e-Drug3D

1477

ASENAPINE


INN
ASENAPINE

cas 65576-45-6
CLASS

ANTIPSYCHOTICS
5-HT2A RECEPTOR AGONIST
NERVOUS SYSTEM
SCHIZOPHRENIA
BIPOLAR DISORDER
HIGH AFFINITY FOR SEROTONIN 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5, 5-HT6, AND 5-HT7 RECEPTORS (KI VALUES OF 2.5, 4.0, 0.06, 0.16, 0.03, 1.6, 0.25, AND 0.13 NM), DOPAMINE D2, D3, D4, AND D1 RECEPTORS (KI VALUES OF 1.3, 0.42, 1.1, AND 1.4 NM), ALPHA1 AND ALPHA2-ADRENERGIC RECEPTORS (KI VALUES OF 1.2 AND 1.2 NM), AND HISTAMINE H1 RECEPTORS (KI VALUE 1.0 NM), AND MODERATE AFFINITY FOR H2 RECEPTORS (KI VALUE OF 6.2 NM)

ROUTE (list)

SUBLINGUAL TRANSDERMAL

ATC code

N05AH05

PK parameters

F 35 PERCENT (5 MILLIGRAM)
VD 1462 LITER (65 KILOGRAM)
Cl 52 LITER / HOUR
PPB 95 PERCENT
t1/2 24 HOUR

Target

TARGET 5-HT2A RECEPTOR (KI = 0.06 NANOMOLAR)
D2 RECEPTOR (KI = 1.3 NANOMOLAR)

DrugCentral

D(2) dopamine receptor UNIPROT P14416 DRD2

5-hydroxytryptamine receptor 2A UNIPROT P28223 HTR2A

Download SDF file 1H-Dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-, (3aR,12bR)-rel-

Formula:
C17H16ClNO

Calculated chemical properties:

MW 285.76
NB_atoms 20
XLogP 4.26
PSA 15.235
NB_HD 0
NB_HA 2
fsp3 0.29
Lipinski(0=no;1=yes) 1

FDA
NDA 022117 (label) INN (ASENAPINE MALEATE) SAPHRIS (ALLERGAN) APPROVAL= AP YEAR= 2009
NDA 212268 (label) INN (ASENAPINE) SECUADO (HISAMITSU) APPROVAL= AP YEAR= 2019
NDA 206098 (pdf not found) INN (ASENAPINE MALEATE) ASENAPINE MALEATE (ALEMBIC) APPROVAL= AP YEAR= 2020
NDA 206107 (pdf not found) INN (ASENAPINE MALEATE) ASENAPINE MALEATE (SIGMAPHARM LABS LLC) APPROVAL= AP YEAR= 2020
NDA 205960 (pdf not found) INN (ASENAPINE MALEATE) ASENAPINE MALEATE (BRECKENRIDGE) APPROVAL= AP YEAR= 2020

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL