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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
Categories
CAS number846-50-4
WeightAverage: 300.74
Monoisotopic: 300.066555377
Chemical FormulaC16H13ClN2O2
InChI KeySEQDDYPDSLOBDC-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
Not Available
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).

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. 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)

Enzymes

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

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