General
Preferred name
SPIPERONE
Synonyms
SPIPERONE HYDROCHLORIDE ()
Spiroperidol ()
Spiropitan ()
[3H]spiperone ()
Spiperone (hydrochloride) ()
Spiroperidol (hydrochloride) ()
[3H]spiperone ()
R-5147 ()
NSC-170983 ()
R 5147 ()
Espiperona ()
P&D ID
PD001491
CAS
749-02-0
2022-29-9
Tags
available
drug
First approval
1969
Drug indication
Discovery agent
Drug Status
approved
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Spiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases[1][2][3][4].
PRICE 50
DESCRIPTION Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective ¦Á1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities[1][2][3][4][5].
DESCRIPTION Spiperone (Spiropitan) is a spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA. (TargetMol Bioactive Compound Library)
DESCRIPTION Selective D2 dopamine receptor antagonist. (LOPAC library)
DESCRIPTION 5-HT2A antagonist. Also D2-like antagonist (Tocriscreen Total)
DESCRIPTION Spiperone hydrochloride is a 5-HT2A and selective dopamine D2 receptor antagonist (Ki = 0.06, 0.6, 0.08, ~ 350, ~ 3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) used as an antipsychotic. It also acts as an activator of calcium-activated chloride channels (EC50 = 9.3 µM). (BOC Sciences Bioactive Compounds)
Cell lines
0
Organisms
4
Compound Sets
23
BOC Sciences Bioactive Compounds
spiperone-hydrochloride-cas-2022-29-9-item-170546
ChEMBL Drugs
CHEMBL267930
Concise Guide to Pharmacology 2017/18
3300
Concise Guide to Pharmacology 2019/20
3300
Concise Guide to Pharmacology 2021/22
3300
Concise Guide to Pharmacology 2023/24
3300
Drug Repurposing Hub
DrugBank
DB17056
DrugCentral
2470
DrugCentral Approved Drugs
2470
DrugMAP
DMWHEV8
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
EOS102379
Guide to Pharmacology
3300
99
Ki Database
SPIPERONE
Spiroperidol
LOPAC library
MedChem Express Bioactive Compound Library
HY-B1371
HY-B1371A
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
TargetMol Bioactive Compound Library
T0280
The Spectrum Collection
Tocriscreen Total
External IDs
40
Properties
(calculated by RDKit )
Molecular Weight
395.2
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
2
cLogP
3.22
TPSA
52.65
Fraction CSP3
0.39
Chiral centers
0.0
Largest ring
6.0
QED
0.76
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
D2
Target
dopamine
ADRA1A, ADRA1B, ADRA1D, DRD1, DRD2, DRD3, DRD4, DRD5, HTR1A, HTR1D, HTR2A, HTR2B, HTR2C, HTR6, HTR7
5-HT Receptor
Adrenergic Receptor
Chloride channel
Dopamine Receptor
Wnt
Indication
schizophrenia
MOA
Dopamine Receptor antagonist
Pathway
GPCR/G protein
Membrane Transporter/Ion Channel
Neuronal Signaling
Stem Cell/Wnt
Neuroscience
Source data