This drug entry is astuband has not been fully annotated. It is scheduled to be annotated soon.

Identification

Summary

Nordazepamis a benzodiazepine indicated in the treatment of insomnia.

Generic Name
Nordazepam
DrugBank Accession Number
DB14028
Background

An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam.

Type
Small Molecule
Groups
Experimental
Structure
Weight
Average: 270.714
Monoisotopic: 270.055990691
Chemical Formula
C15H11ClN2O
Synonyms
  • Desmethyldiazepam
  • N-desmethyldiazepam
  • Nordazepam
  • Nordazepam CIV
  • Nordazepamum
  • Nordiazepam
External IDs
  • A 101
  • A101
  • RO 5-2180

Pharmacology

Indication

不可用

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

不可用

Mechanism of action
Target Actions Organism
AGABA(A) Receptor
positive allosteric modulator
Humans
AGABA(A) Receptor Benzodiazepine Binding Site
ligand
Humans
Absorption

不可用

Volume of distribution

不可用

Protein binding

不可用

Metabolism
不可用
Route of elimination

不可用

Half-life

不可用

Clearance

不可用

Adverse Effects
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Toxicity

不可用

Pathways
不可用
Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
不可用

Interactions

Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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.
Drug Interaction
1,2-Benzodiazepine 不良的风险或严重性effects can be increased when 1,2-Benzodiazepine is combined with Nordazepam.
Acetazolamide 不良的风险或严重性effects can be increased when Acetazolamide is combined with Nordazepam.
Acetophenazine 不良的风险或严重性effects can be increased when Acetophenazine is combined with Nordazepam.
Aclidinium Nordazepam may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
Agomelatine 不良的风险或严重性effects can be increased when Agomelatine is combined with Nordazepam.
Alfentanil 不良的风险或严重性effects can be increased when Alfentanil is combined with Nordazepam.
Alimemazine 不良的风险或严重性effects can be increased when Alimemazine is combined with Nordazepam.
Almotriptan 不良的风险或严重性effects can be increased when Almotriptan is combined with Nordazepam.
Alosetron 不良的风险或严重性effects can be increased when Alosetron is combined with Nordazepam.
Alprazolam 不良的风险或严重性effects can be increased when Alprazolam is combined with Nordazepam.
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Food Interactions
不可用

Products

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International/Other Brands
Calmday/Lomax/Madar/Sopax/Stilny/Vegesan

Categories

ATC Codes
N05BA16 — Nordazepam
Drug Categories
Chemical TaxonomyProvided byClassyfire
Description
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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzodiazepines
Sub Class
1,4-benzodiazepines
Direct Parent
1,4-benzodiazepines
Alternative Parents
Benzene and substituted derivatives/Aryl chlorides/Cyclic carboximidic acids/Ketimines/Propargyl-type 1,3-dipolar organic compounds/Azacyclic compounds/Organopnictogen compounds/Organooxygen compounds/Organochlorides/Hydrocarbon derivatives
Substituents
1,4-benzodiazepine/Aromatic heteropolycyclic compound/Aryl chloride/Aryl halide/Azacycle/Benzenoid/Cyclic carboximidic acid/Hydrocarbon derivative/Imine/Ketimine
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organochlorine compound, 1,4-benzodiazepinone (CHEBI:111762)
Affected organisms
不可用

Chemical Identifiers

UNII
67220MCM01
CAS number
1088-11-5
InChI Key
AKPLHCDWDRPJGD-UHFFFAOYSA-N
InChI
InChI=1S/C15H11ClN2O/c16-11-6-7-13-12(8-11)15(17-9-14(19)18-13)10-4-2-1-3-5-10/h1-8H,9H2,(H,18,19)
IUPAC Name
7-chloro-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
SMILES
ClC1=CC=C2NC(=O)CN=C(C3=CC=CC=C3)C2=C1

References

General References
  1. AIFA: Madar (Nordazepam) Oral Tablet [Link]
Human Metabolome Database
HMDB0060538
KEGG Drug
D08283
KEGG Compound
C07486
ChemSpider
2890
BindingDB
50027835
RxNav
3155
ChEBI
111762
ChEMBL
CHEMBL523
ZINC
ZINC000001249069
Wikipedia
Nordazepam

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count

Pharmacoeconomics

Manufacturers
不可用
Packagers
不可用
Dosage Forms
Form Route Strength
Pill
Tablet, coated
Tablet Oral 15 mg
Prices
不可用
Patents
不可用

Properties

State
Solid
Experimental Properties
不可用
Predicted Properties
Property Value Source
Water Solubility 0.0219 mg/mL ALOGPS
logP 2.79 ALOGPS
logP 3.21 ChemAxon
logS -4.1 ALOGPS
pKa (Strongest Acidic) 12.3 ChemAxon
pKa (Strongest Basic) 2.85 ChemAxon
Physiological Charge 0 ChemAxon
Hydrogen Acceptor Count 2 ChemAxon
Hydrogen Donor Count 1 ChemAxon
Polar Surface Area 41.46 Å2 ChemAxon
Rotatable Bond Count 1 ChemAxon
Refractivity 76.7 m3·mol-1 ChemAxon
Polarizability 27.41 Å3 ChemAxon
Number of Rings 3 ChemAxon
Bioavailability 1 ChemAxon
Rule of Five Yes ChemAxon
Ghose Filter Yes ChemAxon
Veber's Rule No ChemAxon
MDDR-like Rule No ChemAxon
Predicted ADMET Features
不可用

Spectra

Mass Spec (NIST)
不可用
Spectra
Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum - GC-MS Predicted GC-MS 不可用
Mass Spectrum (Electron Ionization) MS splash10-006x-1290000000-16289dee622e983dadb4
Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS 不可用
Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS 不可用
LC-MS/MS Spectrum - LC-ESI-QFT , negative LC-MS/MS splash10-014i-0090000000-08ab493d917dff556803
LC-MS/MS Spectrum - LC-ESI-QFT , negative LC-MS/MS splash10-0006-0090000000-b3902adae33dd2ada996
LC-MS/MS Spectrum - LC-ESI-QFT , negative LC-MS/MS splash10-0006-0090000000-e1f36555cb45aafb3578
LC-MS/MS Spectrum - LC-ESI-QFT , negative LC-MS/MS splash10-0006-0090000000-4599707b6c514e2fd140
LC-MS/MS Spectrum - LC-ESI-QFT , negative LC-MS/MS splash10-0006-0090000000-2afa9f8bad136457e913
LC-MS/MS Spectrum - LC-ESI-QFT , negative LC-MS/MS splash10-052f-0090000000-39292916fbbd987c9c79
LC-MS/MS Spectrum - LC-ESI-QFT , negative LC-MS/MS splash10-0udi-0490000000-93d06070b3ddb4f2bb1d
LC-MS/MS Spectrum - LC-ESI-QFT , negative LC-MS/MS splash10-0udi-0900000000-319db7de66dd214c6036
LC-MS/MS Spectrum - LC-ESI-QTOF , positive LC-MS/MS splash10-00di-0090000000-f12d8a37190a6a1a6260
LC-MS/MS Spectrum - LC-ESI-QTOF , positive LC-MS/MS splash10-00dl-0590000000-6667f22f2eaaa4d7d444
LC-MS/MS Spectrum - LC-ESI-QTOF , positive LC-MS/MS splash10-05mo-0950000000-9f91849bf0ea300eddf6
LC-MS/MS Spectrum - LC-ESI-QTOF , positive LC-MS/MS splash10-052f-0940000000-113f94a665f60922a3cc
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-00di-0090000000-a17b063554f54d5ae790
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-00di-0090000000-00d132ae0ea246d26e2a
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-00di-0390000000-02873020d1329d3d5c38
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-0006-1960000000-010c3ba06f80d4ace994
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-052f-1930000000-327cc931b60592065b64
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-0006-2910000000-0a0897ca546d1bc1cb27
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-0f6x-4900000000-7cc6b852b0d715a021c2
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-0ufr-7900000000-d4ef23e43b78528b7c96
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-0w4i-9700000000-9ef8e88327da379c2b33

Targets

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Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
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
抑制细胞外ligand-gated离子通道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...

Components:
References
  1. 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]
  2. 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]
Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Ligand
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
抑制细胞外ligand-gated离子通道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...

Components:
References
  1. 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]
  2. 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]

Drug created at May 15, 2018 20:27 / Updated at May 14, 2021 01:06