Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM08E9O)

Drug Name
Diazepam Drug Info
Synonyms
diazepam; Valium; 439-14-5; Diazemuls; Ansiolisina; Sibazon; Relanium; Faustan; Apaurin; Stesolid; Seduxen; Methyldiazepinone; Valitran; Tranqdyn; Seduksen; Relaminal; Quiatril; Quetinil; Dipezona; Diazetard; Diazepan; Calmpose; Tranimul; Tensopam; Serenack; Paranten; Kiatrium; Domalium; Condition; Bialzepam; Ansiolin; Unisedil; Stesolin; Serenamin; Ruhsitus; Renborin; Quievita; Tranquirit; Serenzin; Neurolytril; Liberetas; Diacepan; Ceregulart; Calmocitene; Bensedin; Atensine; Apozepam; Umbrium; Sonacon; Sedipam; Levium; Diapam; Atilen; Assival; Amiprol; Diazepam (intranasal, epilepsy)
Indication
Disease Entry ICD 11 Status REF
Alcohol withdrawal Approved [1]
Alcohol withdrawal delirium Approved [1]
Anxiety Approved [1]
Epilepsy 8A60-8A68 Approved [2]
Tetanus 1C13 Investigative [1]
Cross-matching ID
PubChem CID
3016
ChEBI ID
CHEBI:49575
CAS Number
CAS 439-14-5
TTD Drug ID
DM08E9O
VARIDT Drug ID
DR00999
INTEDE Drug ID
DR0480
ACDINA Drug ID
D00190

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Translocator protein (TSPO) TTPTXIN TSPO_HUMAN Agonist [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [5]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [6]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [7]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Approved [8]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [9]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [10]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Approved [11]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Approved [12]
Prostaglandin G/H synthase 1 (COX-1) DE073H6 PGH1_HUMAN Approved [13]
Cytochrome P450 2C18 (CYP2C18) DEZMWRE CP2CI_HUMAN Approved [14]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Translocator protein (TSPO) DTT TSPO 7.51 8.89 7.64 8.008
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Cytochrome P450 2C18 (CYP2C18) DME CYP2C18 8.485 5.28 4.621 8.889
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Prostaglandin G/H synthase 1 (COX-1) DME PTGS1 6.09 7.747 6.04 7.023
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Alcohol withdrawal
ICD Disease Classification
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Translocator protein (TSPO) DTT TSPO 2.65E-05 1.98 4.26
P-glycoprotein 1 (ABCB1) DTP P-GP 7.45E-02 -1.49E-01 -3.47E-01
Cytochrome P450 2C18 (CYP2C18) DME CYP2C18 7.46E-02 -1.26E-01 -3.29E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 7.62E-02 -1.65E-01 -6.38E-01
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 7.53E-01 1.26E-01 4.92E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 7.68E-02 -2.10E-01 -6.42E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 1.34E-01 -2.79E-01 -7.05E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 5.48E-01 1.12E-01 7.24E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 4.28E-02 -1.99E-01 -6.09E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 9.81E-01 2.72E-01 6.95E-01
Prostaglandin G/H synthase 1 (COX-1) DME PTGS1 7.25E-01 -4.31E-02 -5.74E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Diazepam FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3364).
3 Translocator protein (18 kDa) mediates the pro-growth effects of diazepam on Ehrlich tumor cells in vivo. Eur J Pharmacol. 2010 Jan 25;626(2-3):131-8.
4 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
5 Comparative study of the metabolism of drug substrates by human cytochrome P450 3A4 expressed in bacterial, yeast and human lymphoblastoid cells. Xenobiotica. 2002 Nov;32(11):937-47.
6 Phenytoin-diazepam interaction. Ann Pharmacother. 2003 May;37(5):659-63.
7 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
8 In vitro metabolism of zolmitriptan in rat cytochromes induced with beta-naphthoflavone and the interaction between six drugs and zolmitriptan. Chem Biol Interact. 2003 Dec 15;146(3):263-72.
9 Eight inhibitory monoclonal antibodies define the role of individual P-450s in human liver microsomal diazepam, 7-ethoxycoumarin, and imipramine metabolism. Drug Metab Dispos. 1999 Jan;27(1):102-9.
10 Inhibitory monoclonal antibody to human cytochrome P450 2B6. Biochem Pharmacol. 1998 May 15;55(10):1633-40.
11 Use of inhibitory monoclonal antibodies to assess the contribution of cytochromes P450 to human drug metabolism. Eur J Pharmacol. 2000 Apr 14;394(2-3):199-209.
12 Drug Interactions Flockhart Table
13 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
14 Targeted antipeptide antibodies to cytochrome P450 2C18 based on epitope mapping of an inhibitory monoclonal antibody to P450 2C51. Arch Biochem Biophys. 1997 Feb 15;338(2):157-64.