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

General Information of Drug (ID: DMHG57U)

Drug Name
OPC-34712 Drug Info
Synonyms Brexpiprazole
Indication
Disease Entry ICD 11 Status REF
Major depressive disorder 6A70.3 Approved [1]
Cross-matching ID
PubChem CID
11978813
ChEBI ID
CHEBI:134716
CAS Number
CAS 913611-97-9
TTD Drug ID
DMHG57U
VARIDT Drug ID
DR01335
INTEDE Drug ID
DR0227
ACDINA Drug ID
D00076

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Modulator [2]
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Modulator [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Sodium-dependent dopamine transporter (SLC6A3) DT3BA8L SC6A3_HUMAN Approved [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [4]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [4]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
5-HT 1A receptor (HTR1A) DTT HTR1A 4.661 5.289 3.053 3.472
Dopamine D2 receptor (D2R) DTT DRD2 5.345 5.634 5.789 5.901
Sodium-dependent dopamine transporter (SLC6A3) DTP DAT1 4 2.609 5.233 3.7
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 Major depressive disorder
ICD Disease Classification 6A70.3
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
5-HT 1A receptor (HTR1A) DTT HTR1A 1.49E-05 -0.22 -0.58
Dopamine D2 receptor (D2R) DTT DRD2 2.50E-02 -0.08 -0.49
Sodium-dependent dopamine transporter (SLC6A3) DTP DAT1 2.11E-01 1.59E-02 5.57E-02
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 7.30E-01 -1.91E-02 -1.41E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.04E-02 6.29E-02 3.54E-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: 7672).
2 Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.
3 Brexpiprazole reduces hyperactivity, impulsivity, and risk-preference behavior in mice with dopamine transporter knockdown-a model of mania. Psychopharmacology (Berl). 2017 Mar;234(6):1017-1028.
4 Brexpiprazole: first global approval. Drugs. 2015 Sep;75(14):1687-97.