General
Preferred name
PIMOZIDE
Synonyms
Primozida ()
McN-JR-6238 ()
Neoperidole ()
Opiran ()
Orap ()
Pimozidum ()
R6238 ()
Orap, R6238 ()
R-6238 ()
NSC-170984 ()
Pimozida ()
R-623 ()
R 6238 ()
R 623 ()
Pimozide-d4 ()
P&D ID
PD001879
CAS
2062-78-4
1803193-57-8
Tags
available
probe
drug
Approved by
FDA
First approval
1984
Drug indication
Schizophrenia
Psychosis
Drug Status
approved
Max Phase
4.0
Probe info
Probe type
calculated probe
Probe targets
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 Pimozide is a typical antipsychotic drug. (GtoPdb)
PRICE 29
DESCRIPTION Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at ¦Á1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
DESCRIPTION 5-HT2C agonist (Tocris Bioactive Compound Library)
DESCRIPTION D2-like antagonist (Tocriscreen Plus)
DESCRIPTION Ca2+ channel antagonist; antipsychotic; D2 dopamine receptor antagonist (LOPAC library)
DESCRIPTION D2-like antagonist (Tocriscreen Total)
DESCRIPTION Pimozide is a diphenylbutylpiperidine derivative and a dopamine antagonist with antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), and also inhibits STAT3 and STAT5. (BOC Sciences Bioactive Compounds)
DESCRIPTION Pimozide is an antipsychotic used to manage debilitating motor and phonic tics in patients with Tourette's Disorder. It has an ability to blockade dopaminergic receptors on neurons in the central nervous system. (Enamine Bioactive Compounds)
DESCRIPTION Pimozide (R6238) is a diphenylbutylpiperidine derivative and a dopamine antagonist with the antipsychotic property. Pimozide selectively inhibits type 2 dopaminergic receptors in the central nervous system (CNS), thereby decreasing dopamine neurotransmission and reducing the occurrence of the motor and vocal tics and delusions of parasitosis. In addition, this agent antagonizes alpha-adrenergic and 5-HT2 receptors. (TargetMol Bioactive Compound Library)
Cell lines
3
Organisms
2
Compound Sets
38
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Enamine Bioactive Compounds
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Ki Database
LINCS compound set
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
NIH Mechanistic Set
NPC Screening Collection
Prestwick Chemical Library
Probe Miner (suitable probes)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
External IDs
40
Properties
(calculated by RDKit )
Molecular Weight
461.23
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
1
Rotatable Bonds
7
Ring Count
5
Aromatic Ring Count
4
cLogP
5.86
TPSA
41.03
Fraction CSP3
0.32
Chiral centers
0.0
Largest ring
6.0
QED
0.37
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Selectivity
D2
Target
Adrenergic Receptor
dopamine
Potassium Channel
STAT
α1-adrenoceptor
CACNA1I, CALM1, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HTR1A, HTR2A, KCNA10, KCNH2
Dopamine Receptor
Parasite
5-HT Receptor,Adrenergic Receptor,Dopamine Receptor,STAT
Primary Target
Non-selective Dopamine
MOA
Antagonist
Dopamine Receptor antagonist
Indication
Tourette's disorder
Pathway
GPCR/G protein
JAK/STAT Signaling
Membrane Transporter/Ion Channel
Neuroscience
Stem Cells
Anti-infection
Neuronal Signaling
Stem Cell/Wnt
Therapeutic Class
Antipsychotic Agents
Source data