General
Preferred name
MELPERONE
Synonyms
Melperone hydrochloride ()
Metylperon ()
Melperone (hydrochloride) ()
Melperona ()
Bunil ()
FG-5111 ()
FG 5111 ()
Melperone-d4 (hydrochloride) ()
P&D ID
PD008997
CAS
1622-79-3
3575-80-2
1219798-80-7
Tags
available
drug
First approval
1972
Drug Status
approved
investigational
Max Phase
3.0
Drug indication
Psychosis
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
TOXICITY
An overdose of Melperone may result in cardiac arrhythmias [T110, A318622].
DESCRIPTION
Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, ¦Á1-adrenergic, and ¦Á2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ??of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly[1][2][3][4].
PRICE
29
DESCRIPTION
5-HT2A/D2 receptor antagonist; neuroleptic
(Tocriscreen Plus)
DESCRIPTION
5-HT2A/D2 receptor antagonist; neuroleptic
(Tocriscreen Total)
DESCRIPTION
Melperone demonstrates antagonist activity at D2 dopaminergic and 5HT2A serotonergic receptors. Melperone is an atypical antipsychotic of the butyrophenone chemical class, making it structurally related to the typical antipsychotic haloperidol. It is used for the treatment of schizophrenia, sleep, disorders, agitation and mentally confused states.
(Enamine Bioactive Compounds)
DESCRIPTION
Melperone, a butyrophenone tranquillizer, caused bradycardia in vivo and in vitro.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
19
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugCentral
DrugCentral Approved Drugs
DrugMatrix
Enamine Bioactive Compounds
Enamine BioReference Compounds
Ki Database
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
ReFrame library
TargetMol Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
47
Molecular Weight
263.17
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
0
Rotatable Bonds
5
Ring Count
2
Aromatic Ring Count
1
cLogP
3.52
TPSA
20.31
Fraction CSP3
0.56
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)
Target Type
7-TM Receptors
Member status
virtual
MOA
DRD2 antagonist
dopamine receptor antagonist, serotonin receptor antagonist
Target
DRD2, HTR2A
5-HT Receptor
Adrenergic Receptor
Cytochrome P450
Dopamine Receptor
Indication
psychosis
Pathway
GPCR/G protein
Metabolic Enzyme/Protease
Neuronal Signaling
Source data
