General Information of Drug (ID: DMB4OLE)

Drug Name
Propofol Drug Info
Synonyms
Ampofol; Aquafol; Diisopropylphenol; Dipravan; Diprivan; Disoprivan; Disoprofol; Fresofol; Ivofol; PFL; Propofolum; Rapinovet; Recofol; Abbott Brand of Propofol; Alpha Brand of Propofol; Astra Brand of Propofol; AstraZeneca Brand of Propofol; Braun Brand of Propofol; Curamed Brand of Propofol; Diprivan Injectable emulsion; Fresenius Brand of Propofol; Fresenius Kabi Brand of Propofol; Juste Brand of Propofol; Parnell Brand of Propofol; Pisa Brand of Propofol; Propofol Abbott; Propofol Fresenius; Propofol MCT; Propofol Rovi; Propofolum [Latin]; Rovi Brand of Propofol; Schering Brand of Propofol; Zeneca Brand of Propofol; AM-149; DDS-04F; Diprivan (TN); Propofol IDD-D; Propofol-Lipuro; ZD-0859; Ghl.PD_Mitscher_leg0.558; Propofol [USAN:INN:BAN]; Propofol (JAN/USAN/INN); Propofol(2,6-Diisopropylphenol); 2, 6-Diisopropylphenol; 2,6 Diisopropylphenol; 2,6-Bis(1-methylethyl)phenol; 2,6-Bis(Isopropyl)-phenol; 2,6-DIISOPROPYLPHENOL; 2,6-Diisopropyl phenol; 2,6-Diisopropylphenol; 2,6-bis(1-methylethyl)-phenol; 2,6-di(propan-2-yl)phenol
Indication
Disease Entry ICD 11 Status REF
Anaesthesia 9A78.6 Approved [1]
Leukemia Approved [2]
Traumatic brain injury NA07.Z Approved [2]
Coronavirus Disease 2019 (COVID-19) 1D6Y Investigative [3]
Therapeutic Class
Hypnotics and Sedatives
Cross-matching ID
PubChem CID
4943
ChEBI ID
CHEBI:44915
CAS Number
CAS 2078-54-8
TTD Drug ID
DMB4OLE
VARIDT Drug ID
DR00424
INTEDE Drug ID
DR1365
ACDINA Drug ID
D01367

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Fatty acid amide hydrolase (FAAH) TTDP1UC NOUNIPROTAC Inhibitor [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 2E1 (CYP2E1) DEVDYN7 CP2E1_HUMAN Approved [6]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [7]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [5]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Approved [8]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [9]
Cytochrome P450 2A6 (CYP2A6) DEJVYAZ CP2A6_HUMAN Approved [9]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Approved [6]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [10]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Approved [9]
UDP-glucuronosyltransferase 1A9 (UGT1A9) DE85D2P UD19_HUMAN Approved [11]
UDP-glucuronosyltransferase 1A6 (UGT1A6) DESD26P UD16_HUMAN Approved [12]
Cytochrome P450 2C18 (CYP2C18) DEZMWRE CP2CI_HUMAN Approved [9]
Oleamide hydrolase 1 (FAAH) DEUM1EX FAAH1_HUMAN Approved [13]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Fatty acid amide hydrolase (FAAH) DTT FAAH 5.744 5.044 4.818 5.984
Cytochrome P450 2C18 (CYP2C18) DME CYP2C18 8.485 5.28 4.621 8.889
Cytochrome P450 2E1 (CYP2E1) DME CYP2E1 12.054 3.968 2.945 4.1
Oleamide hydrolase 1 (FAAH) DME FAAH 5.744 5.044 4.818 5.984
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Cytochrome P450 2A6 (CYP2A6) DME CYP2A6 10.644 6.631 6.598 6.937
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
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
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 Anaesthesia
ICD Disease Classification 9A78.6
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Fatty acid amide hydrolase (FAAH) DTT NO-GeName 2.65E-01 0.02 0.1
Cytochrome P450 2C18 (CYP2C18) DME CYP2C18 7.90E-01 3.72E-02 2.95E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 1.87E-01 4.98E-02 3.61E-01
Cytochrome P450 2E1 (CYP2E1) DME CYP2E1 9.06E-01 -5.05E-02 -1.20E-01
Oleamide hydrolase 1 (FAAH) DME FAAH 2.65E-01 2.41E-02 1.04E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 3.17E-01 -6.95E-02 -2.88E-01
Cytochrome P450 2B6 (CYP2B6) DME CYP2B6 5.79E-01 -1.30E-02 -9.78E-02
Cytochrome P450 2A6 (CYP2A6) DME CYP2A6 2.21E-02 9.40E-02 6.62E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 8.68E-01 3.64E-02 2.72E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.66E-01 9.19E-03 4.88E-02
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 5.64E-01 2.36E-02 1.75E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 7.83E-01 2.32E-03 1.53E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 6.06E-01 -2.42E-02 -1.64E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 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: 5464).
2 Propofol FDA Label
3 Propofol and sedation in patients with coronavirus disease. Am J Emerg Med. 2020 Jun 18;S0735-6757(20)30512-X.
4 Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
5 Cytochrome P-450 2B6 is responsible for interindividual variability of propofol hydroxylation by human liver microsomes. Anesthesiology. 2001 Jan;94(1):110-9.
6 Inhibition of cytochrome P450 2E1 by propofol in human and porcine liver microsomes. Biochem Pharmacol. 2002 Oct 1;64(7):1151-6.
7 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
8 Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
9 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
10 Involvement of human cytochrome P450 2B6 in the omega- and 4-hydroxylation of the anesthetic agent propofol. Xenobiotica. 2007 Jul;37(7):717-24.
11 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.
12 Pharmacokinetics of propofol and extrahepatic UGT1A6 gene expression in anhepatic rats. Pharmacology. 2009;84(4):219-26.
13 Update of TTD: therapeutic target database. Nucleic Acids Res. 2010 Jan;38(Database issue):D787-91.