Scroll

melperone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tranquillizers, neuroleptics, 4'-fluoro-4-piperidinobutyrophenone derivatives	1677	3575-80-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: melperone flubuperone methylperone	Molecular weight: 263.36 Formula: C16H22FNO CLOGP: 3.88 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 20.31 ALOGS: -3.73 ROTB: 5

Molecule

Description

Molfile Inchi Smiles

Synonyms:

melperone
flubuperone
methylperone

Molecular weight: 263.36
Formula: C16H22FNO
CLOGP: 3.88
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 20.31
ALOGS: -3.73
ROTB: 5

Drug dosage:

Dose	Unit	Route
0.30	g	O
0.30	g	P

ADMET properties:

Show entries

Search:

Property	Value	Reference
CL (Clearance)	46 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	3.90 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	29.98 mg/mL	Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	21.70 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	14 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

Showing 1 to 6 of 6 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1972	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Systemic infection	82.26	46.70	20	1640	4640	63482722
Sleep-related eating disorder	76.30	46.70	14	1646	837	63486525
Haematemesis	69.18	46.70	27	1633	30385	63456977
General physical health deterioration	63.90	46.70	48	1612	201354	63286008
Labelled drug-drug interaction medication error	57.33	46.70	19	1641	13380	63473982
Peripheral circulatory failure	55.88	46.70	11	1649	957	63486405
Atrial fibrillation	53.77	46.70	35	1625	116601	63370761

Showing 1 to 7 of 7 entries

Previous1Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
General physical health deterioration	122.34	40.55	73	1436	128196	34827226
Fall	89.79	40.55	72	1437	202813	34752609
Disorientation	56.90	40.55	28	1481	33160	34922262
Confusional state	56.87	40.55	48	1461	144112	34811310
Pleurothotonus	53.39	40.55	12	1497	1193	34954229
Gastrointestinal hypermotility	49.20	40.55	8	1501	138	34955284
Electrocardiogram QT shortened	48.77	40.55	8	1501	146	34955276
Fracture	44.27	40.55	15	1494	6834	34948588
Epilepsy	42.46	40.55	20	1489	21475	34933947

Showing 1 to 9 of 9 entries

Previous1Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
General physical health deterioration	175.99	38.82	118	3035	275120	79466115
Systemic infection	109.94	38.82	32	3121	9720	79731515
Fall	95.15	38.82	106	3047	487523	79253712
Pleurothotonus	75.72	38.82	18	3135	2498	79738737
Drug interaction	71.95	38.82	85	3068	415098	79326137
Haematemesis	69.13	38.82	36	3117	52228	79689007
Disorientation	60.27	38.82	35	3118	62741	79678494
Medication error	57.37	38.82	35	3118	68607	79672628
Sleep-related eating disorder	54.67	38.82	11	3142	703	79740532
Labelled drug-drug interaction medication error	51.31	38.82	24	3129	27626	79713609

Showing 1 to 10 of 21 entries

Previous1 2 3Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05AD03	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Butyrophenone derivatives

Drug Use | Suggest Off label Use Form| |View source of the data|

None

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.28	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	Ki	6.98	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	Ki	6.82	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN			WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	Ki	5.66	PDSP
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	Ki	6.72	WOMBAT-PK
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	Ki	5.68	PDSP
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	Ki	6.74	WOMBAT-PK
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	Ki	7.06	WOMBAT-PK
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	Ki	6.24	WOMBAT-PK
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN	Ki	5.62	PDSP

Showing 1 to 10 of 14 entries

Previous1 2Next

External reference:

Show entries

Search:

ID	Source
006742	NDDF
15387	PUBCHEM_CID
2070	INN_ID
29961	RXNORM
441821005	SNOMEDCT_US
442519006	SNOMEDCT_US
C0066477	UMLSCUI
CHEBI:93626	CHEBI
CHEMBL1531134	ChEMBL_ID
D07309	KEGG_DRUG

Showing 1 to 10 of 12 entries

Previous1 2Next

Pharmaceutical products:

None