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

Drug dosage:

Dose	Unit	Route
0.30	g	O
0.30	g	P

ADMET properties:

Property	Value	Reference
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
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

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1972	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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	85.93	44.18	18	1235	2265	50601606
Sleep-related eating disorder	78.52	44.18	14	1239	754	50603117
Peripheral circulatory failure	62.46	44.18	11	1242	551	50603320
Syncope	51.84	44.18	32	1221	102970	50500901
General physical health deterioration	51.59	44.18	36	1217	142398	50461473
Epilepsy	45.98	44.18	18	1235	21549	50582322
Haematemesis	44.91	44.18	19	1234	27706	50576165

FDA Adverse Event Reporting System (Male)

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
Fall	94.50	45.73	67	1072	177111	29396277
General physical health deterioration	66.61	45.73	44	1095	102813	29470575
Pleurothotonus	56.56	45.73	12	1127	1026	29572362
Disorientation	53.66	45.73	25	1114	29490	29543898
Gastrointestinal hypermotility	51.11	45.73	8	1131	121	29573267
Electrocardiogram QT shortened	49.95	45.73	8	1131	141	29573247
Fracture	47.79	45.73	15	1124	6038	29567350
Epilepsy	47.64	45.73	20	1119	18412	29554976

FDA Adverse Event Reporting System (Geriatric)

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	118.87	39.20	79	2184	204346	64292123
Fall	110.48	39.20	101	2162	416725	64079744
Pleurothotonus	79.47	39.20	18	2245	2284	64494185
Systemic infection	68.21	39.20	18	2245	4303	64492166
Disorientation	56.76	39.20	31	2232	55797	64440672
Sleep-related eating disorder	56.49	39.20	11	2252	671	64495798
Peripheral circulatory failure	56.34	39.20	11	2252	680	64495789
Epilepsy	55.80	39.20	26	2237	33505	64462964
Drug interaction	51.15	39.20	63	2200	362020	64134449
Depressed level of consciousness	43.56	39.20	30	2233	81406	64415063
Syncope	41.00	39.20	38	2225	157597	64338872

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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA 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
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	5.36		PDSP
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	5.47		PDSP
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN					WOMBAT-PK
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	6.39		WOMBAT-PK

External reference:

ID	Source
D07309	KEGG_DRUG
C0066477	UMLSCUI
CHEBI:93626	CHEBI
CHEMBL1531134	ChEMBL_ID
DB09224	DRUGBANK_ID
15387	PUBCHEM_CID
2070	INN_ID
J8WA3K39B7	UNII
29961	RXNORM
006742	NDDF
441821005	SNOMEDCT_US
442519006	SNOMEDCT_US

Pharmaceutical products:

None