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Identification
NamePentobarbital
Accession NumberDB00312  (APRD01174)
TypeSmall Molecule
GroupsApproved
Description

A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236)

Structure
Thumb
Synonyms
SynonymLanguageCode
5-Ethyl-5-(1-methyl-butyl)-pyrimidine-2,4,6-trioneNot AvailableNot Available
5-Ethyl-5-(1-methylbutyl)-2,4,6(1H,3H,5H)-pyrimidinetrioneNot AvailableNot Available
5-ethyl-5-(1-methylbutyl)barbituric acidNot AvailableNot Available
5-ethyl-5-(sec-pentyl)barbituric acidNot AvailableNot Available
NembutalNot AvailableNot Available
PentobarbitalNot AvailableNot Available
PentobarbitoneNot AvailableNot Available
Prescription ProductsNot Available
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
NembutalLundbeck
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Pentobarbital Sodium
Thumb
  • InChI Key: QGMRQYFBGABWDR-UHFFFAOYNA-M
  • Monoisotopic Mass: 248.113687095
  • Average Mass: 248.254
DBSALT000442
Categories
CAS number76-74-4
WeightAverage: 226.2722
Monoisotopic: 226.131742452
Chemical FormulaC11H18N2O3
InChI KeyWEXRUCMBJFQVBZ-UHFFFAOYSA-N
InChI
InChI=1S/C11H18N2O3/c1-4-6-7(3)11(5-2)8(14)12-10(16)13-9(11)15/h7H,4-6H2,1-3H3,(H2,12,13,14,15,16)
IUPAC Name
5-ethyl-5-(pentan-2-yl)-1,3-diazinane-2,4,6-trione
SMILES
CCCC(C)C1(CC)C(=O)NC(=O)NC1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as barbituric acid derivatives. These are compounds containing a perhydropyrimidine ring substituted at C-2, -4 and -6 by oxo groups.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazines
Sub ClassPyrimidines and pyrimidine derivatives
Direct ParentBarbituric acid derivatives
Alternative Parents
Substituents
  • Barbiturate
  • Ureide
  • 1,3-diazinane
  • Urea
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the short-term treatment of insomnia.
PharmacodynamicsPentobarbital, 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 actionPentobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA 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.
AbsorptionBarbiturates are absorbed in varying degrees following oral, rectal, or parenteral administration.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

by hepatic microsomal enzyme system

Route of eliminationBarbiturates are metabolized primarily by the hepatic microsomal enzyme system, and the metabolic products are excreted in the urine, and less commonly, in the feces. Approximately 25 to 50 percent of a dose of aprobarbital or phenobarbital is eliminated unchanged in the urine, whereas the amount of other barbiturates excreted unchanged in the urine is negligible.
Half life5 to 50 hours (dose dependent)
ClearanceNot Available
ToxicitySymptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9156
Blood Brain Barrier+0.9713
Caco-2 permeable-0.5926
P-glycoprotein substrateSubstrate0.5947
P-glycoprotein inhibitor INon-inhibitor0.6155
P-glycoprotein inhibitor IINon-inhibitor0.9218
Renal organic cation transporterNon-inhibitor0.923
CYP450 2C9 substrateNon-substrate0.7789
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateNon-substrate0.7066
CYP450 1A2 substrateNon-inhibitor0.9086
CYP450 2C9 substrateNon-inhibitor0.7484
CYP450 2D6 substrateNon-inhibitor0.9301
CYP450 2C19 substrateNon-inhibitor0.711
CYP450 3A4 substrateNon-inhibitor0.9522
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9276
Ames testNon AMES toxic0.6789
CarcinogenicityNon-carcinogens0.89
BiodegradationNot ready biodegradable0.9603
Rat acute toxicity3.2266 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9685
hERG inhibition (predictor II)Non-inhibitor0.8771
Pharmacoeconomics
Manufacturers
  • Ovation pharmaceuticals inc
  • Lannett co inc
  • Vitarine pharmaceuticals inc
  • Whiteworth towne paulsen inc
  • Anabolic inc
  • Elkins sinn div ah robins co inc
  • Everylife
  • Halsey drug co inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Parke davis div warner lambert co
  • L perrigo co
  • Purepac pharmaceutical co
  • Valeant pharmaceuticals international
  • Watson laboratories inc
  • Wyeth ayerst laboratories
  • Lundbeck inc
  • Nexgen pharma inc
Packagers
Dosage formsNot Available
Prices
Unit descriptionCostUnit
Pentobarbital sodium powder27.0USD g
Nembutal sodium 50 mg/ml via20.65USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point129.5 °CPhysProp
water solubility679 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.10HANSCH,C ET AL. (1995)
logS-2.52ADME Research, USCD
pKa8.11 (at 25 °C)SERJEANT,EP & DEMPSEY,B (1979)
Predicted Properties
PropertyValueSource
Water Solubility0.864 mg/mLALOGPS
logP2.16ALOGPS
logP1.89ChemAxon
logS-2.4ALOGPS
pKa (Strongest Acidic)8.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.27 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity58 m3·mol-1ChemAxon
Polarizability23.41 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.77 KB)
SpectraMS/MSMS
References
Synthesis ReferenceNot Available
General Reference
  1. Knodell RG, Spector MH, Brooks DA, Keller FX, Kyner WT: Alterations in pentobarbital pharmacokinetics in response to parenteral and enteral alimentation in the rat. Gastroenterology. 1980 Dec;79(6):1211-6. Pubmed
External Links
ATC CodesN05CA01
AHFS Codes
  • 28:24.04
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (50.3 KB)
Interactions
Drug Interactions
Drug
AcebutololMay decrease the serum concentration of Beta-Blockers.
AcenocoumarolMay increase the metabolism of Vitamin K Antagonists.
AcetaminophenBarbiturates may increase the metabolism of Acetaminophen. This may 1) diminish the effect of acetaminophen; and 2) increase the risk of liver damage.
AcetazolamideMay enhance the hypotensive effect of Hypotensive Agents.
AldesleukinMay enhance the hypotensive effect of Hypotensive Agents.
AliskirenMay enhance the hypotensive effect of Hypotensive Agents.
AmilorideMay enhance the hypotensive effect of Hypotensive Agents.
AminophyllineMay decrease the serum concentration of Theophylline Derivatives.
AmitriptylineMay increase the metabolism of Tricyclic Antidepressants.
AmlodipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
AmoxapineMay increase the metabolism of Tricyclic Antidepressants.
AmrinoneBarbiturates may increase the metabolism of Calcium Channel Blockers.
Amyl NitriteMay enhance the hypotensive effect of Hypotensive Agents.
ApraclonidineMay enhance the hypotensive effect of Hypotensive Agents.
AtenololMay enhance the hypotensive effect of Hypotensive Agents.
Azilsartan medoxomilMay enhance the orthostatic hypotensive effect of Thiazide Diuretics.
BenazeprilMay enhance the hypotensive effect of Hypotensive Agents.
BendroflumethiazideMay enhance the orthostatic hypotensive effect of Thiazide Diuretics.
BepridilBarbiturates may increase the metabolism of Calcium Channel Blockers.
BetaxololMay decrease the serum concentration of Beta-Blockers.
BisoprololMay decrease the serum concentration of Beta-Blockers.
BretyliumMay enhance the hypotensive effect of Hypotensive Agents.
BrimonidineMay enhance the hypotensive effect of Hypotensive Agents.
BumetanideMay enhance the hypotensive effect of Hypotensive Agents.
BuprenorphineCNS Depressants may enhance the CNS depressant effect of Buprenorphine.
ButalbitalMay increase the metabolism of Acetaminophen. This may 1) diminish the effect of acetaminophen; and 2) increase the risk of liver damage.
CanagliflozinMay enhance the hypotensive effect of Hypotensive Agents.
CandesartanMay enhance the hypotensive effect of Hypotensive Agents.
CaptoprilMay enhance the hypotensive effect of Hypotensive Agents.
CarteololMay decrease the serum concentration of Beta-Blockers.
CarvedilolMay decrease the serum concentration of Beta-Blockers.
ChloramphenicolBarbiturates may increase the metabolism of Chloramphenicol. Chloramphenicol may decrease the metabolism of Barbiturates.
ChlorothiazideMay enhance the orthostatic hypotensive effect of Thiazide Diuretics.
ChlorthalidoneMay enhance the orthostatic hypotensive effect of Thiazide Diuretics.
CilazaprilMay enhance the hypotensive effect of Hypotensive Agents.
ClevidipineMay enhance the hypotensive effect of Hypotensive Agents.
ClomipramineMay increase the metabolism of Tricyclic Antidepressants.
ClonidineMay enhance the hypotensive effect of Hypotensive Agents.
DapagliflozinMay enhance the hypotensive effect of Hypotensive Agents.
DesipramineMay increase the metabolism of Tricyclic Antidepressants.
DesogestrelMay diminish the therapeutic effect of Contraceptives (Estrogens). Contraceptive failure is possible.
DihydrocodeineMay increase the metabolism of Acetaminophen. This may 1) diminish the effect of acetaminophen; and 2) increase the risk of liver damage.
DiltiazemMay increase the metabolism of Calcium Channel Blockers.
DipyridamoleMay enhance the hypotensive effect of Hypotensive Agents.
DoxazosinMay enhance the hypotensive effect of Hypotensive Agents.
DoxycyclineMay decrease the serum concentration of Doxycycline.
DoxylamineMay enhance the CNS depressant effect of CNS Depressants.
DronabinolMay enhance the CNS depressant effect of CNS Depressants.
DroperidolMay enhance the CNS depressant effect of CNS Depressants.
DrospirenoneMay diminish the therapeutic effect of Contraceptives (Progestins). Contraceptive failure is possible.
EmpagliflozinMay enhance the hypotensive effect of Hypotensive Agents.
EnalaprilMay enhance the hypotensive effect of Hypotensive Agents.
EplerenoneMay enhance the hypotensive effect of Hypotensive Agents.
EprosartanMay enhance the hypotensive effect of Hypotensive Agents.
EsmololMay decrease the serum concentration of Beta-Blockers.
Ethacrynic acidMay enhance the hypotensive effect of Hypotensive Agents.
Ethinyl EstradiolMay diminish the therapeutic effect of Contraceptives (Estrogens). Contraceptive failure is possible.
EthynodiolMay diminish the therapeutic effect of Contraceptives (Estrogens). Contraceptive failure is possible.
EtonogestrelMay diminish the therapeutic effect of Contraceptives (Progestins). Contraceptive failure is possible.
EtoposideBarbiturates may decrease the serum concentration of Etoposide.
FelbamateBarbiturates may decrease the serum concentration of Felbamate. Felbamate may increase the serum concentration of Barbiturates.
FelodipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
FlunarizineBarbiturates may increase the metabolism of Calcium Channel Blockers.
FosinoprilMay enhance the hypotensive effect of Hypotensive Agents.
FurosemideMay enhance the hypotensive effect of Hypotensive Agents.
GabapentinBarbiturates may increase the metabolism of Calcium Channel Blockers.
GriseofulvinBarbiturates may decrease the serum concentration of Griseofulvin.
GuanfacineMay enhance the hypotensive effect of Hypotensive Agents.
HydralazineMay enhance the hypotensive effect of Hypotensive Agents.
HydrochlorothiazideMay enhance the orthostatic hypotensive effect of Thiazide Diuretics.
HydrocodoneCNS Depressants may enhance the CNS depressant effect of Hydrocodone.
HydroxyzineMay enhance the CNS depressant effect of Barbiturates.
ImipramineMay increase the metabolism of Tricyclic Antidepressants.
IndapamideMay enhance the orthostatic hypotensive effect of Thiazide Diuretics.
IrbesartanMay enhance the hypotensive effect of Hypotensive Agents.
IsomethepteneMay increase the metabolism of Acetaminophen. This may 1) diminish the effect of acetaminophen; and 2) increase the risk of liver damage.
Isosorbide DinitrateMay enhance the hypotensive effect of Hypotensive Agents.
Isosorbide MononitrateMay enhance the hypotensive effect of Hypotensive Agents.
IsoxsuprineMay enhance the hypotensive effect of Hypotensive Agents.
IsradipineMay increase the metabolism of Calcium Channel Blockers.
LabetalolMay decrease the serum concentration of Beta-Blockers.
LamotrigineBarbiturates may increase the metabolism of Calcium Channel Blockers.
LercanidipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
LevobunololMay enhance the hypotensive effect of Hypotensive Agents.
LevonorgestrelMay diminish the therapeutic effect of Contraceptives (Progestins). Contraceptive failure is possible.
LisinoprilMay enhance the hypotensive effect of Hypotensive Agents.
LosartanMay enhance the hypotensive effect of Hypotensive Agents.
Magnesium SulfateBarbiturates may increase the metabolism of Calcium Channel Blockers.
MannitolMay enhance the hypotensive effect of Hypotensive Agents.
Medroxyprogesterone AcetateMay diminish the therapeutic effect of Contraceptives (Progestins). Contraceptive failure is possible.
MefloquineMay diminish the therapeutic effect of Anticonvulsants. Mefloquine may decrease the serum concentration of Anticonvulsants.
MestranolMay diminish the therapeutic effect of Contraceptives (Estrogens). Contraceptive failure is possible.
MethazolamideMay enhance the hypotensive effect of Hypotensive Agents.
MethotrimeprazineCNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants.
MethyclothiazideMay enhance the orthostatic hypotensive effect of Thiazide Diuretics.
MethyldopaMay enhance the hypotensive effect of Hypotensive Agents.
MetipranololMay enhance the hypotensive effect of Hypotensive Agents.
MetolazoneMay enhance the orthostatic hypotensive effect of Thiazide Diuretics.
MetoprololMay decrease the serum concentration of Beta-Blockers.
MetyrosineCNS Depressants may enhance the sedative effect of Metyrosine.
MianserinMay enhance the CNS depressant effect of Barbiturates. Mianserin may diminish the therapeutic effect of Barbiturates. Barbiturates may decrease the serum concentration of Mianserin.
MirtazapineCNS Depressants may enhance the CNS depressant effect of Mirtazapine.
MoexiprilMay enhance the hypotensive effect of Hypotensive Agents.
NabiloneMay enhance the CNS depressant effect of CNS Depressants.
NadololMay enhance the hypotensive effect of Hypotensive Agents.
NebivololMay decrease the serum concentration of Beta-Blockers.
NesiritideMay enhance the hypotensive effect of Hypotensive Agents.
NicardipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
NifedipineMay increase the metabolism of Calcium Channel Blockers.
NimodipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
NisoldipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
NitrendipineBarbiturates may increase the metabolism of Calcium Channel Blockers.
NitroglycerinMay enhance the hypotensive effect of Hypotensive Agents.
NitroprussideMay enhance the hypotensive effect of Hypotensive Agents.
NorelgestrominMay diminish the therapeutic effect of Contraceptives (Estrogens). Contraceptive failure is possible.
NorethindroneMay diminish the therapeutic effect of Contraceptives (Progestins). Contraceptive failure is possible.
NorgestimateMay diminish the therapeutic effect of Contraceptives (Progestins). Contraceptive failure is possible.
NortriptylineMay increase the metabolism of Tricyclic Antidepressants.
OlmesartanMay enhance the hypotensive effect of Hypotensive Agents.
OrphenadrineCNS Depressants may enhance the CNS depressant effect of Orphenadrine.
PapaverineMay enhance the hypotensive effect of Hypotensive Agents.
PenbutololMay decrease the serum concentration of Beta-Blockers.
PerampanelMay enhance the CNS depressant effect of CNS Depressants.
PerhexilineBarbiturates may increase the metabolism of Calcium Channel Blockers.
PerindoprilMay enhance the hypotensive effect of Hypotensive Agents.
PethidineMay enhance the CNS depressant effect of Meperidine. Barbiturates may increase serum concentrations of the active metabolite(s) of Meperidine.
PindololMay decrease the serum concentration of Beta-Blockers.
PramipexoleCNS Depressants may enhance the sedative effect of Pramipexole.
PrazosinMay enhance the hypotensive effect of Hypotensive Agents.
PrenylamineBarbiturates may increase the metabolism of Calcium Channel Blockers.
PrimidoneMay enhance the adverse/toxic effect of Barbiturates. Primidone is converted to phenobarbital, and thus becomes additive with existing barbiturate therapy.
PropafenoneBarbiturates may decrease the serum concentration of Propafenone.
PropranololMay decrease the serum concentration of Beta-Blockers.
ProtriptylineMay increase the metabolism of Tricyclic Antidepressants.
PyridoxinePyridoxine may increase the metabolism of Barbiturates. Apparent in high pyridoxine doses (eg, 200 mg/day)
QuetiapineMay enhance the hypotensive effect of Hypotensive Agents.
QuinaprilMay enhance the hypotensive effect of Hypotensive Agents.
RamiprilMay enhance the hypotensive effect of Hypotensive Agents.
ReserpineMay enhance the hypotensive effect of Hypotensive Agents.
RifampicinRifamycin Derivatives may increase the metabolism of Barbiturates.
RifapentineRifamycin Derivatives may increase the metabolism of Barbiturates.
RiociguatMay enhance the hypotensive effect of Hypotensive Agents.
RisedronateBarbiturates may increase the metabolism of Calcium Channel Blockers.
RopiniroleCNS Depressants may enhance the sedative effect of ROPINIRole.
RotigotineCNS Depressants may enhance the sedative effect of Rotigotine.
RufinamideMay enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced.
SotalolMay decrease the serum concentration of Beta-Blockers.
SpironolactoneMay enhance the hypotensive effect of Hypotensive Agents.
SuvorexantCNS Depressants may enhance the CNS depressant effect of Suvorexant.
TapentadolMay enhance the CNS depressant effect of CNS Depressants.
TelmisartanMay enhance the hypotensive effect of Hypotensive Agents.
TeniposideBarbiturates may decrease the serum concentration of Teniposide.
TerazosinMay enhance the hypotensive effect of Hypotensive Agents.
ThalidomideCNS Depressants may enhance the CNS depressant effect of Thalidomide.
TheophyllineMay decrease the serum concentration of Theophylline Derivatives.
TimololMay decrease the serum concentration of Beta-Blockers.
TizanidineMay enhance the hypotensive effect of Hypotensive Agents.
TorasemideMay enhance the hypotensive effect of Hypotensive Agents.
TrandolaprilMay enhance the hypotensive effect of Hypotensive Agents.
TriamtereneMay enhance the hypotensive effect of Hypotensive Agents.
TrimipramineMay increase the metabolism of Tricyclic Antidepressants.
UlipristalBarbiturates may decrease the serum concentration of Ulipristal.
Valproic AcidValproic Acid and Derivatives may decrease the metabolism of Barbiturates. Barbiturates may decrease the serum concentration of Valproic Acid and Derivatives.
ValsartanMay enhance the hypotensive effect of Hypotensive Agents.
VerapamilBarbiturates may increase the metabolism of Calcium Channel Blockers.
VoriconazoleMay decrease the serum concentration of Voriconazole. Exceptions: Methohexital; PENTobarbital; Secobarbital; Thiopental.
ZolpidemCNS Depressants may enhance the CNS depressant effect of Zolpidem.
Food InteractionsNot Available

Targets

1. Gamma-aminobutyric acid receptor subunit alpha-1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-1 P14867 Details

References:

  1. Steinbach JH, Akk G: Modulation of GABA receptor channel gating by pentobarbital. J Physiol. 2001 Dec 15;537(Pt 3):715-33. Pubmed
  2. Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. Pubmed
  3. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. Pubmed
  4. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. Pubmed
  5. 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
  6. Davies DL, McCauley LD, Bolger MB, Alkana RL: Pressure-sensitive and -insensitive coupling in gamma-aminobutyric acid(A) receptors. Psychopharmacology (Berl). 2001 Oct;157(4):401-10. Pubmed
  7. Rahman M, Zhu D, Lindblad C, Johansson IM, Holmberg E, Isaksson M, Taube M, Backstrom T, Wang MD: GABA-site antagonism and pentobarbital actions do not depend on the alpha-subunit type in the recombinant rat GABA receptor. Acta Physiol (Oxf). 2006 Aug;187(4):479-88. Pubmed
  8. Feigenspan A, Weiler R: Electrophysiological properties of mouse horizontal cell GABAA receptors. J Neurophysiol. 2004 Nov;92(5):2789-801. Epub 2004 Jul 7. Pubmed
  9. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  10. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  11. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

2. Gamma-aminobutyric acid receptor subunit alpha-2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-2 P47869 Details

References:

  1. 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
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. Pubmed

3. Gamma-aminobutyric acid receptor subunit alpha-3

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-3 P34903 Details

References:

  1. 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
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. Pubmed

4. Gamma-aminobutyric acid receptor subunit alpha-4

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-4 P48169 Details

References:

  1. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. Pubmed

5. Gamma-aminobutyric acid receptor subunit alpha-5

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-5 P31644 Details

References:

  1. 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
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. Pubmed

6. Gamma-aminobutyric acid receptor subunit alpha-6

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-6 Q16445 Details

References:

  1. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. Pubmed
  2. 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

7. Neuronal acetylcholine receptor subunit alpha-4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Neuronal acetylcholine receptor subunit alpha-4 P43681 Details

References:

  1. 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
  2. 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
  3. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. Pubmed

8. Neuronal acetylcholine receptor subunit alpha-7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Neuronal acetylcholine receptor subunit alpha-7 P36544 Details

References:

  1. 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
  2. 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
  3. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. Pubmed

9. Glutamate receptor 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Glutamate receptor 2 P42262 Details

References:

  1. 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
  2. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. Pubmed

10. Glutamate receptor ionotropic, kainate 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Glutamate receptor ionotropic, kainate 2 Q13002 Details

References:

  1. 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
  2. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. Pubmed

11. GABA-A receptor (anion channel)

Kind: protein group

Organism: Human

Pharmacological action: yes

Actions: positive allosteric modulator

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:

  1. ChEMBL Compound Report Card (Accessed December 2013)

12. NMDA receptor

Kind: protein group

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Glutamate receptor ionotropic, NMDA 1 Q05586 Details
Glutamate receptor ionotropic, NMDA 2A Q12879 Details
Glutamate receptor ionotropic, NMDA 2B Q13224 Details
Glutamate receptor ionotropic, NMDA 2C Q14957 Details
Glutamate receptor ionotropic, NMDA 2D O15399 Details
Glutamate receptor ionotropic, NMDA 3A Q8TCU5 Details
Glutamate receptor ionotropic, NMDA 3B O60391 Details

References:

  1. Daniell LC: Effect of anesthetic and convulsant barbiturates on N-methyl-D-aspartate receptor-mediated calcium flux in brain membrane vesicles. Pharmacology. 1994 Nov;49(5):296-307. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Lexicomp

2. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 2A6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2A6 P11509 Details

References:

  1. Lexicomp

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:09