2185
NERVOUS SYSTEM
ANTIPSYCHOTIC
BIPOLAR I DISORDER
DOPAMINE TYPE 2 (D2) AND SEROTONIN TYPE 2 (5-HT2) ANTAGONISM
ORAL
ATC code
Tmax 4 HOUR
VD 2029 LITER
Cl 50.5 LITER / HOUR
PPB 92 PERCENT
t1/2 26 HOUR
TARGET DOPAMINE TYPE 2 RECEPTOR
SEROTONIN TYPE 2 (5-HT2) RECEPTOR
-
Formula:
C24H29FN2O4
Calculated chemical properties:
NB_atoms 31
XLogP 4.68
PSA 71.824
NB_HD 1
NB_HA 6
fsp3 0.46
Lipinski(0=no;1=yes) 1
1471
ANTIPSYCHOTIC
DOPAMINE ANTAGONIST
SEROTONIN ANTOGONIST
SCHIZOPHRENIA
NERVOUS SYSTEM
SEROTONIN 5-HT2A DOPAMINE D2 AND D3 RECEPTORS (KI VALUES OF 5.6, 6.3, 7.1,NM, RESPECTIVELY). MODERATE AFFINITY FOR DOPAMINE D4, SEROTONIN 5-HT6 AND 5-HT7RECEPTORS AND NOREPINEPHRINE NEAPLHA1 RECEPTORS (KI VALUES OF 25, 43, 22, AND 36 NM RESPECTIVELY), AND LOW AFFINITY FOR THE SEROTONIN 5HT1A, DOPAMINE D1, AND HISTAMINE H1 RECEPTORS (KI VALUES OF 168, 216 AND 473 NM, RESPECTIVELY). NO APPRECIABLE AFFINITY (KI>1000 NM) FOR CHOLINERGIC MUSCARINIC RECEPTORS.
ORAL
ATC code
N05AX14
Tmax 2 HOUR
VD 2070 LITER
Cl 74.5 LITER / HOUR
PPB 95 PERCENT
t1/2 18 HOUR
PRACTICALLY INSOLUBLE IN WATER
TARGET DOPAMINE D2 (KI = 6.3 NANOMOLAR)
SEROTONIN 5-HT2A (KI = 5.6 NANOMOLAR)
DOPAMINE D3 (KI = 7.1 NANOMOLAR)
D(2) dopamine receptor UNIPROT P14416 DRD2
5-hydroxytryptamine receptor 2A UNIPROT P28223 HTR2A
Formula:
C24H27FN2O4
Calculated chemical properties:
NB_atoms 31
XLogP 4.83
PSA 68.947
NB_HD 0
NB_HA 6
fsp3 0.42
Lipinski(0=no;1=yes) 1
NDA 022192 (label) INN (ILOPERIDONE) FANAPT (VANDA PHARMS INC) APPROVAL= AP YEAR= 2009
NDA 207231 (pdf not found) INN (ILOPERIDONE) ILOPERIDONE (INVENTIA) APPROVAL= AP YEAR= 2016 DISCONTINUED
NDA 207409 (pdf not found) INN (ILOPERIDONE) ILOPERIDONE (ALEMBIC PHARMS LTD) APPROVAL= TA YEAR= 2018
NDA 207098 (pdf not found) INN (ILOPERIDONE) ILOPERIDONE (TARO) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 206890 (pdf not found) INN (ILOPERIDONE) ILOPERIDONE (LUPIN) APPROVAL= AP YEAR= 2022 DISCONTINUED