Butabarbital - DrugBank

ID Pharmacology Interactions References Trials Economics Properties Spectra Taxonomy

Targets (5)

Targets (5)Biointeractions (5)

Identification

Name

Butabarbital

Accession Number

DB00237 (APRD00752)

Type

Small Molecule

Groups

Approved, Illicit

Description

Butabarbital (trade name Butisol) is a prescription barbiturate sleep aid. Butabarbital has a particularly fast onset of effects and short duration of action compared to other barbiturates, which makes it useful for certain applications such as treating severe insomnia and relieving anxiety before surgical procedures; however it is also relatively dangerous particularly when combined with alcohol, and so is now rarely used, although it is still prescribed in some Eastern European and South American countries. Its short duration of action gives butabarbital a high abuse potential, comparable to secobarbital. [Wikipedia]

Structure

MOL SDF 3D-SDF PDB SMILES InChI View 3D Structure

Synonyms

5-Ethyl-5-(1-methylpropyl)-2,4,6(1H,3H,5H)-pyrimidinetrione

5-Ethyl-5-(1-methylpropyl)barbituric acid

5-Sec-butyl-5-ethyl-2,4,6(1H,3H,5H)-pyrimidinetrione

5-Sec-butyl-5-ethylbarbituric acid

5-Sec-butyl-5-ethylpyrimidine-2,4,6(1H,3H,5H)-trione

Butabarbital

Butisol

Secbutabarbital

External IDs

Not Available

Product Ingredients

Ingredient	UNII	CAS	InChI Key	Details
Butabarbital Sodium	9WTD50I918	143-81-7	QORQZMBCPRBCAB-UHFFFAOYNA-M	Details

Approved Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Butisol Sodium	Tablet	30 mg/1	Oral	Meda Pharmaceuticals Ltd	1939-08-01	Not applicable	US
Butisol Sodium Tab 100mg	Tablet	100 mg	Oral	Carter Horner Corp.	1982-12-31	2001-01-02	Canada
Butisol Sodium Tab 15mg	Tablet	15 mg	Oral	Carter Horner Corp.	1982-12-31	2001-01-02	Canada
Butisol Sodium Tab 30mg	Tablet	30 mg	Oral	Carter Horner Corp.	1982-12-31	2001-01-02	Canada

Approved Generic Prescription Products

Not Available

Approved Over the Counter Products

Not Available

Unapproved/Other Products

Not Available

International Brands

Name	Company
Butalan	Not Available
Butisol	Not Available
Sarisol No. 2	Not Available

Brand mixtures

Not Available

Categories

UNII

P0078O25A9

CAS number

125-40-6

Weight

Average: 212.2456
Monoisotopic: 212.116092388

Chemical Formula

C₁₀H₁₆N₂O₃

InChI Key

ZRIHAIZYIMGOAB-UHFFFAOYSA-N

InChI

InChI=1S/C10H16N2O3/c1-4-6(3)10(5-2)7(13)11-9(15)12-8(10)14/h6H,4-5H2,1-3H3,(H2,11,12,13,14,15)

IUPAC Name

5-(butan-2-yl)-5-ethyl-1,3-diazinane-2,4,6-trione

SMILES

CCC(C)C1(CC)C(=O)NC(=O)NC1=O

Pharmacology

Indication

For short-term treatment of insomnia and anxiety disorders

Structured Indications

Sleeplessness

Pharmacodynamics

Butabarbital, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.

Mechanism of action

Butabarbital binds at a distinct binding site associated with a Cl^- ionopore at the GABA_A receptor, increasing the duration of time for which the Cl^- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.

Target	Kind	Pharmacological action	Actions	Organism	UniProt ID
GABA-A receptor (anion channel)	Protein group	yes	positive allosteric modulator	Human	not applicable	details
Neuronal acetylcholine receptor subunit alpha-4	Protein	unknown	antagonist	Human	P43681	details
Neuronal acetylcholine receptor subunit alpha-7	Protein	unknown	antagonist	Human	P36544	details
Glutamate receptor 2	Protein	unknown	antagonist	Human	P42262	details
Glutamate receptor ionotropic, kainate 2	Protein	unknown	antagonist	Human	Q13002	details

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Barbiturates are metabolized primarily by the hepatic microsomal enzyme system, and most metabolic products are excreted in the urine.

Half life

Not Available

Clearance

Not Available

Toxicity

Signs of overdose include confusion (severe), decrease in or loss of reflexes, drowsiness (severe), fever, irritability (continuing), low body temperature, poor judgment, shortness of breath or slow or troubled breathing, slow heartbeat, slurred speech, staggering, trouble in sleeping, unusual movements of the eyes, weakness (severe).

Affected organisms

Humans and other mammals

Pathways

Not Available

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

Food Interactions

Not Available

References

Synthesis Reference

Not Available

General References

Not Available

External Links

Resource	Link
Human Metabolome Database (HMDB)	HMDB14382
KEGG Drug	D03180
KEGG Compound	C07827
PubChem Compound	2479
PubChem Substance	46505051
ChemSpider	2385
ChEBI	3228
ChEMBL	CHEMBL449
Therapeutic Targets Database	DAP000667
PharmGKB	PA164743463
Drug Product Database	8245
Drugs.com	http://www.drugs.com/cdi/butabarbital.html
Wikipedia	Butabarbital

ATC Codes

Not Available

AHFS Codes

Not Available

PDB Entries

Not Available

FDA label

Not Available

MSDS

Not Available

Clinical Trials

Not Available

Pharmacoeconomics

Manufacturers

Medpointe pharmaceuticals medpointe healthcare inc
Alpharma us pharmaceuticals division
Wockhardt eu operations (swiss) ag
Lannett co inc
Meda pharmaceuticals inc
Halsey drug co inc
Cm bundy co
Sandoz inc
Solvay pharmaceuticals
Teva pharmaceuticals usa inc
Watson laboratories inc
Whiteworth towne paulsen inc
Ivax pharmaceuticals inc sub teva pharmaceuticals usa
Marshall pharmacal corp
West ward pharmaceutical corp

Packagers

C.O. Truxton Inc.
Chattem Chemicals Inc.
Meda AB

Dosage forms

Form	Route	Strength
Tablet	Oral	30 mg/1
Tablet	Oral	100 mg
Tablet	Oral	15 mg
Tablet	Oral	30 mg

Prices

Unit description	Cost	Unit
Butisol sodium 50 mg tablet	2.46USD	tablet
Butisol sodium 30 mg tablet	1.89USD	tablet

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)	166.5 °C	PhysProp
water solubility	1360 mg/L	Not Available
logP	1.65	WONG,O & MCKEOWN,RH (1988)

Predicted Properties

Property	Value	Source
Water Solubility	1.39 mg/mL	ALOGPS
logP	1.7	ALOGPS
logP	1.45	ChemAxon
logS	-2.2	ALOGPS
pKa (Strongest Acidic)	8.48	ChemAxon
Physiological Charge	0	ChemAxon
Hydrogen Acceptor Count	3	ChemAxon
Hydrogen Donor Count	2	ChemAxon
Polar Surface Area	75.27 Å²	ChemAxon
Rotatable Bond Count	3	ChemAxon
Refractivity	53.4 m³·mol^-1	ChemAxon
Polarizability	21.41 Å³	ChemAxon
Number of Rings	1	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	+	0.9324
Blood Brain Barrier	+	0.9782
Caco-2 permeable	-	0.6013
P-glycoprotein substrate	Substrate	0.5938
P-glycoprotein inhibitor I	Non-inhibitor	0.617
P-glycoprotein inhibitor II	Non-inhibitor	0.961
Renal organic cation transporter	Non-inhibitor	0.9465
CYP450 2C9 substrate	Non-substrate	0.7719
CYP450 2D6 substrate	Non-substrate	0.9014
CYP450 3A4 substrate	Non-substrate	0.7098
CYP450 1A2 substrate	Non-inhibitor	0.8775
CYP450 2C9 inhibitor	Non-inhibitor	0.821
CYP450 2D6 inhibitor	Non-inhibitor	0.933
CYP450 2C19 inhibitor	Non-inhibitor	0.7828
CYP450 3A4 inhibitor	Non-inhibitor	0.9203
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.9458
Ames test	Non AMES toxic	0.6458
Carcinogenicity	Non-carcinogens	0.8533
Biodegradation	Not ready biodegradable	0.9759
Rat acute toxicity	3.6803 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.99
hERG inhibition (predictor II)	Non-inhibitor	0.9233

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
MS	Mass Spectrum (Electron Ionization)	splash10-0a4l-6900000000-6e0cbc3d26c5541ad8eb	View in MoNA

Taxonomy

Description

This compound belongs to the class of chemical entities known as barbituric acid derivatives. These are compounds containing a perhydropyrimidine ring substituted at C-2, -4 and -6 by oxo groups.

Kingdom

Chemical entities

Super Class

Organic compounds

Class

Organoheterocyclic compounds

Sub Class

Diazines

Direct Parent

Barbituric acid derivatives

Alternative Parents

Ureides / Diazinanes / Dicarboximides / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds

Substituents

Barbiturate / Ureide / 1,3-diazinane / Dicarboximide / Urea / Azacycle / Carboxylic acid derivative / Organic oxide / Organooxygen compound / Organonitrogen compound

Molecular Framework

Aliphatic heteromonocyclic compounds

External Descriptors

barbiturates (CHEBI:3228 )

Targets

Details

1. GABA-A receptor (anion channel) (Protein Group)

Kind: Protein group
Organism: Human
Pharmacological action: yes
Actions: positive allosteric modulator

General Function:: Inhibitory extracellular ligand-gated ion channel activity
Specific Function:: Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).

Components:

Name	UniProt ID	Details
Gamma-aminobutyric acid receptor subunit alpha-1	P14867	Details
Gamma-aminobutyric acid receptor subunit alpha-2	P47869	Details
Gamma-aminobutyric acid receptor subunit alpha-3	P34903	Details
Gamma-aminobutyric acid receptor subunit alpha-4	P48169	Details
Gamma-aminobutyric acid receptor subunit alpha-5	P31644	Details
Gamma-aminobutyric acid receptor subunit alpha-6	Q16445	Details
Gamma-aminobutyric acid receptor subunit beta-1	P18505	Details
Gamma-aminobutyric acid receptor subunit beta-2	P47870	Details
Gamma-aminobutyric acid receptor subunit beta-3	P28472	Details
Gamma-aminobutyric acid receptor subunit delta	O14764	Details
Gamma-aminobutyric acid receptor subunit epsilon	P78334	Details
Gamma-aminobutyric acid receptor subunit gamma-1	Q8N1C3	Details
Gamma-aminobutyric acid receptor subunit gamma-2	P18507	Details
Gamma-aminobutyric acid receptor subunit gamma-3	Q99928	Details
Gamma-aminobutyric acid receptor subunit pi	O00591	Details
Gamma-aminobutyric acid receptor subunit theta	Q9UN88	Details

References

Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]

Details

2. Neuronal acetylcholine receptor subunit alpha-4

Kind: Protein
Organism: Human
Pharmacological action: unknown
Actions: antagonist

General Function:: Ligand-gated ion channel activity
Specific Function:: After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeable to sodium ions.
Gene Name:: CHRNA4
Uniprot ID:: P43681
Uniprot Name:: Neuronal acetylcholine receptor subunit alpha-4
Molecular Weight:: 69956.47 Da

References

Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [PubMed:16248797 ]
Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]

Details

3. Neuronal acetylcholine receptor subunit alpha-7

Kind: Protein
Organism: Human
Pharmacological action: unknown
Actions: antagonist

General Function:: Toxic substance binding
Specific Function:: After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin.
Gene Name:: CHRNA7
Uniprot ID:: P36544
Uniprot Name:: Neuronal acetylcholine receptor subunit alpha-7
Molecular Weight:: 56448.925 Da

References

Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [PubMed:16248797 ]
Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]

Details

4. Glutamate receptor 2

Kind: Protein
Organism: Human
Pharmacological action: unknown
Actions: antagonist

General Function:: Ionotropic glutamate receptor activity
Specific Function:: Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and t...
Gene Name:: GRIA2
Uniprot ID:: P42262
Uniprot Name:: Glutamate receptor 2
Molecular Weight:: 98820.32 Da

References

Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]

Details

5. Glutamate receptor ionotropic, kainate 2

Kind: Protein
Organism: Human
Pharmacological action: unknown
Actions: antagonist

General Function:: Kainate selective glutamate receptor activity
Specific Function:: Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inacti...
Gene Name:: GRIK2
Uniprot ID:: Q13002
Uniprot Name:: Glutamate receptor ionotropic, kainate 2
Molecular Weight:: 102582.475 Da

References

Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]

Drug created on June 13, 2005 07:24 / Updated on July 18, 2017 16:47

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Structure for DB00237 (Butabarbital)

Targets

Components:

References

References

References

References

References