e-Drug3D

873

APOMORPHINE

INN
APOMORPHINE

cas 58-00-4

CLASS

NERVOUS SYSTEM
ANTIDYSKINETICS
ANTIPARKINSON AGENTS
NON-ERGOLINE DOPAMINE AGONIST D4 (KI = 4.4 NANOMOLAR) D2 (KI = 35 NANOMOLAR) D3 (KI = 26 NANOMOLAR) D5 (KI = 15 NANOMOLAR)

ROUTE (list)

SUBCUTANEOUS SUBLINGUAL

ATC code

G04BE07
N04BC07

PK parameters

F 100 PERCENT
VD 218 LITER
Cl 223 LITER / HOUR
PPB 94 PERCENT
t1/2 0.66 HOUR

Solubility

SOLUBLE IN WATER

Target

TARGET DOPAMINE D2 RECEPTOR

PDB
7JVQ (CRYO-EM STRUCTURE OF APOMORPHINE-BOUND DOPAMINE RECEPTOR 1 IN COMPLEX WITH GS PROTEIN)

Ligand code = OR9 (link to the list of PDB complexes)

Download experimental 3D coordinates of OR9 with added hydrogens

DrugCentral

D(2) dopamine receptor UNIPROT P14416 DRD2

Download SDF file

4H-Dibenzo[de,g]quinoline-10,11-diol, 5,6,6a,7-tetrahydro-6-methyl-, (6aR)-

Formula:
C17H17NO2

Calculated chemical properties:

MW 267.32
NB_atoms 20
XLogP 2.85
PSA 43.891
NB_HD 2
NB_HA 3
fsp3 0.29
Lipinski(0=no;1=yes) 1

FDA
NDA 021264 (label) INN (APOMORPHINE HYDROCHLORIDE) APOKYN (MDD US) APPROVAL= AP YEAR= 2004 NEWMOLECULARENTITY
NDA 210875 (label) INN (APOMORPHINE HYDROCHLORIDE) KYNMOBI (SUMITOMO PHARMA AM) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 212025 (pdf not found) INN (APOMORPHINE HYDROCHLORIDE) APOMORPHINE HYDROCHLORIDE (TP ANDA HOLDINGS) APPROVAL= AP YEAR= 2022
NDA 214056 (label) INN (APOMORPHINE HYDROCHLORIDE) ONAPGO (MDD US) APPROVAL= AP YEAR= 2025