DIAZEPAM HYDROCHLORIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H13ClN2O.ClH
Molecular Weight	321.201
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CN1C2=CC=C(Cl)C=C2C(=NCC1=O)C3=CC=CC=C3

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	36.461
Charge	0
Count

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

Molecular Formula	C16H13ClN2O
Molecular Weight	284.74
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 38 Target ID: CHEMBL2109243 Sources: http://www.hamiltonhealthsciences.ca/workfiles/basehospital/diazepam.pdf	Agonist 2752		8.6 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Anxiety 275 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Primary	Approved 8583	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 8583	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 41 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8583	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 8583	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
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:
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
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

AUC

Value	Dose	Analyte	Population
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:
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
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

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 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 Health Status: unhealthy Age Group: > 12 years 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 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	unhealthy, adult Health Status: unhealthy 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unhealthy, adult Health Status: unhealthy 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 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 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 Health Status: unhealthy Age Group: > 12 years 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 Health Status: unhealthy Age Group: > 12 years 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 Health Status: unhealthy Age Group: > 12 years 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 Health Status: unhealthy Age Group: > 12 years 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 Health Status: unhealthy Age Group: > 12 years 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 Health Status: unhealthy Age Group: > 12 years 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 Health Status: unhealthy Age Group: > 12 years 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 Health Status: unhealthy Age Group: > 12 years 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 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	unhealthy, adult Health Status: unhealthy 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	unhealthy, adult Health Status: unhealthy 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946	inhibitor 2438 substrate 1193	inhibitor 2507 substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 879 Cav1.2 58 Nav1.5 116 OCT3 159	CYP2C19 1119 CYP1A2 1197 CYP2A6 626 CYP2B6 776 CYP2C8 810 CYP2E1 729 CYP3A5 446

Drug as perpetrator

Target	Modality	Activity
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
OCT3 161	inhibitor 4027 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 776	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	major
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	major
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	major
CYP3A5 446	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	major
CYP1A2 1197	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2A6 626	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2C8 810	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2C9 1193	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2E1 729	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Cav1.2 63	inhibitor 2237 Sources: https://static-content.springer.com/esm/art%3A10.1038%2Fsrep02100/MediaObjects/41598_2013_BFsrep02100_MOESM1_ESM.pdf#page=3 Page: 3.0
Nav1.5 119	inhibitor 2237 Sources: https://static-content.springer.com/esm/art%3A10.1038%2Fsrep02100/MediaObjects/41598_2013_BFsrep02100_MOESM1_ESM.pdf#page=3 Page: 3.0
hERG 2263	inhibitor 2237 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
eMolecules	536763	https://www.emolecules.com/cgi-bin/more?vid=536763
ZINC	ZINC000000006427	http://zinc15.docking.org/substances/ZINC000000006427

PubMed

Title	Date	PubMed
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.	2001-03-16	11251202
Dual effects of melatonin on barbiturate-induced narcosis in rats.	2001-03-16	11226639
Evidence for a common binding cavity for three general anesthetics within the GABAA receptor.	2001-03-15	11245705
The R100Q mutation of the GABA(A) alpha(6) receptor subunit may contribute to voluntary aversion to ethanol in the sNP rat line.	2001-03-05	11245930
Systemic EMD 68843 injections reduce anxiety in the shock-probe, but not the plus-maze test.	2001-03-02	11239925
The octadecaneuropeptide [diazepam-binding inhibitor (33-50)] exerts potent anorexigenic effects in rodents.	2001-03-02	11239923
Trimethylolpropane phosphate induces epileptiform discharges in the CA1 region of the rat hippocampus.	2001-03-01	11222088
A behavioral economic analysis of polydrug abuse in alcoholics: asymmetrical substitution of alcohol and cocaine.	2001-03-01	11173165
Brain-derived neurotrophic factor superinduction parallels anti-epileptic--neuroprotective treatment in the pilocarpine epilepsy model.	2001-03	11259499
[3H]Ro 15-1788 binding sites to brain membrane of the saltwater Mugil cephalus.	2001-03	11255103
Topical anesthesia for cataract surgery: a population-based perspective.	2001-03	11255059
Effect of leaf essential oil from Piper solmsianum C.DC. in mice behaviour.	2001-03	11246267
Molecular targets for the myorelaxant action of diazepam.	2001-03	11179437
Anxiogenic-like effects limit rewarding effects of cocaine in balb/cbyj mice.	2001-03	11166520
Modulation of GABA(A) receptors by benzodiazepines and barbiturates is autonomous of PKC activation.	2001-03	11166325
[Febrile convulsions, Treatment and prognosis].	2001-02-19	11242670
A model of atypical absence seizures: EEG, pharmacology, and developmental characterization.	2001-02-13	11171899
[Premedication in ambulatory surgery].	2001-02-12	11228790
Effects of a novel uncompetitive NMDA receptor antagonist, MRZ 2/579 on ethanol self-administration and ethanol withdrawal seizures in the rat.	2001-02-09	11173066
Evaluation of native GABA(A) receptors containing an alpha 5 subunit.	2001-02-09	11173064
Chronic benzodiazepine administration facilitates the subsequent development of ethanol dependence.	2001-02-09	11164828
Alterations in cerebral diazepam binding inhibitor expression in drug dependence: a possible biochemical alteration common to drug dependence.	2001-02-02	11233989
[Premedication for endoscopy].	2001-02-02	11225389
Inhibition of shock-induced foot tapping behaviour in the gerbil by a tachykinin NK1 receptor antagonist.	2001-02-02	11166289
Negative inotropic effect of diazepam in isolated guinea pig heart.	2001-02	11258448
[Prevention of postoperative nausea and vomiting in gynecologic surgery with 3 fixed doses of metoclopramide, droperidol or placebo].	2001-02	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.	2001-02	11256436
Molecular modeling and QSAR analysis of the interaction of flavone derivatives with the benzodiazepine binding site of the GABA(A) receptor complex.	2001-02	11249125
Prenatal stress and postnatal development of neonatal rats--sex-dependent effects on emotional behavior and learning ability of neonatal rats.	2001-02	11226753
Acyl-CoA binding protein is essential in bloodstream form Trypanosoma brucei.	2001-02	11223138
Lack of reinforcing effect of the benzodiazepine and tricyclic antidepressant combination of diazepam and dothiepin.	2001-02	11174084
Effects of different preparations of propofol, diazepam, and etomidate on human neutrophils in vitro.	2001-02	11167168
Regional and subunit-specific downregulation of acid-sensing ion channels in the pilocarpine model of epilepsy.	2001-02	11162239
Diazepam in the treatment of GHB dependence.	2001-02	11157447
In vivo, the direct and seizure-induced neuronal cytotoxicity of kainate and AMPA is modified by the non-competitive antagonist, GYKI 52466.	2001-01-26	11164769
Detection of aneuploidy in rodent and human sperm by multicolor FISH after chronic exposure to diazepam.	2001-01-25	11152967
Intranasal midazolam for treating febrile seizures in children. Buccal midazolam for childhood seizures at home preferred to rectal diazepam.	2001-01-13	11203721
Effects of melatonin, morphine and diazepam on formalin-induced nociception in mice.	2001-01-12	11213364
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.	2001-01-05	11204222
The role of nitrergic system in lidocaine-induced convulsion in the mouse.	2001-01	11243580
[Anesthesia for a patient with cardiac sarcoidosis].	2001-01	11211755
Development of differential tolerance to the sedative and anti-stress effects of benzodiazepines.	2001-01	11211563
Effect of diazepam and midazolam on the antinociceptive effect of morphine, metamizol and indomethacin in mice.	2001-01	11210678
[Effect of diazepam on apnea attacks in a 6-year-old girl with Rett syndrome: a polysomnographic study].	2001-01	11197898
Neuropharmacological actions of some binuclear lanthanide(III) complexes.	2001-01	11166680
Sedative properties of the decoction of the rhizome of Cyperus articulatus.	2001-01	11163936
Treatment of nonfebrile status epilepticus in Rochester, Minn, from 1965 through 1984.	2001-01	11155411
[Potentiation of local anesthesia in endonasal surgery].	2001	11247245
The effect of cold and diazepam on the toxicity of fenfluramine in mice.	1975-03-15	1116545
[The mechanism of the anticonvulsive action of diazepam].	1975-03	1125412

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 `Mon Mar 31 19:51:50 GMT 2025` Edited by `admin` on `Mon Mar 31 19:51:50 GMT 2025`
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

Preferred Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1012