Lorazepam is a short-acting benzodiazepine commonly used to treat panic disorders, severe anxiety, and seizures.

Brand Names
Ativan, Loreev
Generic Name
DrugBank Accession Number

Lorazepam is a short-acting and rapidly cleared benzodiazepine used commonly as a sedative and anxiolytic.6 It was developed by DJ Richards, presented and marketed initially by Wyeth Pharmaceuticals in the USA in 1977. The first historic FDA label approval is reported in 1985 by the company Mutual Pharm.15

Small Molecule
Average: 321.158
Monoisotopic: 320.011932988
Chemical Formula
  • Loracepam
  • Lorazepam
  • o-Chlorooxazepam
  • o-Chloroxazepam
External IDs
  • WY-4036



Lorazepam is FDA-approved for the short-term relief of anxiety symptoms related to anxiety disorders and anxiety associated with depressive symptoms such as anxiety-associated insomnia. It is as well used as an anesthesia premedication in adults to relieve anxiety or to produce sedation/amnesia and for the treatment of status epilepticus.12

Some off-label indications of lorazepam include rapid tranquilization of an agitated patient, alcohol withdrawal delirium, alcohol withdrawal syndrome, muscle spasms, insomnia, panic disorder, delirium, chemotherapy-associated anticipatory nausea and vomiting, and psychogenic catatonia.12

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofAgitation••• •••••
Treatment ofAlcohol withdrawal delirium••• •••••
Treatment ofAlcohol withdrawal syndrome(aws)••• •••••
Symptomatic treatment ofAnxiety••••••••••••••••••••••••••••••
Management ofAnxiety•••••••••••••••••••••••• ••••••• ••••••••• ••••••
Associated Therapies
Contraindications & Blackbox Warnings
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The effect of lorazepam in GABA-A receptors produces an increase in the frequency of opening of the chloride ion channel. However, for its effect to generate, the neurotransmitter is required.8 The anticonvulsant properties of lorazepam are thought to be related to the binding to voltage-dependent sodium channels in which the sustained repetitive firing gets limited by the slow recovery of sodium channels due to the benzodiazepine effect.9

The effect of lorazepam seems to be very compartmental which was observed with a different generation of sleepiness and a dizziness effect.10

Mechanism of action

Lorazepam allosterically binds on the benzodiazepine receptors in the post-synaptic GABA-A ligand-gated chloride channel in different sites of the central nervous system (CNS). This binding will result in an increase on the GABA inhibitory effects which is translated as an increase in the flow of chloride ions into the cell causing hyperpolarization and stabilization of the cellular plasma membrane.12

According to the binding site of lorazepam, we can observe different activities as the binding in the amygdala is known to help mainly in anxiety disorders while the binding in the cerebral cortex helps in seizure disorders.12

AGABA(A) Receptor
positive allosteric modulator
AGABA(A) Receptor Benzodiazepine Binding Site

Readily absorbed with an absolute bioavailability of 90% when given orally. When intramuscularly administered a dose of 4 mg, lorazepam is completely and rapidly absorbed and achieves a maximal serum concentration of 48 ng/ml in 15-30 minutes. When administered orally, the time to attained maximum concentration is observed to be of 2 hours.12

Volume of distribution

The reported volume of distribution of lorazepam is 1.3 L/kg.13 It is important to mention that due to the lipophilicity of lorazepam, it does not redistribute as fast in the brain.14

Protein binding

Reports indicate that 85% of lorazepam administered dose is protein bound.13


Lorazepam is hepatically metabolized by CYP450 isoenzymes and extensively conjugated to the 3-0-phenolic glucuronide.12 This is an inactive metabolite and is eliminated mainly by the kidneys.

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Route of elimination

When a single 2 mg oral dose is given to healthy subjects, 88% of the administered dose is recovered in urine and 7% was recovered in feces. From the excreted dose in urine, the major form is the glucuronide version that represents 74% while only 0.3% of the dose is recovered as unchanged lorazepam.13


When administered parentally, the registered half-life of lorazepam is of 14 hours.12 Following the administration of 1 mg of lorazepam in healthy adult male volunteers and using a multi-doses equation based on a one-compartment model, the average elimination half-life of lorazepam was estimated to be 11 hours and 8 hours for sublingual and oral doses respectively.11 The absorption half-life was calculated to be 55 minutes for oral doses and 15 minutes for sublingual doses.11


In vivo studies with lorazepam have shown a clearance rate of 5.8 ml.min/kg.7

Adverse Effects
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The LD50 observed by oral administration in a mouse is of 1850 mg/kg.16 When an overdose administration is registered, signs of CNS and respiratory depression are rapidly observed. An overdose stage can result in profound sedation, deep respiratory depression, coma, and death.12 When overdose is observed, it is recommended to administer emergency symptomatic medical support with attention to produce an increase in lorazepam elimination.13

There is no evidence of carcinogenicity nor mutagenicity. At doses higher than 40 mg/kg there is evidence of fetal resorption and increase in fetal loss.Label

Not Available
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Lorazepam is combined with 1,2-Benzodiazepine.
AbacavirLorazepam may decrease the excretion rate of Abacavir which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Lorazepam which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Lorazepam which could result in a higher serum level.
AcetaminophenLorazepam may decrease the excretion rate of Acetaminophen which could result in a higher serum level.
Food Interactions
  • Avoid alcohol.
  • Limit caffeine intake.
  • Take with food.


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Product Images
International/Other Brands
Almazine (Psyco Remedies) / Anxiedin (U-Liang) / Idalprem (Novartis) / Lorabenz / Lorsilan (Belupo) / Somagerol / Temesta (Wyeth) / Wypax (Wyeth KK)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AtivanTablet0.5 mgSublingualPfizer Canada Ulc1995-12-31Not applicableCanada flag
AtivanTablet1 mg/1OralBTA Pharmaceuticals Inc.2010-03-162015-01-31US flag
AtivanTablet1 mg/1OralA-S Medication Solutions2013-05-012017-09-30US flag
AtivanTablet2 mgOralPfizer Canada Ulc1994-12-31Not applicableCanada flag
AtivanTablet1 mg/1OralA S Medication Solutions2010-03-16Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-lorazepamTablet2 mgOralApotex Corporation1985-12-31Not applicableCanada flag
Apo-lorazepamTablet1 mgOralApotex Corporation1985-12-31Not applicableCanada flag
Apo-lorazepamTablet0.5 mgOralApotex Corporation1985-12-31Not applicableCanada flag
Dom-lorazepamTablet1 mgOralDominion Pharmacal2002-04-252019-02-20Canada flag
Dom-lorazepamTablet.5 mgOralDominion Pharmacal2002-04-252019-02-20Canada flag


ATC Codes
N05BA56 — Lorazepam, combinationsN05BA06 — Lorazepam
Drug Categories
Chemical TaxonomyProvided by Classyfire
This compound belongs to the class of organic compounds known as 1,4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1,4-azepine.
Organic compounds
Super Class
Organoheterocyclic compounds
Sub Class
Direct Parent
Alternative Parents
Alpha amino acids and derivatives / Chlorobenzenes / Aryl chlorides / Secondary carboxylic acid amides / Lactams / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Alkanolamines / Organopnictogen compounds
show 4 more
1,4-benzodiazepine / Alkanolamine / Alpha-amino acid or derivatives / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Carbonyl group / Carboxamide group
show 19 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

CAS number
InChI Key


Synthesis Reference

Igor Lifshitz, "Process for preparing pure crystalline lorazepam." U.S. Patent US20010039340, issued November 08, 2001.

General References
  1. Kemper N, Poser W, Poser S: [Benzodiazepine dependence: addiction potential of the benzodiazepines is greater than previously assumed (author's transl)]. Dtsch Med Wochenschr. 1980 Dec 5;105(49):1707-12. [Article]
  2. Lader M: Short-term versus long-term benzodiazepine therapy. Curr Med Res Opin. 1984;8 Suppl 4:120-6. [Article]
  3. Maltais F, Laberge F, Laviolette M: A randomized, double-blind, placebo-controlled study of lorazepam as premedication for bronchoscopy. Chest. 1996 May;109(5):1195-8. [Article]
  4. Heisterkamp DV, Cohen PJ: The effect of intravenous premedication with lorazepam (ativan), pentobarbitone or diazepam on recall. Br J Anaesth. 1975 Jan;47(1):79-81. [Article]
  5. Milligan DW, Howard MR, Judd A: Premedication with lorazepam before bone marrow biopsy. J Clin Pathol. 1987 Jun;40(6):696-8. [Article]
  6. Authors unspecified: Systematic review of the benzodiazepines. Guidelines for data sheets on diazepam, chlordiazepoxide, medazepam, clorazepate, lorazepam, oxazepam, temazepam, triazolam, nitrazepam, and flurazepam. Committee on the Review of Medicines. Br Med J. 1980 Mar 29;280(6218):910-2. [Article]
  7. Li C, Liu T, Cui X, Uss AS, Cheng KC: Development of in vitro pharmacokinetic screens using Caco-2, human hepatocyte, and Caco-2/human hepatocyte hybrid systems for the prediction of oral bioavailability in humans. J Biomol Screen. 2007 Dec;12(8):1084-91. doi: 10.1177/1087057107308892. Epub 2007 Nov 7. [Article]
  8. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [Article]
  9. McLean MJ, Macdonald RL: Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture. J Pharmacol Exp Ther. 1988 Feb;244(2):789-95. [Article]
  10. Kamal MA, Smith DE, Cook J, Feltner D, Moton A, Ouellet D: Pharmacodynamic differentiation of lorazepam sleepiness and dizziness using an ordered categorical measure. J Pharm Sci. 2010 Aug;99(8):3628-41. doi: 10.1002/jps.22093. [Article]
  11. Caille G, Spenard J, Lacasse Y, Brennan J: Pharmacokinetics of two lorazepam formulations, oral and sublingual, after multiple doses. Biopharm Drug Dispos. 1983 Jan-Mar;4(1):31-42. doi: 10.1002/bdd.2510040106. [Article]
  12. Ghiasi N. and Marwaha R. (2018). Lorazepam.. Treasure Island, FL.
  13. Pagliaro L. and Pagliaro A. (1999). Psychologists' psychotropic drug reference. Taylor and Francis.
  14. Volpe J. (2008). Neurology of the Newborn (5th ed.). Saunders Elsevier.
  15. FDA approvals [Link]
  16. Lorazepam monograph [Link]
  17. FDA Approved Drug Products: Ativan (lorazepam) for intravenous or intramuscular injection [Updated 01/2023] [Link]
  18. FDA Approved Drug Products: Ativan (lorazepam) tablets for oral administration [Updated 01/2023] [Link]
Human Metabolome Database
PubChem Compound
PubChem Substance
Therapeutic Targets Database
RxList Drug Page
Drugs.com Drug Page
FDA label
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Clinical Trials

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PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
4CompletedDiagnosticAnxiety Disorders / Generalized Anxiety Disorder1somestatusstop reasonjust information to hide
4CompletedOtherDecline, Cognitive1somestatusstop reasonjust information to hide
4CompletedOtherHealthy Volunteers (HV)1somestatusstop reasonjust information to hide
4CompletedTreatmentAgitation1somestatusstop reasonjust information to hide
4CompletedTreatmentAlcohol Dependency1somestatusstop reasonjust information to hide


  • Amneal pharmaceuticals
  • Paddock laboratories inc
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  • Baxter healthcare corp anesthesia critical care
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  • Mckesson Corp.
  • Meda AB
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  • Murfreesboro Pharmaceutical Nursing Supply
  • Mutual Pharmaceutical Co.
  • Mylan
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  • Va Cmop Dallas
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Dosage Forms
InjectionIntramuscular; Intravenous4.0 mg/1mL
TabletOral0.5 mg
TabletSublingual0.5 mg
TabletSublingual1 mg
TabletSublingual2 mg
TabletOral2 mg
LiquidIntramuscular; Intravenous4 mg / mL
SolutionIntramuscular; Intravenous4 mg / mL
TabletOral.5 mg / tab
TabletOral1 mg / tab
TabletOral2 mg / tab
TabletOral1 mg
Solution / dropsOral
ConcentrateOral2 mg/1mL
InjectionIntramuscular2 mg/1mL
InjectionIntramuscular; Intravenous2 mg/1mL
InjectionIntramuscular; Intravenous2.0 mg/1mL
InjectionIntramuscular; Intravenous4 mg/1mL
Injection, solutionIntramuscular; Intravenous2 mg/1mL
Injection, solutionIntramuscular; Intravenous4 mg/1mL
LiquidOral2 mg/1mL
Solution, concentrateOral2 mg/1mL
TabletOral.5 mg/1
TabletOral0.5 mg/1
TabletOral1 mg/1
TabletOral1.0 mg
TabletOral2 mg/1
TabletOral2.0 mg
Tablet, film coatedOral
TabletOral2.099 mg
Tablet, orally disintegratingOral1 MG
Tablet, orally disintegratingOral2.5 MG
Tablet, orally disintegratingOral
Tablet, film coatedOral1 MG
Tablet, film coatedOral2.5 MG
SolutionIntramuscular; Intravenous2 mg / mL
Injection, solution4 MG/ML
Injection, solutionParenteral
Capsule, extended releaseOral1 mg/1
Capsule, extended releaseOral1.5 mg/1
Capsule, extended releaseOral2 mg/1
Capsule, extended releaseOral3 mg/1
SolutionParenteral1.00 mg
TabletOral2.000 mg
TabletOral.5 mg
TabletOral1.000 mg
TabletOral0.5 mg / tab
CapsuleOral1.0000 mg
Injection, solutionParenteral4 MG/ML
Solution / dropsOral2 MG/ML
Tablet1 MG
Tablet2.5 MG
Tablet0.5 mg
TabletOral2.5 mg
Tablet2 mg
Injection, solutionIntramuscular; Intravenous2 mg/ml
Unit descriptionCostUnit
LORazepam Intensol 2 mg/ml Concentrate 30ml Bottle44.99USD bottle
Lorazepam powder20.81USD g
Lorazepam 4 mg/ml vial9.59USD ml
Lorazepam 2 mg/ml vial2.5USD ml
Ativan 2 mg tablet2.3USD tablet
Ativan 4 mg/ml vial2.16USD ml
Ativan 1 mg tablet1.96USD tablet
Lorazepam intensol 2 mg/ml1.6USD ml
Lorazepam-ns 60 mg/60 ml bag1.53USD ml
Ativan 0.5 mg tablet1.37USD tablet
Lorazepam-d5w 100 mg/100 ml1.16USD ml
Lorazepam-ns 100 mg/100 ml bag1.16USD ml
Lorazepam 2 mg tablet1.01USD tablet
Ativan 2 mg/ml vial0.9USD ml
Lorazepam 1 mg tablet0.69USD tablet
Lorazepam 0.5 mg tablet0.55USD tablet
Ativan 2 mg Sublingual Tablet0.24USD tablet
Ativan 1 mg Sublingual Tablet0.15USD tablet
Ativan 0.5 mg Sublingual Tablet0.12USD tablet
Apo-Lorazepam 2 mg Tablet0.07USD tablet
Novo-Lorazem 2 mg Tablet0.07USD tablet
Pms-Lorazepam 2 mg Tablet0.07USD tablet
Apo-Lorazepam 1 mg Tablet0.05USD tablet
Novo-Lorazem 1 mg Tablet0.05USD tablet
Pms-Lorazepam 1 mg Tablet0.05USD tablet
Apo-Lorazepam 0.5 mg Tablet0.04USD tablet
Novo-Lorazem 0.5 mg Tablet0.04USD tablet
Pms-Lorazepam 0.5 mg Tablet0.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8999393No2015-04-072034-01-08US flag


Experimental Properties
melting point (°C)192-194British Patent 1,022,642.
boiling point (°C)533.8 ºC at 760 mm HgChemspider
water solubility80 mg/LMERCK INDEX (1996)
logP2.39HANSCH,C ET AL. (1995)
logS-3.6ADME Research, USCD
Caco2 permeability200Li C., Liu T., Ciu X., Uss A. and Cheng K. (2007). Society of Biomolecular Science.
pKa13MERCK INDEX (1996); pK1
Predicted Properties
Water Solubility0.0176 mg/mLALOGPS
pKa (Strongest Acidic)10.61Chemaxon
pKa (Strongest Basic)-2.2Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count3Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area61.69 Å2Chemaxon
Rotatable Bond Count1Chemaxon
Refractivity82.7 m3·mol-1Chemaxon
Polarizability30.33 Å3Chemaxon
Number of Rings3Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Human Intestinal Absorption+0.9826
Blood Brain Barrier+0.9641
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.517
P-glycoprotein inhibitor INon-inhibitor0.8866
P-glycoprotein inhibitor IINon-inhibitor0.9167
Renal organic cation transporterNon-inhibitor0.8812
CYP450 2C9 substrateNon-substrate0.7692
CYP450 2D6 substrateNon-substrate0.8685
CYP450 3A4 substrateSubstrate0.5631
CYP450 1A2 substrateInhibitor0.8262
CYP450 2C9 inhibitorNon-inhibitor0.5063
CYP450 2D6 inhibitorNon-inhibitor0.8445
CYP450 2C19 inhibitorInhibitor0.5065
CYP450 3A4 inhibitorNon-inhibitor0.6563
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6407
Ames testNon AMES toxic0.9133
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.8229 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.999
hERG inhibition (predictor II)Non-inhibitor0.8734
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)


Mass Spec (NIST)
Not Available
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-004u-0290000000-b7b54d40e4a40249fc2d
GC-MS Spectrum - EI-BGC-MSsplash10-009i-6791000000-942b7493f1e9fc3d12be
Mass Spectrum (Electron Ionization)MSsplash10-002r-4981000000-a567f7beb26ee18d061c
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-00b9-0298000000-986499cda13643ef7d85
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-001i-0091000000-04730f82e569df7febdd
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-001i-0390000000-dd63d93f2fa81cbb5928
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udi-0930000000-3ecf1f2f10049a3cfee2
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udi-0910000000-95d23a9a121bf45ef8bf
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udi-0900000000-cdbe26e697f259770c28
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udi-0900000000-4046d54b4dd9bf7968be
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-001i-0091000000-abaf38ed3aa6e7d51245
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-052b-9000000000-dda683413448d0461123
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-0009000000-53bbea620bd1e8b49eb3
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0fb9-0095000000-793565a97e3afc2ce858
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-0090000000-41097b8a64363c5e2f94
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-0290000000-a0694111a3943eca2b53
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-0690000000-5a4728cb7e2473fc6b3c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-01rf-0940000000-39d041fbab4fb67a5c41
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00b9-0298000000-986499cda13643ef7d85
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00b9-0196000000-2e53b39b27c66ec73fd2
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-00di-0009000000-d2cf418ee1548b867206
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-00li-0093000000-7db5a2a899600b164680
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-00di-0019000000-793d8ce18330a98ed7fd
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-9013000000-f85a4b2ab78928e00ee5
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0950000000-cb55c9def97c9446913c
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-001l-9500000000-28a9b53f7059bca227b7
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
DarkChem Lite v0.1.0
DeepCCS 1.0 (2019)
DarkChem Lite v0.1.0
DeepCCS 1.0 (2019)
DarkChem Lite v0.1.0
DeepCCS 1.0 (2019)


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Protein group
Pharmacological action
Positive allosteric modulator
Curator comments
The GABA(A) receptor is pentameric (i.e. comprising 5 subunit proteins) and therefore has a multitude of potential isoforms. The above target is a collection of all possible GABA(A) subunits that may participate in the formation of the pentameric receptor and is not meant to imply direct a drug-protein interaction for each individual subunit.
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...

  1. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [Article]
  2. Sigel E, Steinmann ME: Structure, function, and modulation of GABA(A) receptors. J Biol Chem. 2012 Nov 23;287(48):40224-31. doi: 10.1074/jbc.R112.386664. Epub 2012 Oct 4. [Article]
  3. Zhu S, Noviello CM, Teng J, Walsh RM Jr, Kim JJ, Hibbs RE: Structure of a human synaptic GABAA receptor. Nature. 2018 Jul;559(7712):67-72. doi: 10.1038/s41586-018-0255-3. Epub 2018 Jun 27. [Article]
Protein group
Pharmacological action
Curator comments
Benzodiazepines modulate GABA(A) function by binding at the interface between alpha (α) and gamma (γ) subunits. Of the 6 α-subunits, only 4 (α-1, -2, -3, and -5) participate in the formation of this binding site. The above target is a collection of all α- and γ-subunits that are known to participate in the formation of the benzodiazepine binding site.
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...

  1. Zhu S, Noviello CM, Teng J, Walsh RM Jr, Kim JJ, Hibbs RE: Structure of a human synaptic GABAA receptor. Nature. 2018 Jul;559(7712):67-72. doi: 10.1038/s41586-018-0255-3. Epub 2018 Jun 27. [Article]
  2. Sigel E, Steinmann ME: Structure, function, and modulation of GABA(A) receptors. J Biol Chem. 2012 Nov 23;287(48):40224-31. doi: 10.1074/jbc.R112.386664. Epub 2012 Oct 4. [Article]


Pharmacological action
General Function
Glucuronosyltransferase activity
Specific Function
UDPGTs are of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isozyme displays activity toward several classes of xeno...
Gene Name
Uniprot ID
Uniprot Name
UDP-glucuronosyltransferase 2B15
Molecular Weight
61035.815 Da
  1. Chung JY, Cho JY, Yu KS, Kim JR, Jung HR, Lim KS, Jang IJ, Shin SG: Effect of the UGT2B15 genotype on the pharmacokinetics, pharmacodynamics, and drug interactions of intravenous lorazepam in healthy volunteers. Clin Pharmacol Ther. 2005 Jun;77(6):486-94. [Article]

Drug created at June 13, 2005 13:24 / Updated at July 14, 2024 17:59