MELPERONE

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

Structure Search

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

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

Description
Sources: http://www.ratiopharm.de/index.php?eID=dumpFile&t=f&f=60721&g=-1&r=1894%2C1894&token=c00130080812868362409a3ab52b4a122b2af3ad

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

Condition	Modality	Highest Phase	Product
Sleep disorder 20 Sources: http://www.ratiopharm.de/index.php?eID=dumpFile&t=f&f=60721&g=-1&r=1894%2C1894&token=c00130080812868362409a3ab52b4a122b2af3ad	Primary	Approved 8429	MELPERON Approved Use Melperon is used to treat sleep disorders, confusion states, and to suppress psychomotor restlessness and excitement, especially in geriatric and psychiatric patients.
Confusional state 2 Sources: http://www.ratiopharm.de/index.php?eID=dumpFile&t=f&f=60721&g=-1&r=1894%2C1894&token=c00130080812868362409a3ab52b4a122b2af3ad	Primary	Approved 8429	MELPERON Approved Use Melperon is used to treat sleep disorders, confusion states, and to suppress psychomotor restlessness and excitement, especially in geriatric and psychiatric patients.
Psychomotor agitation 6 Sources: http://www.ratiopharm.de/index.php?eID=dumpFile&t=f&f=60721&g=-1&r=1894%2C1894&token=c00130080812868362409a3ab52b4a122b2af3ad	Primary	Approved 8429	MELPERON Approved Use Melperon is used to treat sleep disorders, confusion states, and to suppress psychomotor restlessness and excitement, especially in geriatric and psychiatric patients.

PubMed

Title	Date	PubMed
Broad sensitivity of rodent arrhythmia models to class I, II, III, and IV antiarrhythmic agents.	1989 Jun	2726785
New and old antipsychotics versus clozapine in a monkey model: adverse effects and antiamphetamine effects.	1999 Jun	10435384
Melperone in the treatment of neuroleptic-resistant schizophrenia.	2001 Dec 31	11814539
Clinical management of agitation in the elderly with tiapride.	2001 Jan	11520478
[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 antipsychotic drugs, quetiapine, iloperidone, and melperone, preferentially increase dopamine and acetylcholine release in rat medial prefrontal cortex: role of 5-HT1A receptor agonism.	2002 Nov 29	12445705
Melperone is an inhibitor of the CYP2D6 catalyzed O-demethylation of venlafaxine.	2003 Jan	12649767
The effect of melperone, an atypical antipsychotic drug, on cognitive function in schizophrenia.	2003 Jan 1	12413636
A comparison of two doses of melperone, an atypical antipsychotic drug, in the treatment of schizophrenia.	2003 Jul 1	12765745
Screening, library-assisted identification and validated quantification of fifteen neuroleptics and three of their metabolites in plasma by liquid chromatography/mass spectrometry with atmospheric pressure chemical ionization.	2003 Mar	12644990
P-glycoprotein is a factor in the uptake of dextromethorphan, but not of melperone, into the mouse brain: evidence for an overlap in substrate specificity between P-gp and CYP2D6.	2004 Dec	15582917
[The case of a 86-years old woman first diagnosed with Huntington's disease].	2004 Nov	15570530
Atypical and typical antipsychotic drug interactions with the dopamine D2 receptor.	2005 Feb	15694653
Antipsychotic drugs and QT prolongation.	2005 Sep	16096514
Cytochrome P450 2D6 dependent metabolization of risperidone is inhibited by melperone.	2006 Apr	16534635
Dose-dependent improvement of myoclonic hyperkinesia due to Valproic acid in eight Huntington's Disease patients: a case series.	2006 Feb 28	16507108
Prototypical antipsychotic drugs protect hippocampal neuronal cultures against cell death induced by growth medium deprivation.	2006 Mar 30	16573831
The effect of antipsychotic medication on sexual function and serum prolactin levels in community-treated schizophrenic patients: results from the Schizophrenia Trial of Aripiprazole (STAR) study (NCT00237913).	2008 Dec 22	19102734
[Recurrent dysregulation of body temperature during antipsychotic pharmacotherapy].	2008 Mar	17902059
Further characterization of the discriminative stimulus properties of the atypical antipsychotic drug clozapine in C57BL/6 mice: role of 5-HT(2A) serotonergic and alpha (1) adrenergic antagonism.	2009 Apr	18989659
Antipsychotics and risk of venous thromboembolism: A population-based case-control study.	2009 Aug 9	20865083
Melperone, an aytpical antipsychotic drug with clozapine-like effect on plasma prolactin: contrast with typical neuroleptics.	2009 Jul	19551763
The ABCB1 transporter gene and antidepressant response.	2009 Mar 24	20948663
Changes in weight and body mass index during treatment with melperone, clozapine and typical neuroleptics.	2010 Apr 30	20199813
Acute administration of clozapine and risperidone altered dopamine metabolism more in rat caudate than in nucleus accumbens: a dose-response relationship.	2010 Apr-Jun	21179339
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.	2010 Dec	21818443
Attenuation of phencyclidine-induced object recognition deficits by the combination of atypical antipsychotic drugs and pimavanserin (ACP 103), a 5-hydroxytryptamine(2A) receptor inverse agonist.	2010 Feb	19864614
The effect of metformin on anthropometrics and insulin resistance in patients receiving atypical antipsychotic agents: a meta-analysis.	2010 Oct	20441727
Four-digit replantation in a mentally retarded person: a case report.	2010 Sep 30	20976275

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 Created by `admin` on `Fri Dec 15 15:55:16 UTC 2023` Edited by `admin` on `Fri Dec 15 15:55:16 UTC 2023`
Record UNII	J8WA3K39B7
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MELPERONE

Official Name

English

METYLPERON

Common Name

English

MELPERONE [MI]

Common Name

English

Melperone [WHO-DD]

Common Name

English

melperone [INN]

Common Name

English

BUNIL

Brand Name

English

FG 5111

Code

English

FG-5111

Code

English

4'-FLUORO-4-(4-METHYLPIPERIDINO)BUTYROPHENONE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29710