubMed:8382768]
Enzymes
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Identical protein binding
- Specific Function
- Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
- Gene Name
- BCHE
- Uniprot ID
- P06276
- Uniprot Name
- Cholinesterase
- Molecular Weight
- 68417.575 Da
References
- Elamin B: Dibucaine inhibition of serum cholinesterase. J Biochem Mol Biol. 2003 Mar 31;36(2):149-53. [PubMed:12689511]
Drug created on June 13, 2005 07:24 / Updated on August 15, 2018 09:41