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

General Information of Drug (ID: DMOJZQ9)

Drug Name
Loperamide Drug Info
Synonyms
Ioperamide; Loperacap; Loperamida; Loperamidum; Kaopectate II; Loperamide Monohydrochloride; Pepto Diarrhea Control; Apo-Loperamide; Diamide (TN); Diarr-Eze; Dimor (TN); Imodium (TN); Imodium A-D Caplets; Loperamida [INN-Spanish]; Loperamide (INN); Loperamide [INN:BAN]; Loperamidum [INN-Latin]; Lopex (TN); Maalox Anti-Diarrheal; Nu-Loperamide; PMS-Loperamide; Pepto (TN); R-18553; Rho-Loperamide
Indication
Disease Entry ICD 11 Status REF
Diarrhea ME05.1 Approved [1]
Traveler's diarrhea ME05.1 Approved [2]
Middle East Respiratory Syndrome (MERS) 1D64 Preclinical [3]
Severe acute respiratory syndrome (SARS) 1D65 Preclinical [3]
Therapeutic Class
Antidiarrheals
Cross-matching ID
PubChem CID
3955
ChEBI ID
CHEBI:6532
CAS Number
CAS 53179-11-6
TTD Drug ID
DMOJZQ9
VARIDT Drug ID
DR00171
INTEDE Drug ID
DR0974
ACDINA Drug ID
D00373

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Opioid receptor delta (OPRD1) TT27RFC OPRD_HUMAN Binder [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [6]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [7]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [7]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Approved [7]
Oxygen-insensitive NADPH nitroreductase A (nfsA) DEDPI65 NFSA_ECOLI Approved [8]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Opioid receptor delta (OPRD1) DTT OPRD1 2.848 2.263 1.536 2
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
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 Diarrhea
ICD Disease Classification ME05.1
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Opioid receptor delta (OPRD1) DTT OPRD1 5.52E-01 0.03 0.23
P-glycoprotein 1 (ABCB1) DTP P-GP 7.83E-01 4.69E-02 1.89E-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 2D6 (CYP2D6) DME CYP2D6 5.64E-01 2.36E-02 1.75E-01
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 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 Loperamide FDA Label
3 Screening of an FDA-approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture Antimicrob Agents Chemother. 2014 Aug;58(8):4875-84.
4 Loperamide: evidence of interaction with mu and delta opioid receptors. Life Sci. 1983;33 Suppl 1:315-8.
5 In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system. Drug Metab Dispos. 2008 Feb;36(2):268-75.
6 Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7 Suppl 3:S11-8.
7 Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes. Eur J Clin Pharmacol. 2004 Oct;60(8):575-81.
8 Reduction of the prodrug loperamide oxide to its active drug loperamide in the gut of rats, dogs, and humans. Drug Metab Dispos. 1995 Mar;23(3):354-62.