DIAZEPAM HYDROCHLORIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H13ClN2O.ClH
Molecular Weight	321.2016
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1c2ccc(cc2C(=NCC1=O)c3ccccc3)Cl.Cl

InChI

InChIKey=BPYZIOINRAWEQL-UHFFFAOYSA-N

InChI=1S/C16H13ClN2O.ClH/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;1H

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.4609
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C16H13ClN2O
Molecular Weight	284.7408
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

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 37 Target ID: CHEMBL2109243 Sources: http://www.hamiltonhealthsciences.ca/workfiles/basehospital/diazepam.pdf	Agonist 2470		8.6 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Anxiety 245 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Primary	Approved 8043	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 -1.93449607E11
Acute alcohol withdrawal 2 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8043	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 -1.93449607E11
Muscle spasm 40 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8043	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 -1.93449607E11
Convulsive disorders 2 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8043	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 -1.93449607E11

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 1601	inhibitor 1604 substrate 936	inhibitor 1702 substrate 1118	inhibitor 1475

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 627 Cav1.2 45 Nav1.5 93 OCT3 140	CYP2C19 910 CYP1A2 972 CYP2A6 485 CYP2B6 616 CYP2C8 634 CYP2E1 606 CYP3A5 367

Drug as perpetrator

Target	Modality	Activity
CYP2A6 659	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
CYP2C9 1648	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
CYP2D6 1738	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
OCT3 140	inhibitor 3045 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 616	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	major
CYP2C19 910	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	major
CYP3A4 1601	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	major
CYP3A5 367	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	major
CYP1A2 972	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2A6 485	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2C8 634	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2C9 936	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2D6 1118	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2E1 606	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Cav1.2 48	inhibitor 1489 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 96	inhibitor 1489 Sources: https://static-content.springer.com/esm/art%3A10.1038%2Fsrep02100/MediaObjects/41598_2013_BFsrep02100_MOESM1_ESM.pdf#page=3 Page: 3.0
hERG 1507	inhibitor 1489 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
Letter: Clonazepam in the treatment of drug-induced dyskinesia.	1975 Feb 1	1111773
[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
Diazepam withdrawal syndrome: a case with psychosis, seizure, and coma.	1979 Jan	103443
Influence of adenosine agonists and antiepileptic drugs on theophylline-induced seizures in rats.	1998 Oct	10874349
Chlorambucil-induced seizure in a patient with nephrotic syndrome.	1999	10450047
Binding, partial agonism, and potentiation of alpha(1)-adrenergic receptor function by benzodiazepines: A potential site of allosteric modulation.	1999 Dec	10565838
Distinct features of seizures induced by cocaine and amphetamine analogs.	1999 Jul 21	10456426
Effects of diazepam on extracellular brain neurotransmitters in pilocarpine-induced seizures in rats.	1999 Jun 4	10414434
Involvement of nitric oxide and nitric oxide synthase activity in anticonvulsive action.	1999 Mar 1	10357070
Effects of L-arginine on picrotoxin-induced increase in brain ammonia concentrations and convulsions in rats.	1999 Oct	10776465
Transient syncope and ECG changes associated with the concurrent administration of clozapine and diazepam.	1999 Sep	10520983
Syndrome of inappropriate secretion of antidiuretic hormone complicating neonatal diazepam withdrawal.	2000 Apr	10830465
Seizures caused by possible interaction between olanzapine and clomipramine.	2000 Apr	10770480
The pharmacodynamics of PK 11195 in diazepam-dependent male and female rats.	2000 Aug	10973513
Acute adverse reaction to fentanyl in a 55 year old man.	2000 Aug	10960295
Randomized, double-blind, placebo-controlled trial of diazepam, nitroglycerin, or both for treatment of patients with potential cocaine-associated acute coronary syndromes.	2000 Aug	10958127
Ketamine potentiates cerebrocortical damage induced by the common anaesthetic agent nitrous oxide in adult rats.	2000 Aug	10928976
Manic episode in an ifosfamide-treated patient.	2000 Jan-Feb	10766557
Mice lacking the long splice variant of the gamma 2 subunit of the GABA(A) receptor are more sensitive to benzodiazepines.	2000 Jun	10880692
Heterogeneity of GABA(A) receptor-mediated responses in the human IMR-32 neuroblastoma cell line.	2000 May 15	10797553
Etomidate-induced convulsion prior to electroconvulsive therapy.	2000 Oct	11116789
Analgesic effect of intravenous ketamine in cancer patients on morphine therapy: a randomized, controlled, double-blind, crossover, double-dose study.	2000 Oct	11027905
Flumazenil prevents diazepam-elicited anticonvulsant action and concomitant attenuation of glutamate overflow.	2000 Oct 27	11050301
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
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
[Febrile convulsions, Treatment and prognosis].	2001 Feb 19	11242670
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
Effect of diazepam and midazolam on the antinociceptive effect of morphine, metamizol and indomethacin in mice.	2001 Jan	11210678
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 antiepileptic drugs on rat platelet aggregation: ex vivo and in vitro study.	2001 Jan	11137387
The efficacy of oral clonidine premedication in the prevention of postoperative vomiting in children following strabismus surgery.	2001 Jan	11123735
Enhanced cortical extracellular levels of cholecystokinin-like material in a model of anticipation of social defeat in the rat.	2001 Jan 1	11150343
Diazepam and nicotine increase social interaction in gerbils: a test for anxiolytic action.	2001 Jan 12	11150490
Long-term reduction of benzodiazepine receptor density in the rat cerebellum by acute seizures and kindling and its recovery 6 months later by a pentylenetetrazole challenge.	2001 Jan 12	11150477
Detection of aneuploidy in rodent and human sperm by multicolor FISH after chronic exposure to diazepam.	2001 Jan 25	11152967
Topical anesthesia for cataract surgery: a population-based perspective.	2001 Mar	11255059
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
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
Targeted disruption of the GABA(A) receptor delta subunit gene leads to an up-regulation of gamma 2 subunit-containing receptors in cerebellar granule cells.	2001 Mar 30	11136737
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.

Substance Class	Chemical Created by `admin` on `Sat Jun 26 15:30:17 UTC 2021` Edited by `admin` on `Sat Jun 26 15:30:17 UTC 2021`
Record UNII	6JD21U639H
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

DIAZEPAM HYDROCHLORIDE

Common Name

English

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

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1012