DIAZEPAM

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H13ClN2O
Molecular Weight	284.74
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C3=CC=CC=C3

InChI

InChIKey=AAOVKJBEBIDNHE-UHFFFAOYSA-N

InChI=1S/C16H13ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3

HIDE SMILES / InChI

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24552479

Diazepam is a benzodiazepine first discovered at Hoﬀman-La Roche in the late 1950s. Diazepam was approved by FDA for the treatment of anxiety disorders as well as for such conditions as skeletal muscle spasm, alcohol withdrawal syndrom and convulsions (under the most known brand Valium). The drug acts by binding to GABA-A receptors and potentiating GABA evoked current. Chronic diazepam use is associated with tolerance, dependence, and withdrawal.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABA-A receptor; benzodiazepine site 38 Target ID: CHEMBL2109243 Sources: http://www.hamiltonhealthsciences.ca/workfiles/basehospital/diazepam.pdf	Agonist 2678		8.6 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Anxiety 267 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Primary	Approved 8429	VALIUM Approved Use Valium is indicated for the management of anxiety disorders or for the shortterm relief of the symptoms of anxiety. In acute alcohol withdrawal, Valium may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis. Valium is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia), athetosis, and stiff-man syndrome. Oral Valium may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy. Launch Date 1963
Acute alcohol withdrawal 2 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8429	VALIUM Approved Use Valium is indicated for the management of anxiety disorders or for the shortterm relief of the symptoms of anxiety. In acute alcohol withdrawal, Valium may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis. Valium is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia), athetosis, and stiff-man syndrome. Oral Valium may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy. Launch Date 1963
Muscle spasm 40 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8429	VALIUM Approved Use Valium is indicated for the management of anxiety disorders or for the shortterm relief of the symptoms of anxiety. In acute alcohol withdrawal, Valium may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis. Valium is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia), athetosis, and stiff-man syndrome. Oral Valium may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy. Launch Date 1963
Convulsive disorders 2 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8429	VALIUM Approved Use Valium is indicated for the management of anxiety disorders or for the shortterm relief of the symptoms of anxiety. In acute alcohol withdrawal, Valium may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis. Valium is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia), athetosis, and stiff-man syndrome. Oral Valium may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy. Launch Date 1963

C_max

Value	Dose	Analyte	Population
317 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
75 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
172 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
208 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01417078	20 mg single, intranasal dose: 20 mg route of administration: intranasal experiment type: single co-administered:	DIAZEPAM plasma	Homo sapiens population: unhealthy age: sex: food status:

AUC

Value	Dose	Analyte	Population
1530 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
330 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
779 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1227 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01417078	20 mg single, intranasal dose: 20 mg route of administration: intranasal experiment type: single co-administered:	DIAZEPAM plasma	Homo sapiens population: unhealthy age: sex: food status:

T_1/2

Value	Dose	Co-administered	Analyte	Population
48 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unknown, oral		DIAZEPAM plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
2% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unknown, oral		DIAZEPAM plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
2000 mg single, oral Overdose Dose: 2000 mg Route: oral Route: single Dose: 2000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/357765	healthy, 28 years Health Status: healthy Age Group: 28 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/357765	Sources: https://pubmed.ncbi.nlm.nih.gov/357765
500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: https://pubmed.ncbi.nlm.nih.gov/357765	unhealthy, 61 years Health Status: unhealthy Age Group: 61 years Sex: F Sources: https://pubmed.ncbi.nlm.nih.gov/357765	Sources: https://pubmed.ncbi.nlm.nih.gov/357765
0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	Other AEs: Respiratory depression, Abuse... Other AEs: Respiratory depression (serious\|grade 5) Abuse (serious\|grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	Disc. AE: Somnolence, Hypoventilation... AEs leading to discontinuation/dose reduction: Somnolence (3 patients) Hypoventilation (2 patients) Rash (2 patients) Asthenia (1 patient) Hyperkinesia (1 patient) Incoordination (1 patient) Vasodilatation (1 patient) Urticaria (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
10 mg 2 times / day multiple, intranasal Recommended Dose: 10 mg, 2 times / day Route: intranasal Route: multiple Dose: 10 mg, 2 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf	Other AEs: Respiratory depression... Other AEs: Respiratory depression (serious\|grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf
10 mg 4 times / day multiple, intramuscular Recommended Dose: 10 mg, 4 times / day Route: intramuscular Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: anxiety disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	Other AEs: Respiratory depression, Abuse... Other AEs: Respiratory depression (serious\|grade 5) Abuse (serious\|grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf
10 mg 4 times / day multiple, oral Recommended Dose: 10 mg, 4 times / day Route: oral Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: OPIOIDS Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: Anxiety Disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	Other AEs: Respiratory depression... Other AEs: Respiratory depression (serious\|grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf

AEs

AE	Significance	Dose	Population
Abuse	serious\|grade 5	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Respiratory depression	serious\|grade 5	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Asthenia	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Hyperkinesia	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Incoordination	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Urticaria	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Vasodilatation	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Hypoventilation	2 patients Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Rash	2 patients Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Somnolence	3 patients Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Respiratory depression	serious\|grade 5	10 mg 2 times / day multiple, intranasal Recommended Dose: 10 mg, 2 times / day Route: intranasal Route: multiple Dose: 10 mg, 2 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf
Abuse	serious\|grade 5	10 mg 4 times / day multiple, intramuscular Recommended Dose: 10 mg, 4 times / day Route: intramuscular Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: anxiety disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf
Respiratory depression	serious\|grade 5	10 mg 4 times / day multiple, intramuscular Recommended Dose: 10 mg, 4 times / day Route: intramuscular Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: anxiety disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf
Respiratory depression	serious\|grade 5	10 mg 4 times / day multiple, oral Recommended Dose: 10 mg, 4 times / day Route: oral Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: OPIOIDS Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: Anxiety Disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737	inhibitor 1767 substrate 1037	inhibitor 1852 substrate 1217	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 707 Cav1.2 45 Nav1.5 97 OCT3 150	CYP2C19 991 CYP1A2 1054 CYP2A6 543 CYP2B6 664 CYP2C8 693 CYP2E1 667 CYP3A5 395

Drug as perpetrator

Target	Modality	Activity
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
OCT3 150	inhibitor 3277 Sources: https://link.springer.com/article/10.1007/s00424-013-1335-8 Page: 1.0	strong [IC50 2 uM]

Drug as victim

Target	Modality	Activity
CYP2B6 664	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	major
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	major
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	major
CYP3A5 395	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	major
CYP1A2 1054	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2A6 543	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2C8 693	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2C9 1037	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2D6 1217	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2E1 667	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Cav1.2 49	inhibitor 1626 Sources: https://static-content.springer.com/esm/art%3A10.1038%2Fsrep02100/MediaObjects/41598_2013_BFsrep02100_MOESM1_ESM.pdf#page=3 Page: 3.0
Nav1.5 100	inhibitor 1626 Sources: https://static-content.springer.com/esm/art%3A10.1038%2Fsrep02100/MediaObjects/41598_2013_BFsrep02100_MOESM1_ESM.pdf#page=3 Page: 3.0
hERG 1647	inhibitor 1626 Sources: https://static-content.springer.com/esm/art%3A10.1038%2Fsrep02100/MediaObjects/41598_2013_BFsrep02100_MOESM1_ESM.pdf#page=3 Page: 3.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:49575	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:49575
ZINC	ZINC000000006427	http://zinc15.docking.org/substances/ZINC000000006427
eMolecules	536763	https://www.emolecules.com/cgi-bin/more?vid=536763

PubMed

Title	Date	PubMed

[The mechanism of the anticonvulsive action of diazepam].	1975 Mar	1125412
The effect of cold and diazepam on the toxicity of fenfluramine in mice.	1975 Mar 15	1116545
[Potentiation of local anesthesia in endonasal surgery].	2001	11247245
Negative inotropic effect of diazepam in isolated guinea pig heart.	2001 Feb	11258448
[Prevention of postoperative nausea and vomiting in gynecologic surgery with 3 fixed doses of metoclopramide, droperidol or placebo].	2001 Feb	11257953
Extracellular serotonin is enhanced in the striatum, but not in the dorsal hippocampus or prefrontal cortex, in rats subjected to an operant conflict procedure.	2001 Feb	11256436
Molecular modeling and QSAR analysis of the interaction of flavone derivatives with the benzodiazepine binding site of the GABA(A) receptor complex.	2001 Feb	11249125
Prenatal stress and postnatal development of neonatal rats--sex-dependent effects on emotional behavior and learning ability of neonatal rats.	2001 Feb	11226753
Acyl-CoA binding protein is essential in bloodstream form Trypanosoma brucei.	2001 Feb	11223138
Lack of reinforcing effect of the benzodiazepine and tricyclic antidepressant combination of diazepam and dothiepin.	2001 Feb	11174084
Effects of different preparations of propofol, diazepam, and etomidate on human neutrophils in vitro.	2001 Feb	11167168
Regional and subunit-specific downregulation of acid-sensing ion channels in the pilocarpine model of epilepsy.	2001 Feb	11162239
Diazepam in the treatment of GHB dependence.	2001 Feb	11157447
[Premedication in ambulatory surgery].	2001 Feb 12	11228790
A model of atypical absence seizures: EEG, pharmacology, and developmental characterization.	2001 Feb 13	11171899
[Febrile convulsions, Treatment and prognosis].	2001 Feb 19	11242670
Alterations in cerebral diazepam binding inhibitor expression in drug dependence: a possible biochemical alteration common to drug dependence.	2001 Feb 2	11233989
[Premedication for endoscopy].	2001 Feb 2	11225389
Inhibition of shock-induced foot tapping behaviour in the gerbil by a tachykinin NK1 receptor antagonist.	2001 Feb 2	11166289
Effects of a novel uncompetitive NMDA receptor antagonist, MRZ 2/579 on ethanol self-administration and ethanol withdrawal seizures in the rat.	2001 Feb 9	11173066
Evaluation of native GABA(A) receptors containing an alpha 5 subunit.	2001 Feb 9	11173064
Chronic benzodiazepine administration facilitates the subsequent development of ethanol dependence.	2001 Feb 9	11164828
The role of nitrergic system in lidocaine-induced convulsion in the mouse.	2001 Jan	11243580
[Anesthesia for a patient with cardiac sarcoidosis].	2001 Jan	11211755
Development of differential tolerance to the sedative and anti-stress effects of benzodiazepines.	2001 Jan	11211563
Effect of diazepam and midazolam on the antinociceptive effect of morphine, metamizol and indomethacin in mice.	2001 Jan	11210678
[Effect of diazepam on apnea attacks in a 6-year-old girl with Rett syndrome: a polysomnographic study].	2001 Jan	11197898
Neuropharmacological actions of some binuclear lanthanide(III) complexes.	2001 Jan	11166680
Sedative properties of the decoction of the rhizome of Cyperus articulatus.	2001 Jan	11163936
Treatment of nonfebrile status epilepticus in Rochester, Minn, from 1965 through 1984.	2001 Jan	11155411
Effects of melatonin, morphine and diazepam on formalin-induced nociception in mice.	2001 Jan 12	11213364
Detection of aneuploidy in rodent and human sperm by multicolor FISH after chronic exposure to diazepam.	2001 Jan 25	11152967
In vivo, the direct and seizure-induced neuronal cytotoxicity of kainate and AMPA is modified by the non-competitive antagonist, GYKI 52466.	2001 Jan 26	11164769
Simple and sensitive high-performance liquid chromatographic method for the determination of 1,5-benzodiazepine clobazam and its active metabolite N-desmethylclobazam in human serum and urine with application to 1,4-benzodiazepines analysis.	2001 Jan 5	11204222
Brain-derived neurotrophic factor superinduction parallels anti-epileptic--neuroprotective treatment in the pilocarpine epilepsy model.	2001 Mar	11259499
[3H]Ro 15-1788 binding sites to brain membrane of the saltwater Mugil cephalus.	2001 Mar	11255103
Topical anesthesia for cataract surgery: a population-based perspective.	2001 Mar	11255059
Effect of leaf essential oil from Piper solmsianum C.DC. in mice behaviour.	2001 Mar	11246267
Molecular targets for the myorelaxant action of diazepam.	2001 Mar	11179437
Anxiogenic-like effects limit rewarding effects of cocaine in balb/cbyj mice.	2001 Mar	11166520
Modulation of GABA(A) receptors by benzodiazepines and barbiturates is autonomous of PKC activation.	2001 Mar	11166325
Trimethylolpropane phosphate induces epileptiform discharges in the CA1 region of the rat hippocampus.	2001 Mar 1	11222088
A behavioral economic analysis of polydrug abuse in alcoholics: asymmetrical substitution of alcohol and cocaine.	2001 Mar 1	11173165
Evidence for a common binding cavity for three general anesthetics within the GABAA receptor.	2001 Mar 15	11245705
Female gastrin-releasing peptide receptor (GRP-R)-deficient mice exhibit altered social preference for male conspecifics: implications for GRP/GRP-R modulation of GABAergic function.	2001 Mar 16	11251202
Dual effects of melatonin on barbiturate-induced narcosis in rats.	2001 Mar 16	11226639
Systemic EMD 68843 injections reduce anxiety in the shock-probe, but not the plus-maze test.	2001 Mar 2	11239925
The octadecaneuropeptide [diazepam-binding inhibitor (33-50)] exerts potent anorexigenic effects in rodents.	2001 Mar 2	11239923
The R100Q mutation of the GABA(A) alpha(6) receptor subunit may contribute to voluntary aversion to ethanol in the sNP rat line.	2001 Mar 5	11245930

Patents

Sample Use Guides

In Vivo Use Guide

Tale 2-10 mg, 2 to 4 times daily.

Route of Administration: Oral

In Vitro Use Guide

Rat brain membranes were treated with diazepam (1-1000 nM) and the drug was shown to enhance the effects of iontophoretically applied GABA.

Name

Type

Language

DIAZEPAM

Official Name

English

VALTOCO

Brand Name

English

RO 5-2807

Code

English

DIAZEPAM [VANDF]

Common Name

English

ANSIOLISINA

Common Name

English

DIAZEPAM CIV

Common Name

English

VALIUM

Brand Name

English

LA-III

Code

English

DIAZEPAM [GREEN BOOK]

Common Name

English

DIZAC

Brand Name

English

SERVIZEPAM

Common Name

English

DIAZEPAM [IARC]

Common Name

English

RO-5-2807

Code

English

DIAZEPAM [USAN]

Common Name

English

DIASTAT

Brand Name

English

NSC-77518

Code

English

LA III

Code

English

2H-1,4-BENZODIAZEPIN-2-ONE, 7-CHLORO-1,3-DIHYDRO-1-METHYL-5-PHENYL-

Systematic Name

English

NSC-169897

Code

English

DIAZEPAM [ORANGE BOOK]

Common Name

English

RO-52807

Code

English

7-CHLORO-1-METHYL-5-PHENYL-3H-1,4-BENZODIAZEPIN-2(1H)-ONE

Systematic Name

English

DIAZEPAM [HSDB]

Common Name

English

WY-3467

Code

English

METHYL DIAZEPINONE

Systematic Name

English

CENTRAZEPAM

Common Name

English

Q-PAM

Brand Name

English

7-CHLORO-1,3-DIHYDRO-1-METHYL-5-PHENYL-2H-1,4-BENZODIAZEPINE-2-ONE

Systematic Name

English

VALRELEASE

Brand Name

English

DIAZEPAM [MART.]

Common Name

English

DIACEPIN

Common Name

English

Diazepam [WHO-DD]

Common Name

English

DIAZEPAM [MI]

Common Name

English

diazepam [INN]

Common Name

English

DIAZEPAM [USP MONOGRAPH]

Common Name

English

DIAZEPAM [JAN]

Common Name

English

NRL-1

Code

English

DIAZEPAM [EP MONOGRAPH]

Common Name

English

DIAZEPAM CIV [USP-RS]

Common Name

English

7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one

Systematic Name

English

TRANQUASE

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000007542