e-Drug3D

808

ZIPRASIDONE


INN
ZIPRASIDONE

cas 146939-27-7
CLASS

NERVOUS SYSTEM
TREATMENT OF BIPOLAR DISORDER
ANTIPSYCHOTIC
DOPAMINE D2 (KI = 4.8 NANOMOLAR) AND D3 (KI = 7.2 NANOMOLAR) ANTAGONISTS
SEROTONIN 5HT2A (KI = 0.4 NANOMOLAR) 5HT2C (KI = 1.3 NANOMOLAR) 5HT1D (KI = 2 NANOMOLAR) ANTAGONISTS
ALPHA 1 ADRENERGIC RECEPTOR (KI = 10 NANOMOLAR) ANTAGONISTS
5HT1A RECEPTOR AGONIST (KI = 3.4 NANOMOLAR)

ROUTE (list)

ORAL INTRAMUSCULAR

ATC code

N05AE04

PK parameters

F 60 PERCENT
Tmax 7 HOUR
VD 97.5 LITER (65 KILOGRAM)
Cl 29.2 LITER / HOUR (65 KILOGRAM)
PPB 99 PERCENT
t1/2 7 HOUR

Target

TARGET ALPHA 1 ADRENERGIC RECEPTOR
5-HYDROXYTRYPTAMINE 1A RECEPTOR
D(2) DOPAMINE RECEPTOR
5-HYDROXYTRYPTAMINE 2A RECEPTOR
5-HYDROXYTRYPTAMINE 2C RECEPTOR
D(3) DOPAMINE RECEPTOR
5-HYDROXYTRYPTAMINE 1D RECEPTOR

PDB
8WTY (CRYO-EM STRUCTURE OF NORADRENALINE TRANSPORTER IN COMPLEX WITH ZIPRASIDONE)

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

Download experimental 3D coordinates of XEF with added hydrogens

DrugCentral

D(2) dopamine receptor UNIPROT P14416 DRD2

5-hydroxytryptamine receptor 2A UNIPROT P28223 HTR2A

Download SDF file 5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one

Formula:
C21H21ClN4OS

Calculated chemical properties:

MW 412.94
NB_atoms 28
XLogP 3.81
PSA 53.248
NB_HD 1
NB_HA 5
fsp3 0.33
Lipinski(0=no;1=yes) 1

FDA
NDA 020825 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) GEODON (VIATRIS) APPROVAL= AP YEAR= 2001
NDA 020919 (pdf not found) INN (ZIPRASIDONE MESYLATE) GEODON (VIATRIS) APPROVAL= AP YEAR= 2002
NDA 021483 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) GEODON (PFIZER INC) APPROVAL= AP YEAR= 2006 DISCONTINUED
NDA 077560 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) ZIPRASIDONE HYDROCHLORIDE (LUPIN PHARMS) APPROVAL= AP YEAR= 2012
NDA 077562 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) ZIPRASIDONE HYDROCHLORIDE (SANDOZ INC) APPROVAL= AP YEAR= 2012
NDA 077565 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) ZIPRASIDONE HYDROCHLORIDE (DR REDDYS LABS INC) APPROVAL= AP YEAR= 2012
NDA 077561 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) ZIPRASIDONE HYDROCHLORIDE (APOTEX) APPROVAL= AP YEAR= 2012
NDA 090348 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) ZIPRASIDONE HYDROCHLORIDE (CHARTWELL RX) APPROVAL= AP YEAR= 2012
NDA 202395 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) ZIPRASIDONE HYDROCHLORIDE (MYLAN) APPROVAL= AP YEAR= 2013 DISCONTINUED
NDA 204117 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) ZIPRASIDONE HYDROCHLORIDE (AUROBINDO PHARMA) APPROVAL= AP YEAR= 2016
NDA 204375 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) ZIPRASIDONE HYDROCHLORIDE (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2017
NDA 208988 (pdf not found) INN (ZIPRASIDONE HYDROCHLORIDE) ZIPRASIDONE HYDROCHLORIDE (ZYDUS LIFESCIENCES) APPROVAL= AP YEAR= 2017
NDA 211908 (pdf not found) INN (ZIPRASIDONE MESYLATE) ZIPRASIDONE MESYLATE (GLAND) APPROVAL= AP YEAR= 2019
NDA 216091 (pdf not found) INN (ZIPRASIDONE MESYLATE) ZIPRASIDONE MESYLATE (MSN) APPROVAL= AP YEAR= 2022

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL