e-Drug3D

1794

CARIPRAZINE

INN
CARIPRAZINE

cas 839712-12-8

CLASS

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)

ROUTE (list)

ORAL

ATC code

N05AX15

PK parameters

Tmax 4.5 HOUR
PPB 94 PERCENT
t1/2 72 HOUR

Target

TARGET DOPAMINE D2 RECEPTOR
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

DrugCentral

D(2) dopamine receptor UNIPROT P14416 DRD2

5-hydroxytryptamine receptor 1A UNIPROT P08908 HTR1A

Download SDF file

Urea, N'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N-dimethyl-

Formula:
C21H32Cl2N4O

Calculated chemical properties:

MW 427.41
NB_atoms 28
XLogP 4.34
PSA 39.114
NB_HD 1
NB_HA 5
fsp3 0.67
Lipinski(0=no;1=yes) 1

FDA
NDA 204370 (pdf not found) INN (CARIPRAZINE HYDROCHLORIDE) VRAYLAR (ABBVIE) APPROVAL= AP YEAR= 2015 NEWMOLECULARENTITY
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