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Identification
NameFospropofol
Accession NumberDB06716  (DB05279)
TypeSmall Molecule
GroupsApproved, Illicit
DescriptionFospropofol is a water soluble prodrug and is converted to propofol in the liver. Fospropofol is a short acting hypnotic/sedative/anesthetic agent. Unlike propofol, does not cause injection-site pain as it is unable to activate TRPA1. FDA approved in December 2008. Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act.
Structure
Thumb
Synonyms
Fospropofol
External Identifiers
  • GPI 15715
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LusedraInjection35 mg/mLIntravenousEisai, Inc2008-12-12Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AquavanNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Fospropofol disodium
258516-87-9
Thumb
  • InChI Key: LWYLQNWMSGFCOZ-UHFFFAOYSA-L
  • Monoisotopic Mass: 332.07654958
  • Average Mass: 332.2403
DBSALT000090
Categories
UNIILZ257RZP7K
CAS number258516-89-1
WeightAverage: 288.2766
Monoisotopic: 288.112660294
Chemical FormulaC13H21O5P
InChI KeyQVNNONOFASOXQV-UHFFFAOYSA-N
InChI
InChI=1S/C13H21O5P/c1-9(2)11-6-5-7-12(10(3)4)13(11)17-8-18-19(14,15)16/h5-7,9-10H,8H2,1-4H3,(H2,14,15,16)
IUPAC Name
[2,6-bis(propan-2-yl)phenoxymethoxy]phosphonic acid
SMILES
CC(C)C1=CC=CC(C(C)C)=C1OCOP(O)(O)=O
Pharmacology
IndicationFor monitored anaesthesia care sedation in patients undergoing diagnostic procedures like bronchoscopy and colonscopy or minor surgical procedures like arthroscopy and bunionectomy.
Structured Indications Not Available
PharmacodynamicsFospropofol is a prodrug of propofol, a sedative hypnotic drug. Unlike propofol, fospropofol is water soluble and can be administered in an aqueous solution. 1.86 mg of fospropofol is the molar equivalent for 1mg of propofol.
Mechanism of actionAfter in-vivo conversion of fospropofol into propofol by endothelial alkaline phosphatase, propofol crosses the blood-brain barrier, binds to GABA-A receptors and acts as an agonist. By binding to GABA-A receptor, it will cause an increase in chloride conductance, thus inhibiting the firing of new action potentials in the post-synaptic neuron.
TargetKindPharmacological actionActionsOrganismUniProt ID
Gamma-aminobutyric acid receptor subunit beta-2Proteinyes
potentiator
HumanP47870 details
Gamma-aminobutyric acid receptor subunit beta-3Proteinyes
potentiator
HumanP28472 details
Related Articles
AbsorptionAdequate sedation achieved after 7 minutes with a IV bolus dose of 10mg/kg. It takes 21-45 minutes for patients to recover for fospropopol-induced sedation. Following an intravenous bolus administration of 6 mg/kg in a healthy subject, the pharmacokinetic parameters of fospropofol are as follows: Cmax = 78.7 μg/mL; Tmax = 4 minutes; AUC(0-∞) = 19.0 μg ⋅ h/mL;
Volume of distribution

Fospropofol = 0.33±0.069 L/kg;
Propofol metabolite = 5.8 L/kg.

Protein bindingBoth fospropofol and its active metabolite propofol are highly protein bound (approximately 98%), primarily to albumin. Fospropofol does not affect the binding of propofol to albumin.
Metabolism

Fospropofol is metabolized into propofol, formaldehyde, and phosphate by endothelial alkaline phosphatase. The metabolite, formaldehyde, is quickly oxidized into formic acid by glutathione dependent and independent dehydrogenases and erythrocytes. Excess formic acid is eliminated via oxidation to carbon dioxide through the tetrahydrofolate pathway. Propofol is further metabolized into propofol glucuronide, quinol-4-sulfate, quinol-1-fluronide, and quinol-4-glucuronide. The cytochrome P450 enzyme system is not involved with the metabolism of fospropofol.

SubstrateEnzymesProduct
Fospropofol
Not Available
Formic acidDetails
Fospropofol
Not Available
FormaldehydeDetails
Fospropofol
Not Available
PhosphateDetails
Fospropofol
Not Available
PropofolDetails
Route of eliminationChiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney. There is negligible renal elimination of unchanged fospropofol (<0.02%).
Half lifeWhen given to a patient, the half-lives are as follows: Fospropofol = 0.81 hours; Propofol metabolite = 1.13 hours
Clearance

Total body clearance (CLp), Fospropofol, healthy subject = 0.28 L/h/kg;
CLp, fospropofol, patients = 0.31 L/h/kg;
CLp/F, propofol, healthy subjects or patients = 2.74 L/h/kg.

ToxicityOverdosage may lead to cardiorespiratory depression, formic acid toxicity (methanol toxicity-like effects), and/or phosphate-induced hypocalemia. Most common adverse reactions (> 20%) are paresthesia and pruritus.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,1,1,2 TetrafluoroethaneThe risk or severity of adverse effects can be increased when Fospropofol is combined with 1,1,1,2 Tetrafluoroethane.Investigational
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Fospropofol.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Fospropofol.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Fospropofol.Approved
adipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with Fospropofol.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Fospropofol.Approved, Investigational
AlfaxaloneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Fospropofol.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Fospropofol.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Fospropofol.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Fospropofol.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Amitriptyline.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Fospropofol.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Fospropofol is combined with Amperozide.Experimental
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Fospropofol.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Fospropofol.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Azaperone.Vet Approved
AzelastineFospropofol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Azelastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Fospropofol is combined with Baclofen.Approved
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Fospropofol.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Fospropofol.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Fospropofol is combined with Benzyl alcohol.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Fospropofol is combined with Brexpiprazole.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Brimonidine.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Fospropofol.Approved, Illicit
BrompheniramineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Fospropofol is combined with Brotizolam.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Fospropofol.Approved, Investigational
BuprenorphineFospropofol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Fospropofol.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Fospropofol.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Fospropofol is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Fospropofol is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Fospropofol.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Fospropofol.Approved, Illicit, Vet Approved
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Fospropofol.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Fospropofol.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Carisoprodol.Approved
CetirizineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Fospropofol.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Fospropofol.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Fospropofol.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Fospropofol.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Chlorphenamine.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Fospropofol.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Fospropofol.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Chlorzoxazone.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Fospropofol.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Fospropofol is combined with Citalopram.Approved
ClemastineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Clemastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Fospropofol is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Fospropofol is combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with Fospropofol.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Fospropofol is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Clonidine.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Fospropofol.Approved, Illicit
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Fospropofol.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Fospropofol.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Fospropofol.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Fospropofol.Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Cyproheptadine.Approved
DantroleneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Fospropofol.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Dapoxetine.Investigational
deramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with Fospropofol.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Fospropofol.Approved
DesipramineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Detomidine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Fospropofol.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Fospropofol.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Fospropofol.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Fospropofol.Approved
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Fospropofol.Approved, Illicit, Vet Approved
DifenoxinThe risk or severity of adverse effects can be increased when Fospropofol is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Fospropofol.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Fospropofol.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Fospropofol.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Fospropofol is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Fospropofol.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Fospropofol.Approved, Illicit
DoramectinThe risk or severity of adverse effects can be increased when Fospropofol is combined with Doramectin.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Fospropofol is combined with Doxepin.Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Fospropofol is combined with DPDPE.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Fospropofol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Fospropofol.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Fospropofol.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Fospropofol.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Fospropofol is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Fospropofol is combined with Efavirenz.Approved, Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Fospropofol.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Fospropofol is combined with Entacapone.Approved, Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Fospropofol is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Fospropofol.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Fospropofol.Approved
EthanolFospropofol may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Fospropofol.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Fospropofol is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Fospropofol is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Fospropofol.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Fospropofol.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Fospropofol.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Etifoxine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Fospropofol is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Fospropofol.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Fospropofol.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Fospropofol is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Fospropofol.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Fospropofol.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Fexofenadine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Fospropofol is combined with Flibanserin.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Fospropofol.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Fospropofol.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Fospropofol.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Fospropofol.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Fospropofol.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Fospropofol.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fospropofol is combined with Fluticasone Propionate.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Fospropofol.Approved, Investigational
FosphenytoinThe risk or severity of adverse effects can be increased when Fospropofol is combined with Fosphenytoin.Approved
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Fospropofol.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Fospropofol is combined with gabapentin enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Fospropofol.Approved, Illicit
GepironeThe risk or severity of adverse effects can be increased when Fospropofol is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Fospropofol.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Fospropofol.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Fospropofol.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Fospropofol.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Fospropofol.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Fospropofol.Approved
HydrocodoneFospropofol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Fospropofol.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Iloperidone.Approved
ImipramineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Imipramine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Indalpine.Investigational, Withdrawn
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Fospropofol.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Fospropofol.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Fospropofol.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Ketobemidone.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Lamotrigine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Fospropofol is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Fospropofol.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Fospropofol is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Fospropofol.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Fospropofol is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Fospropofol.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Fospropofol.Approved, Vet Approved
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Fospropofol.Approved
LofentanilThe risk or severity of adverse effects can be increased when Fospropofol is combined with Lofentanil.Illicit
LoratadineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Fospropofol.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Fospropofol.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Lu AA21004 is combined with Fospropofol.Investigational
LurasidoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Lurasidone.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Maprotiline.Approved
MeclizineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Meclizine.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Medetomidine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Fospropofol.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Melperone.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Fospropofol.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Fospropofol.Approved, Illicit
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Fospropofol.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Metaxalone.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Fospropofol.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Fospropofol.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Fospropofol.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Fospropofol.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Fospropofol.Approved
MethotrimeprazineFospropofol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Fospropofol.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Fospropofol is combined with Methsuximide.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Fospropofol.Approved
MetyrosineFospropofol may increase the sedative activities of Metyrosine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Fospropofol.Approved, Illicit
MilnacipranThe risk or severity of adverse effects can be increased when Fospropofol is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved, Investigational
MirtazapineFospropofol may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Fospropofol.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Fospropofol.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Fospropofol.Approved
NefazodoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Nefazodone.Approved, Withdrawn
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Fospropofol.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Fospropofol.Approved, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Nortriptyline.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Fospropofol.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Olopatadine.Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Fospropofol.Approved
OpiumThe risk or severity of adverse effects can be increased when Fospropofol is combined with Opium.Approved, Illicit
OrphenadrineFospropofol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Fospropofol.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Fospropofol.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Fospropofol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Fospropofol.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Fospropofol.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Fospropofol.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Fospropofol.Approved
ParaldehydeFospropofol may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Paroxetine.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Fospropofol.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Fospropofol.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved
PerazineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Fospropofol is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Fospropofol.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Fospropofol.Approved
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Fospropofol.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Phenoxyethanol.Approved
PhenytoinThe risk or severity of adverse effects can be increased when Fospropofol is combined with Phenytoin.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Fospropofol.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Pipotiazine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Fospropofol is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Fospropofol is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Fospropofol is combined with Pomalidomide.Approved
PramipexoleFospropofol may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Fospropofol.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Fospropofol.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Pregnanolone.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Fospropofol.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Fospropofol is combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Fospropofol.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Fospropofol.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Fospropofol.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Promethazine.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Fospropofol.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Fospropofol.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Propoxycaine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Protriptyline.Approved
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with Fospropofol.Investigational
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Fospropofol.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Fospropofol.Approved
RacloprideThe risk or severity of adverse effects can be increased when Fospropofol is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Fospropofol is combined with Ramelteon.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Fospropofol.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Fospropofol.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Fospropofol.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Fospropofol.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Fospropofol is combined with Ritanserin.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Romifidine.Vet Approved
RopiniroleFospropofol may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Fospropofol.Approved
RotigotineFospropofol may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fospropofol.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Fospropofol.Experimental
Sage 547The risk or severity of adverse effects can be increased when Fospropofol is combined with Sage 547.Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Scopolamine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Fospropofol.Approved, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Fospropofol.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Fospropofol.Approved, Vet Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved
StiripentolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Fospropofol.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Fospropofol.Approved
SuvorexantFospropofol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tasimelteon.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Fospropofol.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tetracaine.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Fospropofol.Investigational
ThalidomideFospropofol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Fospropofol.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Fospropofol.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Fospropofol.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Fospropofol.Approved
TiagabineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tiapride.Investigational
TiletamineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tiletamine.Vet Approved
TizanidineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tizanidine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tolcapone.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Fospropofol is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Fospropofol.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Fospropofol.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Fospropofol.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Fospropofol.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Fospropofol.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Fospropofol.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Fospropofol.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Triprolidine.Approved
Uc1010The risk or severity of adverse effects can be increased when Fospropofol is combined with Uc1010.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Fospropofol.Approved, Investigational
VenlafaxineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Venlafaxine.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Fospropofol is combined with Vigabatrin.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Vortioxetine.Approved
XylazineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Xylazine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Fospropofol.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Fospropofol is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Zimelidine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Fospropofol.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Fospropofol is combined with Zolazepam.Vet Approved
ZolpidemFospropofol may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Fospropofol is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Fospropofol.Approved
ZotepineThe risk or severity of adverse effects can be increased when Fospropofol is combined with Zotepine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Fospropofol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Garnock-Jones KP, Scott LJ: Fospropofol. Drugs. 2010 Mar 5;70(4):469-77. doi: 10.2165/11204450-000000000-00000. [PubMed:20205488 ]
  2. Schywalsky M, Ihmsen H, Tzabazis A, Fechner J, Burak E, Vornov J, Schwilden H: Pharmacokinetics and pharmacodynamics of the new propofol prodrug GPI 15715 in rats. Eur J Anaesthesiol. 2003 Mar;20(3):182-90. [PubMed:12650488 ]
  3. Bengalorkar GM, Bhuvana K, Sarala N, Kumar T: Fospropofol: clinical pharmacology. J Anaesthesiol Clin Pharmacol. 2011 Jan;27(1):79-83. [PubMed:21804712 ]
  4. Patwardhan A, Edelmayer R, Annabi E, Price T, Malan P, Dussor G: Receptor specificity defines algogenic properties of propofol and fospropofol. Anesth Analg. 2012 Oct;115(4):837-40. Epub 2012 May 14. [PubMed:22584560 ]
External Links
ATC CodesNot Available
AHFS Codes
  • 28:04.92
PDB EntriesNot Available
FDA labelDownload (536 KB)
MSDSDownload (479 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.5105
Blood Brain Barrier+0.8462
Caco-2 permeable-0.546
P-glycoprotein substrateNon-substrate0.6735
P-glycoprotein inhibitor INon-inhibitor0.8244
P-glycoprotein inhibitor IINon-inhibitor0.9747
Renal organic cation transporterNon-inhibitor0.9124
CYP450 2C9 substrateNon-substrate0.8021
CYP450 2D6 substrateNon-substrate0.8086
CYP450 3A4 substrateNon-substrate0.5052
CYP450 1A2 substrateNon-inhibitor0.7667
CYP450 2C9 inhibitorNon-inhibitor0.7807
CYP450 2D6 inhibitorNon-inhibitor0.9205
CYP450 2C19 inhibitorNon-inhibitor0.7375
CYP450 3A4 inhibitorNon-inhibitor0.8538
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8754
Ames testNon AMES toxic0.7212
CarcinogenicityNon-carcinogens0.6902
BiodegradationNot ready biodegradable0.7478
Rat acute toxicity2.3516 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8892
hERG inhibition (predictor II)Non-inhibitor0.926
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
InjectionIntravenous35 mg/mL
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6204257 No2002-07-012022-07-01Us
US6872838 No1998-08-072018-08-07Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
pKa8.2 - 9.0FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.302 mg/mLALOGPS
logP2.23ALOGPS
logP3.6ChemAxon
logS-3ALOGPS
pKa (Strongest Acidic)1.44ChemAxon
pKa (Strongest Basic)-5ChemAxon
Physiological Charge-2ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.99 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity72.88 m3·mol-1ChemAxon
Polarizability29 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as cumenes. These are aromatic compounds containing a prop-2-ylbenzene moiety.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassCumenes
Direct ParentCumenes
Alternative Parents
Substituents
  • Phenylpropane
  • Cumene
  • Phenol ether
  • Monoalkyl phosphate
  • Alkyl phosphate
  • Phosphoric acid ester
  • Organic phosphoric acid derivative
  • Organic phosphate
  • Hydrocarbon derivative
  • Organooxygen compound
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
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.
Gene Name:
GABRB2
Uniprot ID:
P47870
Molecular Weight:
59149.895 Da
References
  1. Franks NP: Molecular targets underlying general anaesthesia. Br J Pharmacol. 2006 Jan;147 Suppl 1:S72-81. [PubMed:16402123 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Gaba-gated chloride 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.
Gene Name:
GABRB3
Uniprot ID:
P28472
Molecular Weight:
54115.04 Da
References
  1. Franks NP: Molecular targets underlying general anaesthesia. Br J Pharmacol. 2006 Jan;147 Suppl 1:S72-81. [PubMed:16402123 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
substrate
General Function:
Pyrophosphatase activity
Specific Function:
This isozyme may play a role in skeletal mineralization.
Gene Name:
ALPL
Uniprot ID:
P05186
Molecular Weight:
57304.435 Da
References
  1. Bergese SD, Dalal P, Vandse R, Satlin A, Lin Z, Candiotti K, Cohen L, Gan TJ: A double-blind, randomized, multicenter, dose-ranging study to evaluate the safety and efficacy of fospropofol disodium as an intravenous sedative for colonoscopy in high-risk populations. Am J Ther. 2013 Mar-Apr;20(2):163-71. doi: 10.1097/MJT.0b013e318256ecfc. [PubMed:22820718 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
Comments
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Drug created on May 16, 2010 17:53 / Updated on December 07, 2016 02:39