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Identification
NameTemazepam
Accession NumberDB00231  (APRD00676)
Typesmall molecule
Groupsapproved
Description

A benzodiazepine that acts as a gamma-aminobutyric acid modulator and anti-anxiety agent. [PubChem]

Structure
Thumb
SynonymsNot Available
SaltsNot Available
Brand names
NameCompany
EuhypnosNot Available
NorkotralNot Available
NormisonNot Available
NortemNot Available
RemestanNot Available
RestorilNot Available
TemazeNot Available
TemtabsNot Available
Brand mixturesNot Available
CategoriesNot Available
CAS number846-50-4
WeightAverage: 300.74
Monoisotopic: 300.066555377
Chemical FormulaC16H13ClN2O2
InChI KeyInChIKey=SEQDDYPDSLOBDC-UHFFFAOYSA-N
InChI
InChI=1S/C16H13ClN2O2/c1-19-13-8-7-11(17)9-12(13)14(18-15(20)16(19)21)10-5-3-2-4-6-10/h2-9,15,20H,1H3
IUPAC Name
7-chloro-3-hydroxy-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
SMILES
CN1C2=C(C=C(Cl)C=C2)C(=NC(O)C1=O)C1=CC=CC=C1
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassHeterocyclic Compounds
ClassBenzodiazepines
SubclassNot Available
Direct parentBenzodiazepines
Alternative parentsChlorobenzenes; Aryl Chlorides; Tertiary Carboxylic Acid Amides; Tertiary Amines; Polyamines; Carboxylic Acids; Organochlorides
Substituentschlorobenzene; benzene; aryl halide; aryl chloride; tertiary carboxylic acid amide; tertiary amine; carboxamide group; polyamine; carboxylic acid; carboxylic acid derivative; organohalogen; organochloride; amine; organonitrogen compound
Classification descriptionThis compound belongs to the benzodiazepines. These are organic compounds containing a benzene ring fused to either isomers of diazepine(unsaturated seven-member heterocycle with two nitrogen atoms replacing two carbon atoms).
Pharmacology
IndicationFor the short-term treatment of insomnia (generally 7-10 days).
PharmacodynamicsTemazepam is a benzodiazepine used as a hypnotic agent in the management of insomnia. Temazepam produces CNS depression at limbic, thalamic, and hypothalamic levels of the CNS. Temazepam increases the affinity of the neurotransmitter gamma-aminobutyric acid (GABA) for GABA receptors by binding to benzodiazepine receptors. Results are sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action.
Mechanism of actionBenzodiazepines bind nonspecifically to benzodiazepine receptors, which affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
AbsorptionWell absorbed, minimal first-pass metabolism.
Volume of distributionNot Available
Protein binding96%
Metabolism

Hepatic. Temazepam is completely metabolized through conjugation prior to excretion. The major metabolite is the O-conjugate of temazepam (90%).

SubstrateEnzymesProduct
Temazepam
OxazepamDetails
Temazepam
    Oxazepam glucuronideDetails
    Route of eliminationTemazepam was completely metabolized through conjugation prior to excretion; 80% to 90% of the dose appeared in the urine.
    Half life10-20 hours
    ClearanceNot Available
    ToxicityNot Available
    Affected organisms
    • Humans and other mammals
    PathwaysNot Available
    SNP Mediated EffectsNot Available
    SNP Mediated Adverse Drug ReactionsNot Available
    ADMET
    Predicted ADMET features
    Property Value Probability
    Human Intestinal Absorption + 0.9913
    Blood Brain Barrier + 0.9745
    Caco-2 permeable + 0.7979
    P-glycoprotein substrate Non-substrate 0.55
    P-glycoprotein inhibitor I Non-inhibitor 0.7388
    P-glycoprotein inhibitor II Inhibitor 0.546
    Renal organic cation transporter Non-inhibitor 0.7776
    CYP450 2C9 substrate Non-substrate 0.6281
    CYP450 2D6 substrate Non-substrate 0.9116
    CYP450 3A4 substrate Substrate 0.6962
    CYP450 1A2 substrate Inhibitor 0.5916
    CYP450 2C9 substrate Non-inhibitor 0.5454
    CYP450 2D6 substrate Non-inhibitor 0.891
    CYP450 2C19 substrate Non-inhibitor 0.5615
    CYP450 3A4 substrate Non-inhibitor 0.6014
    CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6494
    Ames test Non AMES toxic 0.7974
    Carcinogenicity Non-carcinogens 0.8093
    Biodegradation Not ready biodegradable 1.0
    Rat acute toxicity 2.0888 LD50, mol/kg Not applicable
    hERG inhibition (predictor I) Weak inhibitor 0.9987
    hERG inhibition (predictor II) Non-inhibitor 0.8308
    Pharmacoeconomics
    Manufacturers
    • Tyco healthcare group lp
    • Quantum pharmics ltd
    • Actavis elizabeth llc
    • Duramed pharmaceuticals inc sub barr laboratories inc
    • Mutual pharmaceutical co inc
    • Mylan pharmaceuticals inc
    • Novel laboratories inc
    • Sandoz inc
    • Usl pharma inc
    • Watson laboratories inc
    Packagers
    Dosage forms
    FormRouteStrength
    CapsuleOral
    Prices
    Unit descriptionCostUnit
    Restoril 22.5 mg capsule11.37USDcapsule
    Restoril 7.5 mg capsule11.37USDcapsule
    Temazepam 22.5 mg capsule9.94USDcapsule
    Temazepam 7.5 mg capsule9.94USDcapsule
    Restoril 15 mg capsule7.87USDcapsule
    Restoril 30 mg capsule7.67USDcapsule
    Temazepam 30 mg capsule0.69USDcapsule
    Temazepam 15 mg capsule0.58USDcapsule
    Apo-Temazepam 30 mg Capsule0.14USDcapsule
    Co Temazepam 30 mg Capsule0.14USDcapsule
    Novo-Temazepam 30 mg Capsule0.14USDcapsule
    Pms-Temazepam 30 mg Capsule0.14USDcapsule
    Ratio-Temazepam 30 mg Capsule0.14USDcapsule
    Apo-Temazepam 15 mg Capsule0.12USDcapsule
    Co Temazepam 15 mg Capsule0.12USDcapsule
    Novo-Temazepam 15 mg Capsule0.12USDcapsule
    Pms-Temazepam 15 mg Capsule0.12USDcapsule
    Ratio-Temazepam 15 mg Capsule0.12USDcapsule
    DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
    Patents
    CountryPatent NumberApprovedExpires (estimated)
    United States52119541993-05-182010-05-18
    Properties
    Statesolid
    Experimental Properties
    PropertyValueSource
    melting point119-121 °CPhysProp
    water solubility164 mg/LNot Available
    logP2.19HANSCH,C ET AL. (1995)
    Predicted Properties
    PropertyValueSource
    water solubility5.34e-02 g/lALOGPS
    logP2.16ALOGPS
    logP2.79ChemAxon
    logS-3.8ALOGPS
    pKa (strongest acidic)10.68ChemAxon
    pKa (strongest basic)-1.4ChemAxon
    physiological charge0ChemAxon
    hydrogen acceptor count3ChemAxon
    hydrogen donor count1ChemAxon
    polar surface area52.9ChemAxon
    rotatable bond count1ChemAxon
    refractivity81.01ChemAxon
    polarizability30.32ChemAxon
    number of rings3ChemAxon
    bioavailability1ChemAxon
    rule of fiveYesChemAxon
    Ghose filterYesChemAxon
    Veber's ruleNoChemAxon
    MDDR-like ruleNoChemAxon
    Spectra
    SpectraNot Available
    References
    Synthesis ReferenceNot Available
    General Reference
    1. Rickels K: The clinical use of hypnotics: indications for use and the need for a variety of hypnotics. Acta Psychiatr Scand Suppl. 1986;332:132-41. Pubmed
    2. Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. Pubmed
    3. Vozeh S: [Pharmacokinetic of benzodiazepines in old age] Schweiz Med Wochenschr. 1981 Nov 21;111(47):1789-93. Pubmed
    4. Shats V, Kozacov S: [Falls in the geriatric department: responsibility of the care-giver and the hospital] Harefuah. 1995 Jun 1;128(11):690-3, 743. Pubmed
    5. Rooke KC: The use of flurazepam (dalmane) as a substitute for barbiturates and methaqualone/diphenhydramine (mandrax) in general practice. J Int Med Res. 1976;4(5):355-9. Pubmed
    External Links
    ResourceLink
    KEGG DrugD00370
    PubChem Compound5391
    PubChem Substance46506604
    ChemSpider5198
    Therapeutic Targets DatabaseDAP000238
    PharmGKBPA451608
    Drug Product Database2244815
    RxListhttp://www.rxlist.com/cgi/generic/temaz.htm
    Drugs.comhttp://www.drugs.com/temazepam.html
    PDRhealthhttp://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/res1373.shtml
    WikipediaTemazepam
    ATC CodesN05CD07
    AHFS Codes
    • 28:24.08
    PDB EntriesNot Available
    FDA labelNot Available
    MSDSNot Available
    Interactions
    Drug Interactions
    Drug
    AminophyllineAminophylline may decrease the efficacy of Temazepam. Monitor for changes in the therapeutic effect of Temazepam if Aminophylline is initiated, discontinued or dose changed.
    ClozapineThe benzodiazepine, Temazepam, may increase the adverse effects of Clozapine. Monitor for respiratory depression and hypotension if concomitant therapy is initiated.
    DyphyllineDyphylline may decrease the efficacy of Temazepam. Monitor for changes in the therapeutic effect of Temazepam if Dyphylline is initiated, discontinued or dose changed.
    KavaKava may increase the effect of the benzodiazepine, temazepam.
    TheophyllineTheophylline may decrease the efficacy of Temazepam. Monitor for changes in the therapeutic effect of Temazepam if Theophylline is initiated, discontinued or dose changed.
    TriprolidineThe CNS depressants, Triprolidine and Temazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
    Food Interactions
    • Avoid alcohol.
    • Avoid avocado.
    • Avoid excessive quantities of coffee or tea (Caffeine).

    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. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. 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. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. 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. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. 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. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. 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. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. 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. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    7. Gamma-aminobutyric acid receptor subunit beta-1

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit beta-1 P18505 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    8. Gamma-aminobutyric acid receptor subunit beta-2

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit beta-2 P47870 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    9. Gamma-aminobutyric acid receptor subunit beta-3

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit beta-3 P28472 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    10. Gamma-aminobutyric acid receptor subunit gamma-1

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit gamma-1 Q8N1C3 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    11. Gamma-aminobutyric acid receptor subunit gamma-2

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit gamma-2 P18507 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    12. Gamma-aminobutyric acid receptor subunit gamma-3

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit gamma-3 Q99928 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    13. Gamma-aminobutyric acid receptor subunit delta

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit delta O14764 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    14. Gamma-aminobutyric acid receptor subunit epsilon

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit epsilon P78334 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    15. Gamma-aminobutyric acid receptor subunit pi

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit pi O00591 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    16. Gamma-aminobutyric acid receptor subunit rho-1

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit rho-1 P24046 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    17. Gamma-aminobutyric acid receptor subunit rho-2

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit rho-2 P28476 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    18. Gamma-aminobutyric acid receptor subunit rho-3

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit rho-3 A8MPY1 Details

    References:

    1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. Pubmed
    2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed

    19. Gamma-aminobutyric acid receptor subunit theta

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: potentiator

    Components

    Name UniProt ID Details
    Gamma-aminobutyric acid receptor subunit theta Q9UN88 Details

    References:

    1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. Epub 2008 Mar 31. Pubmed
    2. Giersch A, Boucart M, Elliott M, Vidailhet P: Atypical behavioural effects of lorazepam: clues to the design of novel therapies? Pharmacol Ther. 2010 Apr;126(1):94-108. Epub 2010 Feb 4. Pubmed

    20. Translocator protein

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: other

    Components

    Name UniProt ID Details
    Translocator protein P30536 Details

    References:

    1. Dobbin M, Martyres RF, Clode D, Champion De Crespigny FE: Association of benzodiazepine injection with the prescription of temazepam capsules. Drug Alcohol Rev. 2003 Jun;22(2):153-7. Pubmed
    2. Miller EI, Wylie FM, Oliver JS: Detection of benzodiazepines in hair using ELISA and LC-ESI-MS-MS. J Anal Toxicol. 2006 Sep;30(7):441-8. Pubmed
    3. Mant A, Whicker SD, McManus P, Birkett DJ, Edmonds D, Dumbrell D: Benzodiazepine utilisation in Australia: report from a new pharmacoepidemiological database. Aust J Public Health. 1993 Dec;17(4):345-9. Pubmed

    21. 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)

    1. Cytochrome P450 2C19

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Cytochrome P450 2C19 P33261 Details

    References:

    1. Application available online: The P450 Program
    2. 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

    2. Cytochrome P450 3A4

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Cytochrome P450 3A4 P08684 Details

    References:

    1. Shou M, Mei Q, Ettore MW Jr, Dai R, Baillie TA, Rushmore TH: Sigmoidal kinetic model for two co-operative substrate-binding sites in a cytochrome P450 3A4 active site: an example of the metabolism of diazepam and its derivatives. Biochem J. 1999 Jun 15;340 ( Pt 3):845-53. Pubmed
    2. 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 2B6

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Cytochrome P450 2B6 P20813 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

    4. Cytochrome P450 2C8

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Cytochrome P450 2C8 P10632 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

    5. Cytochrome P450 2C9

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Cytochrome P450 2C9 P11712 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

    Comments
    Drug created on June 13, 2005 07:24 / Updated on September 25, 2013 14:46