1795
NERVOUS SYSTEM
ANTIPSYCHOTIC
TREATMENT OF SCHIZOPHRENIA
PARTIAL AGONIST DOPAMINE D2 RECEPTOR
PARTIAL AGONIST SEROTONIN 5-HT1A RECEPTOR
ANTAGONIST 5-HT2A RECEPTOR
HISTAMINE H1 RECEPTOR
-
ATC code
N05AX15
Cmax 10 NANOMOLAR
PPB 94 PERCENT
TARGET DOPAMINE D2 RECEPTOR
5-HT1A RECEPTOR
D(2) dopamine receptor UNIPROT P14416 DRD2
5-hydroxytryptamine receptor 1A UNIPROT P08908 HTR1A
Formula:
C20H30Cl2N4O
Calculated chemical properties:
NB_atoms 27
XLogP 3.99
PSA 52.494
NB_HD 2
NB_HA 5
fsp3 0.65
Lipinski(0=no;1=yes) 1
-
1794
NERVOUS SYSTEM
ANTIPSYCHOTIC
TREATMENT OF SCHIZOPHRENIA
PARTIAL AGONIST DOPAMINE D2 RECEPTOR (KI = 0.49 NANOMOLAR)
PARTIAL AGONIST SEROTONIN 5-HT1A RECEPTOR (KI = 2.6 NANOMOLAR)
ANTAGONIST 5-HT2A RECEPTOR (KI = 18.8 NANOMOLAR)
HISTAMINE H1 RECEPTOR (KI = 23.2 NANOMOLAR)
ORAL
ATC code
N05AX15
Tmax 4.5 HOUR
Cmax 20 NANOMOLAR
PPB 94 PERCENT
t1/2 72 HOUR
5-HT1A RECEPTOR
PDB
7VOD (CRYSTAL STRUCTURE OF 5-HT2AR IN COMPLEX WITH CARIPRAZINE)
Ligand code = 7RU (link to the list of PDB complexes)
Download experimental 3D coordinates of 7RU with added hydrogens
D(2) dopamine receptor UNIPROT P14416 DRD2
5-hydroxytryptamine receptor 1A UNIPROT P08908 HTR1A
Formula:
C21H32Cl2N4O
Calculated chemical properties:
NB_atoms 28
XLogP 4.34
PSA 39.114
NB_HD 1
NB_HA 5
fsp3 0.67
Lipinski(0=no;1=yes) 1
NDA 204370 (label) INN (CARIPRAZINE HYDROCHLORIDE) VRAYLAR (ABBVIE) APPROVAL= AP YEAR= 2015
NDA 213932 (pdf not found) INN (CARIPRAZINE HYDROCHLORIDE) CARIPRAZINE HYDROCHLORIDE (SUN PHARM) APPROVAL= AP YEAR= 2022 DISCONTINUED
NDA 213984 (pdf not found) INN (CARIPRAZINE HYDROCHLORIDE) CARIPRAZINE HYDROCHLORIDE (ZYDUS) APPROVAL= AP YEAR= 2022 DISCONTINUED
NDA 213982 (pdf not found) INN (CARIPRAZINE HYDROCHLORIDE) CARIPRAZINE HYDROCHLORIDE (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2025 DISCONTINUED