General
Preferred name
RISPERIDONE
Synonyms
Risperidone (mesylate) ()
Risperidone (hydrochloride) ()
R 64 766 mesylate ()
R 64 766 hydrochloride ()
R 64 766 ()
Risperidal ()
Risperidone (Risperdal) ()
3-(2-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ONE ()
Risperdal ()
R-64766 ()
Risperdal M-Tab ()
RCN-3028 ()
Risperdal Quicklet ()
R-64-766 ()
LY03004 ()
Perseris kit ()
LY-03004 ()
R-64,766 ()
RCN3028 ()
Risperdal M ()
Perseris ()
NSC-759895 ()
Risperdal Consta ()
Risperdal Consta Long Acting ()
N05AX08 ()
Risperidone-d4 ()
P&D ID
PD000218
CAS
106266-06-2
1020719-76-9
Tags
prodrug
natural product
drug
available
Approved by
EMA
FDA
First approval
1993
Drug Status
investigational
approved
Drug indication
Neuroleptic
Schizophrenia
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS The primary action of risperidone is to decrease dopaminergic and serotonergic pathway activity in the brain, therefore decreasing symptoms of schizophrenia and mood disorders [A1115, A1116, L1212].; ; Risperidone has high affinity binding to serotonergic 5-HT2A receptors versus dopaminergic D2 receptors in the brain [A1114, A1115]. Risperidone binds the D2 receptors with lower affinity than the traditional, first generation antipsychotic drugs, which bind with very high affinity. A reduction in extrapyramidal symptoms in Risperidone use is attributed to its moderate affinity for dopaminergic D2 receptors [A1119, L1212, A1117]. ; ;
HALF-LIFE 3 hours in extensive metabolizers [A31772]; Up to 20 hours in poor metabolizers [A31772];
DESCRIPTION Risperidone is an atypical antipsychotic drug, functioning as a dopamine D2, serotonin 5-HT2 and α2-adrenoceptor antagonist. (GtoPdb)
MOA Though its mechanism of action is not fully understood at this time, current focus is on the ability of risperidone to inhibit the D2 dopaminergic receptors and 5-HT2A serotonergic receptors in the brain. Schizophrenia is thought to be caused by an excess of dopaminergic D2 and serotonergic 5-HT2A activity, resulting in overactivity of central mesolimbic pathways and mesocortical pathways, respectively [A1115, A1116, A1117]. ; ; D2 dopaminergic receptors are transiently inhibited by risperidone, reducing dopaminergic neurotransmission, therefore decreasing positive symptoms of schizophrenia, such as delusions and hallucinations. Risperidone binds transiently and with loose affinity to the dopaminergic D2 receptor, with an ideal receptor occupancy of 60-70% for optimal effect [A1119, A31773]. Rapid dissociation of risperidone from the D2 receptors contributes to decreased risk of extrapyramidal symptoms (EPS), which occur with permanent and high occupancy blockade of D2 dopaminergic receptors [A1118, A1119]. Low affinity binding and rapid dissociation from the D2 receptor distinguish risperidone from the traditional antipsychotic drugs. A higher occupancy rate of D2 receptors is said to increase the risk of extrapyramidal symptoms and is therefore to be avoided [A1118, A1119, A31771]. ; ; Increased serotonergic mesocortical activity in schizophrenia results in negative symptoms, such as depression and decreased motivation [L1212, L1213]. The high affinity binding of risperidone to 5-HT2A receptors leads to a decrease in serotonergic activity. In addition, 5-HT2A receptor blockade results in decreased risk of extrapyramidal symptoms, likely by increasing dopamine release from the frontal cortex, and not the nigrostriatal tract. Dopamine level is ; therefore not completely inhibited [A1117, A1119]. Through the above mechanisms, both serotonergic and D2 blockade by risperidone are thought to synergistically work to decrease the risk of extrapyramidal symptoms. ; ; Risperidone has also been said to be an antagonist of alpha-1 (α1) alpha-2 (α2) receptors, and histamine (H1) receptors [L1212]. Blockade of these receptors is thought to improve symptoms of schizophrenia, however the exact mechanism of action on these receptors is not fully understood at this time [L1212, L1213].
DESCRIPTION Potent and selective NK1 antagonist (Tocris Bioactive Compound Library)
Cell lines
4
Organisms
2
Compound Sets
37
AdooQ Bioactive Compound Library
A10797
Axon Medchem Screening Library
1454
Cayman Chemical Bioactives
13629
10010570
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
CHEMBL85
ChEMBL Drugs
CHEMBL85
Concise Guide to Pharmacology 2017/18
96
Concise Guide to Pharmacology 2019/20
96
Concise Guide to Pharmacology 2021/22
96
Concise Guide to Pharmacology 2023/24
96
Drug Repurposing Hub
DrugBank
DB00734
DrugBank Approved Drugs
DB00734
DrugCentral
2389
DrugCentral Approved Drugs
2389
DrugMAP
DMN6DXL
DrugMAP Approved Drugs
DMN6DXL
DrugMatrix
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS101648
Guide to Pharmacology
96
Ki Database
RISPERIDONE
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL85
MedChem Express Bioactive Compound Library
HY-11018
Natural product-based probes and drugs
NCATS Inxight Approved Drugs
L6UH7ZF8HC
NIH Clinical Collections (NCC)
NPC Screening Collection
Other bioactive compounds
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
Risperidone(Risperdal)
TargetMol Bioactive Compound Library
T0351
The Spectrum Collection
Tocris Bioactive Compound Library
2865
VGSC-DB
NA0061
ZINC Tool Compounds
ZINC000000538312
External IDs
66
Properties
(calculated by RDKit )
Molecular Weight
410.21
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
0
Rotatable Bonds
4
Ring Count
5
Aromatic Ring Count
3
cLogP
3.59
TPSA
64.16
Fraction CSP3
0.52
Chiral centers
0.0
Largest ring
6.0
QED
0.66
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Dopamine Receptor
5-HT Receptor
Dopamine D2 receptor
5-hydroxytryptamine receptor 1D
5-hydroxytryptamine receptor 1B
Serotonin 2a (5-HT2a) receptor
Serotonin 2c (5-HT2c) receptor
5-HT2A
??2C-adrenergic receptor
D2
D2L
D3
ADRA1A, ADRA1B, ADRA1D, ADRA2A, ADRA2B, ADRA2C, DRD1, DRD2, DRD3, DRD4, HRH1, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2C, HTR6, HTR7
Atypical antipsychotic
P-glycoprotein
Pathway
GPCR/G protein
Neuronal Signaling
Neuroscience
Membrane Transporter/Ion Channel
MOA
serotonin receptor antagonist
Dopamine Receptor antagonist
alpha adrenergic receptor antagonist
Antagonist
dopamine receptor antagonist, serotonin receptor antagonist
Primary Target
5-HT2A Receptors
Indication
schizophrenia, bipolar disorder, irritability
Therapeutic Indication
Neuroleptic
Therapeutic Class
CNS & PNS
Antipsychotic Agents
VGSC Target
Nav1.5
Source data