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

General Information of Drug (ID: DM5PCS7)

Drug Name
Bupropion Drug Info
Synonyms
bupropion; Amfebutamone; 34911-55-2; Amfebutamon; 2-(tert-butylamino)-1-(3-chlorophenyl)propan-1-one; amfebutamonum; Amfebutamona; (+-)-Bupropion; Wellbatrin; Bupropion [INN:BAN]; 34841-39-9; Elontril; Amfebutamonum [INN-Latin]; Zyban; Amfebutamona [INN-Spanish]; Bupropion SR; AMFEBUTAMONE HCl; alpha-(tert-butylamino)-m-chloropropiophenone; CHEMBL894; BRN 2101062; (+-)-1-(3-chlorophenyl)-2-((1,1-dimethylethyl)amino)-1-propanone; CHEBI:3219; SNPPWIUOZRMYNY-UHFFFAOYSA-N; 1-(3-chlorophenyl)-2-[(1,1-dimethylethyl)amino]propan-1-one; Amfebutamon; Amfebutamonum; Elont; Bupropion Hcl; Bupropion hydrocloride; Bupropion (INN); Bupropion (Old RN); Bupropion (USAN); Alpha-(tert-Butylamino)-m-chloropropiophenone; Alpha-(tert-butylamino)-m-chloropropiophenone; (-)-2-(tert-Butylamino)-3'-chloropropiophenone; (-)-2-(tert-Butylamino)-3'-chlorpropiophenon; 1-Propanone; 2-(Tert-Butylamino)-3'-chloropropiophenone
Indication
Disease Entry ICD 11 Status REF
Depression 6A70-6A7Z Approved [1]
Lung cancer 2C25.0 Approved [1]
Major depressive disorder 6A70.3 Approved [1]
Obesity 5B81 Approved [1]
Seasonal affective disorder Approved [1]
Smoking dependence 6C4A.2 Approved [2]
Cross-matching ID
PubChem CID
444
ChEBI ID
CHEBI:3219
CAS Number
CAS 34911-55-2
TTD Drug ID
DM5PCS7
VARIDT Drug ID
DR00836
INTEDE Drug ID
DR0247
ACDINA Drug ID
D00083

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Norepinephrine transporter (NET) TTAWNKZ SC6A2_HUMAN Inhibitor [3]
Serotonin transporter (SERT) TT3ROYC SC6A4_HUMAN Inhibitor [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [4]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
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 [8]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Approved [9]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Norepinephrine transporter (NET) DTT SLC6A2 2.459 3.426 3.322 3.35
Serotonin transporter (SERT) DTT SLC6A4 6.278 5.469 6.075 6.966
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Cytochrome P450 2E1 (CYP2E1) DME CYP2E1 12.054 3.968 2.945 4.1
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
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

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

ICD Disease Classification 06 Mental, behavioural or neurodevelopmental disorder
Disease Class ICD-11: 6A20 Schizophrenia
The Studied Tissue Pre-frontal cortex
The Studied Disease Major depressive disorder [ICD-11:6A20]
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Norepinephrine transporter (NET) DTT SLC6A2 7.05E-01 7.02E-03 0.07
Serotonin transporter (SERT) DTT SLC6A4 1.17E-01 0.07 0.59
P-glycoprotein 1 (ABCB1) DTP P-GP 7.83E-01 4.69E-02 1.89E-01
Breast cancer resistance protein (ABCG2) DTP BCRP 3.72E-02 -1.56E-01 -4.33E-01
Cytochrome P450 2E1 (CYP2E1) DME CYP2E1 9.06E-01 -5.05E-02 -1.20E-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 2C9 (CYP2C9) DME CYP2C9 7.83E-01 2.32E-03 1.53E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Bupropion FDA Label
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
3 Clinically relevant drug interactions with new generation antidepressants and antipsychotics. Ther Umsch. 2009 Jun;66(6):485-92.
4 Role of transporter-mediated efflux in the placental biodisposition of bupropion and its metabolite, OH-bupropion. Biochem Pharmacol. 2010 Oct 1;80(7):1080-6.
5 Sertraline and its metabolite desmethylsertraline, but not bupropion or its three major metabolites, have high affinity for P-glycoprotein. Biol Pharm Bull. 2008 Feb;31(2):231-4.
6 Validation of bupropion hydroxylation as a selective marker of human cytochrome P450 2B6 catalytic activity. Drug Metab Dispos. 2000 Oct;28(10):1222-30.
7 In vitro to in vivo extrapolation of the complex drug-drug interaction of bupropion and its metabolites with CYP2D6; simultaneous reversible inhibition and CYP2D6 downregulation. Biochem Pharmacol. 2017 Jan 1;123:85-96.
8 Product Monograph of Wellbutrin SR(Bupropion Hydrochloride).
9 Laparoscopic Roux-en-Y gastric bypass surgery influenced pharmacokinetics of several drugs given as a cocktail with the highest impact observed for CYP1A2, CYP2C8 and CYP2E1 substrates. Basic Clin Pharmacol Toxicol. 2019 Aug;125(2):123-132.