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

Stem definitionDrug idCAS RN
tranquillizers, neuroleptics, 4'-fluoro-4-piperidinobutyrophenone derivatives 1677 3575-80-2

Description:

MoleculeDescription

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:

DoseUnitRoute
0.30 g O
0.30 g P

ADMET properties:

PropertyValueReference
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
S (Water solubility) 29.98 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1972 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Depressed level of consciousness 51.00 38.82 37 3116 96615 79644620
Dehydration 49.94 38.82 55 3098 248132 79493103
Peripheral circulatory failure 49.48 38.82 11 3142 1135 79740100
Epilepsy 47.95 38.82 26 3127 40834 79700401
Syncope 45.45 38.82 45 3108 179404 79561831
Restlessness 44.81 38.82 26 3127 46466 79694769
Tongue spasm 44.33 38.82 7 3146 109 79741126
Confusional state 43.58 38.82 58 3095 317939 79423296
Product monitoring error 41.66 38.82 15 3138 8891 79732344
Dementia 41.45 38.82 20 3133 24639 79716596
Hypotension 41.10 38.82 67 3086 440250 79300985

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 levelDissociation constantType (acidic/basic)
pKa1 9.28 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR Ki 6.98 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 6.82 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 5.66 PDSP
5-hydroxytryptamine receptor 2A GPCR Ki 6.72 WOMBAT-PK
5-hydroxytryptamine receptor 2C GPCR Ki 5.68 PDSP
Alpha-1A adrenergic receptor GPCR Ki 6.74 WOMBAT-PK
D(3) dopamine receptor GPCR Ki 7.06 WOMBAT-PK
Histamine H1 receptor GPCR Ki 6.24 WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR Ki 5.62 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 5.36 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 5.47 PDSP
Cytochrome P450 2D6 Enzyme WOMBAT-PK
D(4) dopamine receptor GPCR Ki 6.39 WOMBAT-PK

External reference:

IDSource
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