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

Stem definitionDrug idCAS RN
serotonin and/or norepinephrine reuptake inhibitors, fluoxetine derivatives 2361 71620-89-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • reboxetine mesilate
  • reboxetine mesylate
  • edronax
  • reboxetine
  • norebox
  • reboxitine
A morpholine derivative that is a selective and potent noradrenaline reuptake inhibitor; it is used in the treatment of DEPRESSIVE DISORDER.
  • Molecular weight: 313.40
  • Formula: C19H23NO3
  • CLOGP: 3.06
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 39.72
  • ALOGS: -4.15
  • ROTB: 6

Drug dosage:

DoseUnitRoute
8 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 8 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.55 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 94 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.65 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.82 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1997 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N06AX18 NERVOUS SYSTEM
PSYCHOANALEPTICS
ANTIDEPRESSANTS
Other antidepressants
MeSH PA D018663 Adrenergic Agents
MeSH PA D018759 Adrenergic Uptake Inhibitors
MeSH PA D000928 Antidepressive Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D014179 Neurotransmitter Uptake Inhibitors
MeSH PA D011619 Psychotropic Drugs

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

DiseaseRelationSNOMED_IDDOID
Major depressive disorder indication 370143000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.44 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
Sodium-dependent serotonin transporter Transporter Ki 8.05 CHEMBL
Sodium-dependent noradrenaline transporter Transporter Ki 8.96 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 6.34 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 6.34 WOMBAT-PK
Sodium-dependent dopamine transporter Transporter Ki 7.22 CHEMBL
G protein-activated inward rectifier potassium channel 2 Ion channel IC50 4.19 WOMBAT-PK
Kir3.1/Kir3.2 Ion channel IC50 4.32 WOMBAT-PK
Kir3.1/Kir3.4 Ion channel IC50 4.39 WOMBAT-PK
Sodium-dependent serotonin transporter Transporter Ki 6.30 CHEMBL
Transporter Transporter Ki 7.86 CHEMBL
Transporter Transporter Ki 9.16 CHEMBL

External reference:

IDSource
4025264 VUID
N0000171792 NUI
D02573 KEGG_DRUG
98769-84-7 SECONDARY_CAS_RN
4025263 VANDF
4025264 VANDF
C0168388 UMLSCUI
CHEBI:135342 CHEBI
41X PDB_CHEM_ID
CHEMBL180101 ChEMBL_ID
CHEMBL14370 ChEMBL_ID
CHEMBL2146087 ChEMBL_ID
DB00234 DRUGBANK_ID
D000077593 MESH_DESCRIPTOR_UI
127151 PUBCHEM_CID
4808 IUPHAR_LIGAND_ID
5858 INN_ID
947S0YZ36I UNII
153494 RXNORM
006792 NDDF
321995004 SNOMEDCT_US
395859006 SNOMEDCT_US
783568009 SNOMEDCT_US

Pharmaceutical products:

None