MELPERONE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H22FNO
Molecular Weight	263.3504
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC1CCN(CCCC(=O)C2=CC=C(F)C=C2)CC1

InChI

InChIKey=DKMFBWQBDIGMHM-UHFFFAOYSA-N

InChI=1S/C16H22FNO/c1-13-8-11-18(12-9-13)10-2-3-16(19)14-4-6-15(17)7-5-14/h4-7,13H,2-3,8-12H2,1H3

HIDE SMILES / InChI

Molecular Formula	C16H22FNO
Molecular Weight	263.3504
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

Melperone is an antipsychotic drug which is used in Europe for the treatment of sleep disorders, agitation and confusion states. The exact mechanism of melperone action is unknown.

CNS Activity

Approval Year

Conditions

Conditions

Condition	Modality	Highest Phase	Product
Sleep disorder 25	Primary	Approved 8,583	MELPERON
Confusional state 2	Primary	Approved 8,583	MELPERON
Psychomotor agitation 6	Primary	Approved 8,583	MELPERON

C_max

Value	Dose	Analyte	Population
43 nM	25 mg single, oral	MELPERONE plasma	Homo sapiens
100 nM	50 mg single, oral	MELPERONE plasma	Homo sapiens
340 nM	100 mg single, oral	MELPERONE plasma	Homo sapiens
206 nM	50 mg single, intramuscular	MELPERONE plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
218 nM × h	25 mg single, oral	MELPERONE plasma	Homo sapiens
478 nM × h	50 mg single, oral	MELPERONE plasma	Homo sapiens
1490 nM × h	100 mg single, oral	MELPERONE plasma	Homo sapiens
211 nM × h	10 mg single, intravenous	MELPERONE plasma	Homo sapiens
523 nM × h	20 mg single, intravenous	MELPERONE plasma	Homo sapiens
570 nM × h	50 mg single, intramuscular	MELPERONE plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
4 h	25 mg single, oral	MELPERONE plasma	Homo sapiens
4.3 h	50 mg single, oral	MELPERONE plasma	Homo sapiens
2.9 h	100 mg single, oral	MELPERONE plasma	Homo sapiens
3.2 h	10 mg single, intravenous	MELPERONE plasma	Homo sapiens
2.8 h	20 mg single, intravenous	MELPERONE plasma	Homo sapiens
6.6 h	50 mg single, intramuscular	MELPERONE plasma	Homo sapiens

Doses

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Dose	Population	Adverse events
100 mg 3 times / day multiple, oral Highest studied dose	unhealthy, ADULT	Other AEs: extrapyramidal side effects...
100 mg 4 times / day multiple, oral Highest studied dose	unhealthy, ADULT

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AEs

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AE	Significance	Dose	Population
extrapyramidal side effects	4 patients	100 mg 3 times / day multiple, oral Highest studied dose	unhealthy, ADULT

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Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1,087 inhibitor 2,252	inhibitor 2,438	inhibitor 2,507	inhibitor 2,217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
MRP3 246 MRP4 290 MRP2 499 BSEP 550 CYP1A2 2,153 CYP2C19 2,057 CYP19A1 429	P-gp 2,052

Drug as perpetrator

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Target	Modality	Activity
BSEP 554	inhibitor 4,027	no [IC50 >133 uM]
MRP2 625	inhibitor 4,027	no [IC50 >133 uM]
MRP3 326	inhibitor 4,027	no [IC50 >133 uM]
MRP4 345	inhibitor 4,027	no [IC50 >133 uM]
CYP19A1 430	inhibitor 4,027	no

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Drug as victim

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Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2,052	substrate 4,014	no

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Tox targets

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Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2,263	inhibitor 2,237

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PubMed

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Title	Date	PubMed
Broad sensitivity of rodent arrhythmia models to class I, II, III, and IV antiarrhythmic agents.	1989 Jun	2726785
Melperone in the treatment of neuroleptic-resistant schizophrenia.	2001 Dec 31	11814539
[Pharmacotherapeutical approaches to insomnia patients with cardiac diseases and after heart transplantation].	2001 Oct	11757467
Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor.	2001 Oct	11561066
Atypical and typical antipsychotic drug interactions with the dopamine D2 receptor.	2005 Feb	15694653

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Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose of melperone (in form of hydrochloride salt) is 25-75 mg/day. In the case of restless and confused patients the drug is given at a dose of 50-100 mg at the beginning of the treatment. The dose can be increased up to 200 mg if necessary. In severe disorders of confusion and confusion with aggression and hallucinatory conditions, the daily dose can be increased to up to 400 mg melperone HCl.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical
Record UNII	J8WA3K39B7
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BUNIL

Preferred Name

English

MELPERONE

Official Name

English

METYLPERON

Common Name

English

MELPERONE [MI]

Common Name

English

Melperone [WHO-DD]

Common Name

English

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Classification Tree

Code System

Code

Agent Affecting Nervous System

NCI_THESAURUS

C29710

Butyrophenone derivatives

WHO-ATC

N05AD03

Butyrophenone derivatives

WHO-VATC

QN05AD03

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Code System

Code

Type

Description

ChEMBL

CHEMBL1531134

PRIMARY

CAS

3575-80-2

PRIMARY

MESH

C008522

PRIMARY

SMS_ID

100000081468

PRIMARY

RXCUI

29961

PRIMARY

RxNorm

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Related Record

Type

Details


					88G640374K

MELPERONE HYDROCHLORIDE

SALT/SOLVATE -> PARENT


					50U1BO5G5P

ALPHA-2A ADRENERGIC RECEPTOR

TARGET -> AGONIST

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Related Record

Type

Details


					J8WA3K39B7

MELPERONE

ACTIVE MOIETY

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SMILES

InChI

CNS Activity

Approval Year

Conditions

Cmax

AUC

T1/2

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

PubMed

Patents

Sample Use Guides

C_max

T_1/2

Drug as perpetrator